5-HT receptor

Short description: Class of transmembrane proteins

The 5-HT1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation

5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.[1][2][3] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[4]

Serotonin receptors are found in almost all animals and are even known to regulate longevity and behavioral aging in the primitive nematode, Caenorhabditis elegans.[5][6]

## Contents

* 1 Classification
* 1.1 Families
* 1.2 Subtypes
* 2 Expression patterns
* 3 5-HT1-like
* 4 References
* 5 External links

## Classification

5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in the central and peripheral nervous systems.[1][2] They can be divided into 7 families of G protein-coupled receptors which activate an intracellular second messenger cascade to produce an excitatory or inhibitory response. The exception to this is the 5-HT3 receptor which is a ligand-gated ion channel. In 2014, a novel 5-HT receptor was isolated from the small white butterfly, Pieris rapae, and named pr5-HT8. It does not occur in mammals and shares relatively low similarity to the known 5-HT receptor classes.[7]

### Families

Family | Type | Mechanism | Potential

|
|
|

5-HT1 | Gi/Go-protein coupled. | Decreasing cellular levels of cAMP. | Inhibitory
5-HT2 | Gq/G11-protein coupled. | Increasing cellular levels of IP3 and DAG. | Excitatory
5-HT3 | Ligand-gated Na+ and K+ cation channel. | Depolarizing plasma membrane. | Excitatory
5-HT4 | Gs-protein coupled. | Increasing cellular levels of cAMP. | Excitatory
5-HT5 | Gi/Go-protein coupled.[8] | Decreasing cellular levels of cAMP. | Inhibitory
5-HT6 | Gs-protein coupled. | Increasing cellular levels of cAMP. | Excitatory
5-HT7 | Gs-protein coupled. | Increasing cellular levels of cAMP. | Excitatory

### Subtypes

The 7 general serotonin receptor classes include a total of 14 known serotonin receptors.[9] The 15th receptor 5-HT1P has been distinguished on the basis of functional and radioligand binding studies, its existence has never been definitely affirmed or refuted.[10][11] The specific types have been characterized as follows:[12][13][14]

Information on serotonin receptors (human isoforms if nothing else is stated)

Receptor  | First cloned – PDB entries | Gene(s)  | Distribution  | Function  | Agonists | Antagonists | Uses of drugs that act on this receptor
Blood vessels | CNS | GI Tract | Platelets | PNS | Smooth Muscle
5-HT1A | 1987 –

* 7e2x
* 7e2y
* 7e2z

* HTR1A

| Yes  | Yes  | No  | No  | No  | No  |

* Addiction[15][16][17]
* Aggression[18]
* Anxiety[19]
* Appetite[20]
* Autoreceptor
* Blood Pressure[21][22]
* Cardiovascular Function[23]
* Emesis[24]
* Heart Rate[21][22]
* Impulsivity[25]
* Memory[26][27]
* Mood[28]
* Nausea[24]
* Nociception[29]
* Penile Erection[30]
* Pupil Dilation[31]
* Respiration[32]
* Sexual Behavior[33]
* Sleep[34]
* Sociability[35]
* Thermoregulation[36]
* Vasoconstriction[37]

Selective (for 5-HT1A over other 5-HT receptors)

* Vilazodone (Viibryd)
* F-15,599 (research compound, highly potent and selective for 5-HT1A)
* Flesinoxan (potent, EC50 = 24 nM)
* Gepirone (partial agonist, Ki = 70 nM)
* Haloperidol
* Ipsapirone (partial agonist, Ki = 12.1 nM)
* Quetiapine
* Trazodone (SARI, selective in the sense that on all other 5-HT receptors it acts as either an antagonist or has no action. Kd = 78 nM)
* Yohimbine (unselective partial agonist)
* Tandospirone (potent and selective partial agonist)

Nonselective

* 5-CT (potent – Ki = 250 ± 50 pM)
* 8-OH-DPAT (potent)
* Aripiprazole (atypical antipsychotic)
* Asenapine (atypical antipsychotic)
* Buspirone[38] (partial agonist)
* Vortioxetine (high-efficacy partial agonist)[39]
* Ziprasidone (partial agonist, Ki = 3.4 nM)
* Methylphenidate (weak agonist)

* BMY 7378
* Cyanopindolol
* Iodocyanopindolol
* Lecozotan
* Methiothepin
* Methysergide[40]
* NAN-190
* Nebivolol
* Nefazodone
* WAY-100,135
* WAY-100,635
* Mefway

* Analgesics (agonists)
* Antidepressants (post-synaptic receptor agonists and pre-synaptic autoreceptor antagonists serve as antidepressants)
* Anxiolytics[41] (agonist and antagonist)

5-HT1B | 1992 –

* 6g79

* HTR1B

| Yes  | Yes  | No  | No  | No  | No  |

* Addiction[42]
* Aggression[18]
* Anxiety[43][44][45]
* Autoreceptor
* Learning[46]
* Locomotion[47]
* Memory[46]
* Mood[45]
* Penile Erection[30]
* Sexual Behavior[33]
* Vasoconstriction

* 5-CT
* CGS-12066A
* CP-93,129
* CP-94,253
* Dihydroergotamine
* Eltoprazine
* Ergotamine
* Methysergide
* RU 24969
* TFMPP
* Triptans[38] (antimigraine[38])
* Zolmitriptan
* Eletriptan
* Sumatriptan
* Vortioxetine (partial agonist, Ki = 33 nM)[39]

* Alprenolol
* AR-A000002
* Asenapine
* Cyanopindolol
* GR-127,935
* Iodocyanopindolol
* Isamoltane
* Metergoline
* Methiothepin
* Oxprenolol
* Pindolol
* Propranolol
* SB-216,641
* Yohimbine

* Migraines (e.g., triptans)

5-HT1D | 1991 –

* 7e32

* HTR1D

| Yes  | Yes  | No  | No  | No  | No  |

* Anxiety[48][49]
* Autoreceptor
* Locomotion[47]
* Vasoconstriction

* 5-CT
* CP-135,807
* Dihydroergotamine
* Ergotamine
* Methysergide
* Triptans[38] (antimigraine[38])
* Almotriptan
* Eletriptan
* Frovatriptan
* Naratriptan
* Rizatriptan
* Sumatriptan
* Zolmitriptan
* Yohimbine

* BRL-15572
* GR-127,935
* Ketanserin
* Metergoline
* Methiothepin
* Rauwolscine
* Ritanserin
* Vortioxetine (Ki = 54 nM)[39]
* Ziprasidone

* Migraines (e.g., triptans)

5-HT1E | 1992 –

* 7e33

* HTR1E

| Yes  | Yes  | No  | No  | No  | No  |  |

* BRL-54443

|  |

* None known

5-HT1F | 1993 –

* 7exd

* HTR1F

| No  | Yes  | No  | No  | No  | No  |

* Migraine

* BRL-54443
* Lasmiditan
* LY-334,370
* Naratriptan
* Eletriptan

|  |

* None known

5-HT1P | Not cloned  |  | No  | No  | Yes  | No  | No  | No  |

* Peristalsis[11][50]

* 5-OHIP[11][51]
* 2-Methyl-5-HT[52]
* 5-BOHIP[53]

* 5-HTP-DP[11]

* None known

5-HT2A | 1988  |

* HTR2A

| Yes  | Yes  | Yes  | Yes  | Yes  | Yes  |

* Addiction (potentially modulating)[54]
* Anxiety[55]
* Appetite
* Cognition
* Imagination
* Learning
* Memory
* Mood
* Perception
* Sexual Behavior[56]
* Sleep[57]
* Thermoregulation[58]
* Vasoconstriction[59]

* 25I-NBOMe (Full agonist)
* 5-MeO-DMT
* BZP
* Bufotenin
* DMT
* DOM
* Ergonovine
* Lisuride
* LSD
* Mescaline
* PNU-22394 (partial agonist)[60][61][62]
* Psilocin
* Psilocybin
* TFMPP (partial agonist or antagonist)

* Atypical antipsychotics
* Aripiprazole
* Clozapine[38]
* Olanzapine
* Quetiapine
* Risperidone
* Ziprasidone
* Asenapine
* Amitriptyline
* Clomipramine
* Cyproheptadine
* Doxepin
* Eplivanserin
* Etoperidone
* Haloperidol
* Hydroxyzine
* Iloperidone
* Ketanserin[38] (antihypertensive[38])
* Methysergide
* Mianserin
* Mirtazapine
* Nefazodone
* Pimavanserin
* Pizotifen
* Ritanserin
* Trazodone
* Yohimbine

* Atypical antipsychotics (antagonist)
* Psychedelics (agonists)
* NaSSAs (antidepressants and anxiolytics; they serve as antagonists at this site)
* Treating serotonin syndrome (antagonists; e.g., cyproheptadine)
* Sleeping aid (antagonists; e.g., trazodone)

5-HT2B | 1992  |

* HTR2B

| Yes  | Yes  | Yes  | Yes  | Yes  | Yes  |

* Anxiety[63][64][65]
* Appetite[66]
* Cardiovascular Function
* GI Motility[67]
* Sleep[57]
* Vasoconstriction

* 6-APB (full agonist)
* BW-723C86
* Fenfluramine
* MDMA
* Norfenfluramine
* PNU-22394 (partial agonist)[60][61][62]
* Ro60-0175
* Methylphenidate (weak agonist)

* Agomelatine
* Asenapine
* BZP
* Ketanserin
* Methysergide
* Ritanserin
* RS-127,445
* Tegaserod
* Yohimbine

* Migraines (antagonists)

5-HT2C | 1988  |

* HTR2C

| Yes  | Yes  | Yes  | Yes  | Yes  | Yes  |

* Addiction. (potentially modulating)[54]
* Anxiety[68][69][70]
* Appetite
* GI Motility[71]
* Heteroreceptor for norepinephrine and dopamine
* Locomotion
* Mood[69][70]
* Penile Erection[72][73]
* Sexual Behavior[56]
* Sleep[74]
* Thermoregulation[58]
* Vasoconstriction

* 2C-B (partial agonist)[75]
* A-372,159
* AL-38022A
* Aripiprazole
* Ergonovine
* Lorcaserin
* PNU-22394 (full agonist)[60][61][62]
* Ro60-0175
* TFMPP
* Trazodone[38] (hypnotic[38])
* YM-348

* Agomelatine[38] (antidepressant[38])
* Amitriptyline
* Asenapine
* Clomipramine
* Clozapine[38] (antipsychotic[38])
* Cyproheptadine
* Dimebolin
* Eltoprazine
* Etoperidone
* Fluoxetine
* Haloperidol
* Iloperidone
* Ketanserin[38] (antihypertensive[38])
* Lisuride
* Methysergide[76]
* Mianserin
* Mirtazapine
* Nefazodone
* Olanzapine
* Paroxetine
* Quetiapine
* Risperidone
* Ritanserin
* SB-242084
* Tramadol
* Trazodone
* Ziprasidone

* Antidepressant (antagonists; e.g., agomelatine, fluoxetine, mirtazapine)
* Orexigenic (e.g., mirtazapine, clozapine and olanzapine; antagonists)
* Anorectic (Lorcaserin; agonist)
* Antipsychotic (Vabicaserin; agonists)

5-HT3 | 1993  |

* HTR3A
* HTR3B
* HTR3C
* HTR3D
* HTR3E

| No  | Yes  | Yes  | No  | Yes  | No  |

* Addiction
* Anxiety
* Emesis
* GI Motility[77]
* Learning[78]
* Memory[78]
* Nausea

* 2-Methyl-5-HT
* BZP
* Quipazine
* RS-56812

* Alosetron
* Several antiemetics[38]
* Dolasetron
* Ondansetron[38]
* Granisetron
* Tropisetron
* Clozapine
* Memantine
* Metoclopramide
* Mianserin
* Mirtazapine
* Olanzapine
* Quetiapine
* Vortioxetine (Ki = 3.7 nM)[39]

* Antiemetic
* Antidepressant (e.g., mirtazpine)
* antipsychotic (e.g., olanzapine, quetiapine)

5-HT4 | 1995  |

* HTR4

| No  | Yes  | Yes  | No  | Yes  | No  |

* Anxiety[79][80]
* Appetite[81][82]
* GI Motility
* Learning[83][84]
* Memory[83][84][85]
* Mood[86][87]
* Respiration[88]

* 5-MT
* BIMU-8
* Cinitapride
* Cisapride[38] (gastroprokinetic)
* Dazopride
* Metoclopramide
* Mosapride
* Prucalopride
* RS-67333
* Renzapride
* Tegaserod
* Zacopride

* L-Lysine[79]
* Piboserod

* Gastroprokinetics (e.g., Tegaserod)

5-HT5A | 1994

* 7UM4
* 7UM5
* 7UM6
* 7UM7

* HTR5A

| No  | Yes  | No  | No  | No  | No  |

* Autoreceptor
* Locomotion[89]
* Sleep[90]

* 5-CT
* Ergotamine
* Lisuride (partial)[91]
* Methylergometrine (full)[91]
* Valerenic Acid (partial agonist)[90]

* Asenapine
* Dimebolin
* Methiothepin
* Ritanserin
* SB-699,551
* SB-699,551-A
* MS112[91]

* None thus far

5-HT5B | 1993  |

* HTR5BP

| No  | No  | No  | No  | No  | No  |

Functions in rodents,
pseudogene in humans

|  |  |

* None thus far

5-HT6 | 1993  |

* HTR6

| No  | Yes  | No  | No  | No  | No  |

* Anxiety[92][93]
* Cognition[94]
* Learning[95]
* Memory[95]
* Mood[93][96]

* EMD-386,088
* EMDT
* WAY-181,187
* WAY-208,466
* E-6837
* N-(inden-5-yl)imidazothiazole-5-sulfonamide (43)[97]

* Amitriptyline
* Aripiprazole
* Asenapine
* Clomipramine
* Clozapine
* Dimebolin
* EGIS-12233
* Haloperidol
* Iloperidone
* MS-245
* Olanzapine
* Ro04-6790
* SB-258,585
* SB-271,046[98]
* SB-357,134
* SB-399,885

* Antidepressant (antagonists and agonists)
* Anxiolytic (antagonists and agonist)
* Nootropic (antagonists)
* Anorectic (antagonists)

5-HT7 | 1993  |

* HTR7

| Yes  | Yes  | Yes  | No  | No  | No  |

* Anxiety[99][100]
* Autoreceptor
* Memory[101][102]
* Mood[99][100]
* Respiration[32][103]
* Sleep[99][103][104]
* Thermoregulation
* Vasoconstriction

* 5-CT
* 8-OH-DPAT
* Aripiprazole (weak partial agonist)[105]
* AS-19
* E-55888

* Amitriptyline
* Asenapine
* Clomipramine
* Clozapine
* EGIS-12233
* Haloperidol
* Iloperidone
* Imipramine
* Ketanserin
* Mirtazapine
* Olanzapine
* RA-7
* Ritanserin
* Risperidone
* SB-269,970
* Vortioxetine (Ki = 19 nM)[39]

* Antidepressant (antagonists)
* Anxiolytics (antagonists)
* Nootropic (antagonists)

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor.[106]

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[38] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A and 5-HT6 agonist.[38]

## Expression patterns

The genes coding for serotonin receptors are expressed across the mammalian brain. Genes coding for different receptors types follow different developmental curves. Specifically, there is a developmental increase of HTR5A expression in several subregions of the human cortex, paralleled by a decreased expression of HTR1A from the embryonic period to the post-natal one. [107]

## 5-HT1-like

A number of receptors were classed as "5-HT1-like" - by 1998 it was being argued that, since these receptors were "a heterogeneous population of 5-HT1B, 5-HT1D and 5-HT7" receptors the classification was redundant.[108]

## References

1. ↑ 1.0 1.1 "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacological Reviews 46 (2): 157–203. June 1994. PMID 7938165. http://pharmrev.aspetjournals.org/cgi/content/abstract/46/2/157.
2. ↑ 2.0 2.1 "Chapter 13: Serotonin Receptors". Basic Neurochemistry: MolecularCellular, and Medical Aspects. Philadelphia: Lippincott-Raven. 1999. pp. 263–292. ISBN 978-0-397-51820-3. https://www.ncbi.nlm.nih.gov/books/bv.fcgi?call=bv.View..ShowSection&rid=bnchm.section.963.
3. ↑ "A High-Resolution In Vivo Atlas of the Human Brain's Serotonin System". The Journal of Neuroscience 37 (1): 120–128. January 2017. doi:10.1523/jneurosci.2830-16.2016. PMID 28053035.
4. ↑ "Serotonin receptors". Chemical Reviews 108 (5): 1614–1641. May 2008. doi:10.1021/cr078224o. PMID 18476671.
5. ↑ "Serotonin receptors antagonistically modulate Caenorhabditis elegans longevity". Aging Cell 6 (4): 483–488. August 2007. doi:10.1111/j.1474-9726.2007.00303.x. PMID 17559503.
6. ↑ "Manipulation of serotonin signal suppresses early phase of behavioral aging in Caenorhabditis elegans". Neurobiology of Aging 29 (7): 1093–1100. July 2008. doi:10.1016/j.neurobiolaging.2007.01.013. PMID 17336425.
7. ↑ "Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor". Journal of Neurochemistry 131 (6): 767–777. December 2014. doi:10.1111/jnc.12940. PMID 25187179.
8. ↑ "The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells". European Journal of Pharmacology 361 (2–3): 299–309. November 1998. doi:10.1016/S0014-2999(98)00744-4. PMID 9865521.
9. ↑ Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (2nd ed.). New York: McGraw-Hill Medical. 2009. p. 4. ISBN 9780071481274. "Similarly, little is known about which of serotonin's 14 known receptors must be activated to achieve an antidepressant response."
10. ↑ Basic Neurochemistry - Principles of Molecular, Cellular and Medical Neurobiology (8th ed.). Waltham, MA: USA: Elsevier. 2012. pp. 320–321. ISBN 978-0-12-374947-5.
11. ↑ 11.0 11.1 11.2 11.3 "5-hydroxyindalpine, an agonist at the putative 5-HT receptor, has no activity on human recombinant monoamine receptors but accelerates distension-induced peristalsis in mouse isolated colon". Neurogastroenterology and Motility 21 (7): 760–e48. July 2009. doi:10.1111/j.1365-2982.2009.01275.x. PMID 19309442.
12. ↑ "Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology. 2000-01-01. http://www.acnp.org/g4/GN401000039/Ch039.html.
13. ↑ "5-Hydroxytryptamine Receptors". IUPHAR Receptor Database. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288.
14. ↑ "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors". Polish Journal of Pharmacology 54 (4): 327–341. 2002. PMID 12523486. http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf.
15. ↑ "Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake". Psychopharmacology 115 (1–2): 173–179. June 1994. doi:10.1007/BF02244769. PMID 7862892.
16. ↑ "Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors". Progress in Neurobiology 81 (3): 133–178. February 2007. doi:10.1016/j.pneurobio.2007.01.001. PMID 17316955.
17. ↑ "Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects". Brain Research 1034 (1–2): 162–171. February 2005. doi:10.1016/j.brainres.2004.12.012. PMID 15713268.
18. ↑ 18.0 18.1 "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". European Journal of Pharmacology 526 (1–3): 125–139. December 2005. doi:10.1016/j.ejphar.2005.09.065. PMID 16310183.
19. ↑ "Increased anxiety of mice lacking the serotonin1A receptor". Proceedings of the National Academy of Sciences of the United States of America 95 (18): 10734–10739. September 1998. doi:10.1073/pnas.95.18.10734. PMID 9724773. Bibcode: 1998PNAS...9510734P.
20. ↑ "8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors". Methods and Findings in Experimental and Clinical Pharmacology 29 (4): 269–272. May 2007. doi:10.1358/mf.2007.29.4.1075362. PMID 17609739.
21. ↑ 21.0 21.1 "Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors". European Journal of Pharmacology 149 (3): 213–223. May 1988. doi:10.1016/0014-2999(88)90651-6. PMID 2842163.
22. ↑ 22.0 22.1 "Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation". Autonomic Neuroscience 142 (1–2): 71–76. November 2008. doi:10.1016/j.autneu.2008.06.004. PMID 18667366.
23. ↑ "Activation of 5-HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology 289 (2): R596–R604. August 2005. doi:10.1152/ajpregu.00845.2004. PMID 15802554.
24. ↑ 24.0 24.1 "Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin". European Journal of Pharmacology 253 (1–2): 53–60. February 1994. doi:10.1016/0014-2999(94)90756-0. PMID 8013549.
25. ↑ "Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders". Neuropsychopharmacology 30 (4): 669–682. April 2005. doi:10.1038/sj.npp.1300610. PMID 15688093.
26. ↑ "The role of 5-HT(1A) receptors in learning and memory". Behavioural Brain Research 195 (1): 54–77. December 2008. doi:10.1016/j.bbr.2008.02.023. PMID 18394726.
27. ↑ "Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory". The American Journal of Psychiatry 160 (2): 334–340. February 2003. doi:10.1176/appi.ajp.160.2.334. PMID 12562581.
28. ↑ "Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression". European Journal of Pharmacology 134 (3): 265–274. February 1987. doi:10.1016/0014-2999(87)90357-8. PMID 2883013.
29. ↑ "Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain". Pharmacology 67 (4): 182–194. April 2003. doi:10.1159/000068404. PMID 12595749.
30. ↑ 30.0 30.1 "Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors". European Journal of Pharmacology 321 (3): R11–R13. March 1997. doi:10.1016/S0014-2999(97)00050-2. PMID 9085055.
31. ↑ "8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation". European Journal of Pharmacology 317 (1): 21–28. December 1996. doi:10.1016/S0014-2999(96)00693-0. PMID 8982715.
32. ↑ 32.0 32.1 "Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology 290 (2): R405–R413. February 2006. doi:10.1152/ajpregu.00440.2005. PMID 16166206.
33. ↑ 33.0 33.1 "Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice". Psychoneuroendocrinology 27 (5): 609–618. July 2002. doi:10.1016/S0306-4530(01)00097-X. PMID 11965359.
34. ↑ "Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat". Journal of Sleep Research 1 (3): 169–175. September 1992. doi:10.1111/j.1365-2869.1992.tb00033.x. PMID 10607047.
35. ↑ "A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy")". Neuroscience 146 (2): 509–514. May 2007. doi:10.1016/j.neuroscience.2007.02.032. PMID 17383105.
36. ↑ "Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors". Neuropharmacology 25 (12): 1307–1313. December 1986. doi:10.1016/0028-3908(86)90101-2. PMID 2951611.
37. ↑ "Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits". Brain Research 1073-1074: 252–261. February 2006. doi:10.1016/j.brainres.2005.12.031. PMID 16455061.
38. ↑ 38.00 38.01 38.02 38.03 38.04 38.05 38.06 38.07 38.08 38.09 38.10 38.11 38.12 38.13 38.14 38.15 38.16 38.17 38.18 38.19 38.20 Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09
39. ↑ 39.0 39.1 39.2 39.3 39.4 "BRINTELLIX (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. [1]
40. ↑ "A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Therapie 277 (2): 235–252. October 1985. PMID 2933009.
41. ↑ "Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice". Psychopharmacology 139 (3): 185–194. October 1998. doi:10.1007/s002130050703. PMID 9784072.
42. ↑ "RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist". Psychopharmacology 141 (3): 242–250. January 1999. doi:10.1007/s002130050831. PMID 10027505.
43. ↑ "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". The Journal of Pharmacy and Pharmacology 57 (2): 253–257. February 2005. doi:10.1211/0022357055399. PMID 15720791.
44. ↑ "Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze". Pharmacology, Biochemistry, and Behavior 71 (4): 581–587. April 2002. doi:10.1016/S0091-3057(01)00712-2. PMID 11888549.
45. ↑ 45.0 45.1 "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behavioural Pharmacology 15 (8): 523–534. December 2004. doi:10.1097/00008877-200412000-00001. PMID 15577451.
46. ↑ 46.0 46.1 "Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission". Neuropharmacology 54 (7): 1041–1050. June 2008. doi:10.1016/j.neuropharm.2008.02.007. PMID 18394658.
47. ↑ 47.0 47.1 "Pharmacological studies of the acute and chronic effects of (+)-3, 4-methylenedioxymethamphetamine on locomotor activity: role of 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B/1D) receptors". The Journal of Pharmacology and Experimental Therapeutics 290 (3): 965–973. September 1999. PMID 10454466.
48. ↑ "Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study". European Neuropsychopharmacology 15 (3): 279–282. May 2005. doi:10.1016/j.euroneuro.2004.12.002. PMID 15820416.
49. ↑ "5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex". Neuroscience Letters 209 (3): 210–214. May 1996. doi:10.1016/0304-3940(96)12637-9. PMID 8736648.
50. ↑ "Serotonergic Control of Gastrointestinal Development, Motility, and Inflammation". Comprehensive Physiology 13 (3): 4851–4868. June 2023. doi:10.1002/cphy.c220024. ISBN 9780470650714. PMID 37358510.
51. ↑ "Characterization and localization of a peripheral neural 5-hydroxytryptamine receptor subtype (5-HT1P) with a selective agonist, 3H-5-hydroxyindalpine". The Journal of Neuroscience 8 (7): 2582–2595. July 1988. doi:10.1523/JNEUROSCI.08-07-02582.1988. PMID 3249244.
52. ↑ "Peripheral neural serotonin receptors: identification and characterization with specific antagonists and agonists". Proceedings of the National Academy of Sciences of the United States of America 83 (24): 9799–9803. December 1986. doi:10.1073/pnas.83.24.9799. PMID 3467338.
53. ↑ Annaházi, Anita; Berger, Thomas Erwin; Demir, Ihsan Ekin; Zeller, Florian; Müller, Michael; Anneser, Markus; Skerra, Arne; Michel, Klaus et al. (April 2022). "Metabotropic 5‐HT receptor‐mediated effects in the human submucous plexus" (in en). Neurogastroenterology & Motility 34 (10): e14380. doi:10.1111/nmo.14380. ISSN 1350-1925. PMID 35438222.
54. ↑ 54.0 54.1 "Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence". Current Topics in Medicinal Chemistry 6 (18): 1971–1985. 2006. doi:10.2174/156802606778522131. PMID 17017968.
55. ↑ "The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test". Psychopharmacology 135 (4): 383–391. February 1998. doi:10.1007/s002130050526. PMID 9539263.
56. ↑ 56.0 56.1 "5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female". Neuroendocrinology 76 (1): 28–34. July 2002. doi:10.1159/000063681. PMID 12097814.
57. ↑ 57.0 57.1 "Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors". The Journal of Neuroscience 25 (49): 11231–11238. December 2005. doi:10.1523/JNEUROSCI.1724-05.2005. PMID 16339018.
58. ↑ 58.0 58.1 "Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists". Psychopharmacology 130 (2): 144–151. March 1997. doi:10.1007/s002130050222. PMID 9106912. https://zenodo.org/record/1232625.
59. ↑ "5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats". Neuroscience 117 (4): 939–948. 2003. doi:10.1016/S0306-4522(02)00810-2. PMID 12654345.
60. ↑ 60.0 60.1 60.2 "PNU-22394, a 5-HT2C receptor agonist, reduced feeding in rodents and produces weight loss in humans" (Online). Society for Neuroscience. 27. Presentation Number 309.2. San Diego, CA: Society for Neuroscience Abstracts. 2001. p. TT-45. http://www.sfn.org/Annual-Meeting/Past-and-Future-Annual-Meetings/Abstract-Archive/Abstract-Archive-Detail?AbsYear=2001&AbsID=4715. Retrieved 18 July 2014.
61. ↑ 61.0 61.1 61.2 "Pharmacological targeting of the serotonergic system for the treatment of obesity". The Journal of Physiology 587 (1): 49–60. January 2009. doi:10.1113/jphysiol.2008.164152. PMID 19029184.
62. ↑ 62.0 62.1 62.2 "Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties". Journal of Medicinal Chemistry 56 (3): 1211–1227. February 2013. doi:10.1021/jm301656h. PMID 23301527.
63. ↑ "Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety". British Journal of Pharmacology 117 (7): 1443–1448. April 1996. doi:10.1111/j.1476-5381.1996.tb15304.x. PMID 8730737.
64. ↑ "Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat". Neuropharmacology 36 (4–5): 601–608. 1997. doi:10.1016/S0028-3908(97)00042-7. PMID 9225285.
65. ↑ "Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated". Neuropharmacology 37 (12): 1603–1610. December 1998. doi:10.1016/S0028-3908(98)00115-4. PMID 9886683.
66. ↑ "BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats". Neuropharmacology 36 (2): 233–239. February 1997. doi:10.1016/S0028-3908(96)00171-2. PMID 9144661.
67. ↑ "5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro". British Journal of Pharmacology 135 (5): 1144–1151. March 2002. doi:10.1038/sj.bjp.0704571. PMID 11877320.
68. ↑ "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 609–620. 1997. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286.
69. ↑ 69.0 69.1 "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade". Psychopharmacology 177 (4): 448–458. February 2005. doi:10.1007/s00213-004-1962-z. PMID 15289999.
70. ↑ 70.0 70.1 "S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models". Psychopharmacology 199 (4): 549–568. September 2008. doi:10.1007/s00213-008-1177-9. PMID 18523738.
71. ↑ "Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin". Biological Psychiatry 65 (9): 748–759. May 2009. doi:10.1016/j.biopsych.2008.10.031. PMID 19058784.
72. ↑ "5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists". European Journal of Pharmacology 325 (1): 9–12. April 1997. doi:10.1016/S0014-2999(97)89962-1. PMID 9151932.
73. ↑ "Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission". European Journal of Pharmacology 261 (1–2): 149–155. August 1994. doi:10.1016/0014-2999(94)90313-1. PMID 8001637.
74. ↑ "Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor". Neuropsychopharmacology 27 (5): 869–873. November 2002. doi:10.1016/S0893-133X(02)00353-6. PMID 12431861.
75. ↑ "4-Bromo-2,5-dimethoxyphenethylamine (2C-B) and structurally related phenylethylamines are potent 5-HT2A receptor antagonists in Xenopus laevis oocytes". British Journal of Pharmacology 141 (7): 1167–1174. April 2004. doi:10.1038/sj.bjp.0705722. PMID 15006903.
76. ↑ Pharmacology. Edinburgh: Churchill Livingstone. 2003. ISBN 978-0-443-07145-4. Page 187
77. ↑ "Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors". Gastroenterology 128 (5): 1317–1326. May 2005. doi:10.1053/j.gastro.2005.02.005. PMID 15887114.
78. ↑ 78.0 78.1 "Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task". Pharmacology, Biochemistry, and Behavior 47 (1): 95–99. January 1994. doi:10.1016/0091-3057(94)90116-3. PMID 8115433.
79. ↑ 79.0 79.1 "L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated intestinal pathologies and anxiety in rats". Proceedings of the National Academy of Sciences of the United States of America 100 (26): 15370–15375. December 2003. doi:10.1073/pnas.2436556100. PMID 14676321. Bibcode: 2003PNAS..10015370S.
80. ↑ "Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats". Neuropharmacology 36 (4–5): 707–712. 1997. doi:10.1016/S0028-3908(97)00037-3. PMID 9225297.
81. ↑ "Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens". Proceedings of the National Academy of Sciences of the United States of America 104 (41): 16335–16340. October 2007. doi:10.1073/pnas.0701471104. PMID 17913892. Bibcode: 2007PNAS..10416335J.
82. ↑ "[Feeding disorders in 5-HT4 receptor knockout mice]". Journal de la Société de Biologie 198 (1): 37–49. 2004. doi:10.1051/jbio/2004198010037. PMID 15146954.
83. ↑ 83.0 83.1 "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacology, Biochemistry, and Behavior 56 (3): 347–351. March 1997. doi:10.1016/S0091-3057(96)00224-9. PMID 9077568.
84. ↑ 84.0 84.1 "The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation". Neuropharmacology 36 (4–5): 689–696. 1997. doi:10.1016/S0028-3908(97)00055-5. PMID 9225295.
85. ↑ "Role of 5-HT4 receptors in the mouse passive avoidance test". The Journal of Pharmacology and Experimental Therapeutics 286 (3): 1115–1121. September 1998. PMID 9732367.
86. ↑ "Serotonin(4) (5-HT(4)) receptor agonists are putative antidepressants with a rapid onset of action". Neuron 55 (5): 712–725. September 2007. doi:10.1016/j.neuron.2007.07.041. PMID 17785179.
87. ↑ "A silver bullet for the treatment of depression?". Neuron 55 (5): 679–681. September 2007. doi:10.1016/j.neuron.2007.08.011. PMID 17785173.
88. ↑ "5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia". Science 301 (5630): 226–229. July 2003. doi:10.1126/science.1084674. PMID 12855812. Bibcode: 2003Sci...301..226M.
89. ↑ "5-HT5 receptors". Current Drug Targets. CNS and Neurological Disorders 3 (1): 53–58. February 2004. doi:10.2174/1568007043482606. PMID 14965244.
90. ↑ 90.0 90.1 "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Research. Molecular Brain Research 138 (2): 191–197. August 2005. doi:10.1016/j.molbrainres.2005.04.009. PMID 15921820.
91. ↑ 91.0 91.1 91.2 "Inactive and active state structures template selective tools for the human 5-HT5A receptor". Nature Structural & Molecular Biology 29 (7): 677–687. July 2022. doi:10.1038/s41594-022-00796-6. PMID 35835867.
92. ↑ "The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors". European Journal of Pharmacology 580 (3): 355–360. February 2008. doi:10.1016/j.ejphar.2007.11.022. PMID 18096153.
93. ↑ 93.0 93.1 "Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression". Neuropharmacology 52 (5): 1274–1283. April 2007. doi:10.1016/j.neuropharm.2007.01.007. PMID 17320917.
94. ↑ "SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models". European Journal of Pharmacology 553 (1–3): 109–119. December 2006. doi:10.1016/j.ejphar.2006.09.049. PMID 17069795.
95. ↑ 95.0 95.1 "Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task". Pharmacology, Biochemistry, and Behavior 81 (3): 673–682. July 2005. doi:10.1016/j.pbb.2005.05.005. PMID 15964617.
96. ↑ "The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats". European Journal of Pharmacology 582 (1–3): 88–93. March 2008. doi:10.1016/j.ejphar.2007.12.013. PMID 18234190.
97. ↑ "Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists". Journal of Medicinal Chemistry 52 (3): 675–87. Feb 2009. doi:10.1021/jm8009469. PMID 19159187.
98. ↑ "Target Schizophrenia - Possible future developments". The Association of the British Pharmaceutical Industry. http://www.abpi.org.uk/publications/publication_details/targetSchizophrenia-2003/section5.asp.
99. ↑ 99.0 99.1 99.2 "5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern". Biological Psychiatry 58 (10): 831–837. November 2005. doi:10.1016/j.biopsych.2005.05.012. PMID 16018977.
100. ↑ 100.0 100.1 "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression". Neuropharmacology 51 (3): 578–586. September 2006. doi:10.1016/j.neuropharm.2006.04.017. PMID 16828124.
101. ↑ "Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat". Behavioural Brain Research 195 (1): 164–170. December 2008. doi:10.1016/j.bbr.2007.12.020. PMID 18308404.
102. ↑ "Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model". Hippocampus 18 (9): 965–974. 2008. doi:10.1002/hipo.20459. PMID 18570192.
103. ↑ 103.0 103.1 "Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents". The Journal of Pharmacology and Experimental Therapeutics 321 (2): 690–698. May 2007. doi:10.1124/jpet.107.119404. PMID 17314195.
104. ↑ "SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats". British Journal of Pharmacology 139 (4): 705–714. June 2003. doi:10.1038/sj.bjp.0705290. PMID 12812993.
105. ↑ Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf
106. ↑ "HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) "]. 19 Mar 2017. https://www.ncbi.nlm.nih.gov/gene?cmd=Retrieve&dopt=full_report&list_uids=3358.
107. ↑ "Gene Expression Switching of Receptor Subunits in Human Brain Development". PLOS Computational Biology 11 (12): e1004559. December 2015. doi:10.1371/journal.pcbi.1004559. PMID 26636753. Bibcode: 2015PLSCB..11E4559B.
108. ↑ "5-HT1-like receptors: a time to bid goodbye". Trends in Pharmacological Sciences 19 (8): 311–316. August 1998. doi:10.1016/S0165-6147(98)01228-0. PMID 9745358.

## External links

* Serotonin+Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
* "5-Hydroxytryptamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288.
* "Activation of G protein-coupled receptors entails cysteine modulation of agonist binding". Cogprints. 2005-02-16. http://cogprints.org/4095/.
* "5-HT radioligands for human brain imaging with PET and SPECT". Medicinal Research Reviews 33 (1): 54–111. January 2013. doi:10.1002/med.20245. PMID 21674551.

* v
* t
* e

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

| Neurotransmitter|

| Adrenergic|

* α1 (A
* B
* D)
* α2 (A
* B
* C)
* β1
* β2
* β3

|

Purinergic|

* Adenosine (A1
* A2A
* A2B
* A3)
* P2Y (1
* 2
* 4
* 5
* 6
* 8
* 9
* 10
* 11
* 12
* 13
* 14)

Serotonin|

* (all but 5-HT3) 5-HT1 (A
* B
* D
* E
* F)
* 5-HT2 (A
* B
* C)
* 5-HT (4
* 5A
* 6
* 7)

Other|

* Acetylcholine (M1
* M2
* M3
* M4
* M5)
* Dopamine
* D1
* D2
* D3
* D4
* D5
* GHB receptor
* Histamine
* H1
* H2
* H3
* H4
* Melatonin (1A
* 1B
* 1C)
* TAAR (1
* 2
* 5
* 6
* 8
* 9)

Metabolites and
signaling molecules|

| Eicosanoid|

* CysLT (1
* 2)
* LTB4
* 1
* 2
* FPRL1
* OXE
* Prostaglandin
* DP (1
* 2), EP (1
* 2
* 3
* 4), FP
* Prostacyclin
* Thromboxane

|

Other|

* Bile acid
* Cannabinoid (CB1
* CB2, GPR (18
* 55
* 119))
* EBI2
* Estrogen
* Free fatty acid (1
* 2
* 3
* 4)
* Hydroxycarboxylic acids
* 1
* 2
* 3
* Lysophosphatidic acid (1
* 2
* 3
* 4
* 5
* 6)
* Lysophospholipid (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8)
* Oxoglutarate
* PAF
* Sphingosine-1-phosphate (1
* 2
* 3
* 4
* 5)
* Succinate

Peptide|

| Neuropeptide|

* B/W (1
* 2)
* FF (1
* 2)
* S
* Y (1
* 2
* 4
* 5)
* Neuromedin (B
* U (1
* 2))
* Neurotensin (1
* 2)

|

Other|

* Anaphylatoxin (C3a
* C5a)
* Angiotensin (1
* 2)
* Apelin
* Bombesin
* BRS3
* GRPR
* NMBR)
* Bradykinin (B1
* B2)
* Chemokine
* Cholecystokinin (A
* B)
* Endothelin
* A
* B
* Formyl peptide (1
* 2
* 3)
* FSH
* Galanin (1
* 2
* 3)
* Gonadotropin-releasing hormone (1
* 2)
* Ghrelin
* Kisspeptin
* Luteinizing hormone/choriogonadotropin
* MAS (1
* 1L
* D
* E
* F
* G
* X1
* X2
* X3
* X4)
* Melanocortin (1
* 2
* 3
* 4
* 5)
* MCHR (1
* 2)
* Motilin
* Opioid (Delta
* Kappa
* Mu
* Nociceptin & Zeta, but not Sigma)
* Orexin (1
* 2)
* Oxytocin
* Prokineticin (1
* 2)
* Prolactin-releasing peptide
* Relaxin (1
* 2
* 3
* 4)
* Somatostatin (1
* 2
* 3
* 4
* 5)
* Tachykinin (1
* 2
* 3)
* Thyrotropin
* Thyrotropin-releasing hormone
* Urotensin-II
* Vasopressin (1A
* 1B
* 2)

Miscellaneous|

| Taste, bitter|

* TAS2R
* 1
* 3
* 4
* 5
* 7
* 8
* 9
* 10
* 13
* 14
* 16
* 19
* 20
* 30
* 31
* 38
* 39
* 40
* 41
* 42
* 43
* 45
* 46
* 50
* 60
* Vomeronasal receptor type 1

|

Orphan|

* GPR (1
* 3
* 4
* 6
* 12
* 15
* 17
* 18
* 19
* 20
* 21
* 22
* 23
* 25
* 26
* 27
* 31
* 32
* 33
* 34
* 35
* 37
* 39
* 42
* 44
* 45
* 50
* 52
* 55
* 61
* 62
* 63
* 65
* 68
* 75
* 77
* 78
* 81
* 82
* 83
* 84
* 85
* 87
* 88
* 92
* 101
* 103
* 109A
* 109B
* 119
* 120
* 132
* 135
* 137B
* 139
* 141
* 142
* 146
* 148
* 149
* 150
* 151
* 152
* 153
* 160
* 161
* 162
* 171
* 173
* 174
* 176
* 177
* 182
* 183)

Other|

* Adrenomedullin
* Olfactory
* Opsin (3
* 4
* 5
* 1LW
* 1MW
* 1SW
* RGR
* RRH)
* Protease-activated (1
* 2
* 3
* 4)
* SREB (1
* 2
* 3)

Class B: Secretin-like

| Adhesion|

* ADGRG (1
* 2
* 3
* 4
* 5
* 6
* 7)

|

Orphan|

* GPR (56
* 64
* 97
* 98
* 110
* 111
* 112
* 113
* 114
* 115
* 116
* 123
* 124
* 125
* 126
* 128
* 133
* 143
* 144
* 155
* 157)

Other|

* Brain-specific angiogenesis inhibitor (1
* 2
* 3)
* Cadherin (1
* 2
* 3)
* Calcitonin
* CALCRL
* CD97
* Corticotropin-releasing hormone (1
* 2)
* EMR (1
* 2
* 3)
* Glucagon (GR
* GIPR
* GLP1R
* GLP2R)
* Growth-hormone-releasing hormone
* PACAPR1
* GPR
* Latrophilin (1
* 2
* 3
* ELTD1)
* Methuselah-like proteins
* Parathyroid hormone (1
* 2)
* Secretin
* Vasoactive intestinal peptide (1
* 2)

Class C: Metabotropic glutamate / pheromone

| Taste, sweet|

* TAS1R
* 1
* 2
* 3
* Vomeronasal receptor, type 2

|

Other|

* Calcium-sensing receptor
* GABAB (1
* 2)
* Glutamate receptor (Metabotropic glutamate (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8))
* GPRC6A
* GPR (156
* 158
* 179)
* RAIG (1
* 2
* 3
* 4)

Class F: Frizzled & Smoothened

| Frizzled|

* Frizzled (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8
* 9
* 10)

|

Smoothened|

* Smoothened

* v
* t
* e

Ion channel, cell surface receptor: ligand-gated ion channels

Cys-loop receptors|

| 5-HT/serotonin|

* 5-HT3
* A
* B
* C
* D
* E

|

GABA|

* GABAA
* α1
* α2
* α3
* α4
* α5
* α6
* β1
* β2
* β3
* γ1
* γ2
* γ3
* δ
* ε
* π
* θ
* GABAA-ρ
* ρ1
* ρ2
* ρ3

Glycine|

* α1
* α2
* α3
* α4
* β

Nicotinic acetylcholine|

* monomers: α1
* α2
* α3
* α4
* α5
* α6
* α7
* α9
* α10
* β1
* β2
* β3
* β4
* δ
* ε

* pentamers: (α3)2(β4)3
* (α4)2(β2)3
* (α7)5
* (α1)2(β4)3 \- Ganglion type
* (α1)2β1δε - Muscle type

Zinc|

* Zinc-activated

Ionotropic glutamates|

| Ligand-gated only|

* AMPA (1
* 2
* 3
* 4)
* Kainate
* 1
* 2
* 3
* 4
* 5

|

Voltage- and ligand-gated|

* NMDA
* 1
* 2A
* 2B
* 2C
* 2D
* 3A
* 3B
* L1A
* L1B

‘Orphan’|

* GluD
* δ1
* δ2

ATP-gated channels|

| Purinergic receptors|

* P2X
* 1
* 2
* 3
* 4
* 5
* 6
* 7

|

* v
* t
* e

Serotonin receptor modulators

5-HT1|

| 5-HT1A|

* Agonists: 8-OH-DPAT
* Adatanserin
* Amphetamine
* Antidepressants (e.g., etoperidone, hydroxynefazodone, nefazodone, trazodone, triazoledione, vilazodone, vortioxetine)
* Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, lurasidone, quetiapine, ziprasidone)
* Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone)
* Bay R 1531
* Befiradol
* BMY-14802
* Cannabidiol
* Dimemebfe
* Dopamine
* Ebalzotan
* Eltoprazine
* Enciprazine
* Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, lisuride, LSD, methylergometrine (methylergonovine), methysergide, pergolide)
* F-11461
* F-12826
* F-13714
* F-14679
* F-15063
* F-15,599
* Flesinoxan
* Flibanserin
* Flumexadol
* Hypidone
* Lesopitron
* LY-293284
* LY-301317
* mCPP
* MKC-242
* Naluzotan
* NBUMP
* Osemozotan
* Oxaflozane
* Pardoprunox
* Piclozotan
* Rauwolscine
* Repinotan
* Roxindole
* RU-24,969
* S-14,506
* S-14671
* S-15535
* Sarizotan
* Serotonin (5-HT)
* SSR-181507
* Sunepitron
* Tryptamines (e.g., 5-CT, 5-MeO-DMT, 5-MT, bufotenin, DMT, indorenate, N-Me-5-HT, psilocin, psilocybin)
* TGBA01AD
* U-92,016-A
* Urapidil
* Vilazodone
* Xaliproden
* Yohimbine

* Antagonists: Atypical antipsychotics (e.g., iloperidone, risperidone, sertindole)
* AV965
* Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, pindolol, propranolol, tertatolol)
* BMY-7,378
* CSP-2503
* Dotarizine
* Ergolines (e.g., metergoline)
* FCE-24379
* Flopropione
* GR-46611
* Isamoltane
* Lecozotan
* Mefway
* Metitepine (methiothepin)
* MIN-117 (WF-516)
* MPPF
* NAN-190
* Robalzotan
* S-15535
* SB-649,915
* SDZ 216-525
* Spiperone
* Spiramide
* Spiroxatrine
* UH-301
* WAY-100135
* WAY-100635
* Xylamidine

* Unknown/unsorted: Acetryptine
* Carvedilol
* Ergolines (e.g., ergometrine (ergonovine))

5-HT1B|

* Agonists: Anpirtoline
* CGS-12066A
* CP-93129
* CP-94253
* CP-122,288
* CP-135807
* Eltoprazine
* Ergolines (e.g., bromocriptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)
* mCPP
* RU-24,969
* Serotonin (5-HT)
* Triptans (e.g., avitriptan, donitriptan, eletriptan, sumatriptan, zolmitriptan)
* TFMPP
* Tryptamines (e.g., 5-BT, 5-CT, 5-MT, DMT)
* Vortioxetine

* Antagonists: AR-A000002
* Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, tertatolol)
* Elzasonan
* Ergolines (e.g., metergoline)
* GR-127935
* Isamoltane
* LY-393558
* Metitepine (methiothepin)
* SB-216641
* SB-224289
* SB-236057
* Yohimbine

* Unknown/unsorted: Ergolines (e.g., cabergoline, ergometrine (ergonovine), lisuride)

5-HT1D|

* Agonists: CP-122,288
* CP-135807
* CP-286601
* Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, LSD, methysergide)
* Chemistry:GR-46611
* L-694247
* Chemistry:L-772405
* mCPP
* PNU-109291
* PNU-142633
* Serotonin (5-HT)
* TGBA01AD
* Triptans (e.g., almotriptan, avitriptan, donitriptan, [[Chemistry:Eleeletriptan, Frovatriptan|frovatriptan]], naratriptan, rizatriptan, sumatriptan, zolmitriptan)
* Tryptamines (e.g., 5-BT, 5-CT, 5-Et-DMT, 5-MT, 5-(nonyloxy)tryptamine, DMT)

* Antagonists: Alniditan
* BRL-15,572
* Elzasonan
* Ergolines (e.g., metergoline)
* GR-127935
* Ketanserin
* LY-310762
* LY-367642
* LY-393558
* LY-456219
* LY-456220
* Metitepine (methiothepin)
* Mianserin
* Ritanserin
* Yohimbine
* Ziprasidone

* Unknown/unsorted: Acetryptine
* Ergolines (e.g., lisuride, lysergol, pergolide)

5-HT1E|

* Agonists: BRL-54443
* Ergolines (e.g., methysergide)
* Serotonin (5-HT)
* Triptans (e.g., eletriptan)
* Tryptamines (e.g., tryptamine)

* Antagonists: Metitepine (methiothepin)

* Unknown/unsorted: ErgIrindaloneolines (e.g., ergometrine (ergonovine), lysergol, methylergometrine (methylergonovine)

5-HT1F|

* Agonists: BRL-54443
* CP-122,288
* Ergolines (e.g., bromocriptine, lysergol, methylergometrine (methylergonovine) methysergide)
* Lasmiditan
* LY-334370
* Serotonin (5-HT)
* Triptans (e.g., eletriptan, naratriptan, sumatriptan)
* Tryptamines (e.g., 5-MT)

* Antagonists: Metitepine (methiothepin)
* Mianserin

5-HT2|

| 5-HT2A|

* Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN-NBOH, 2CBFly-NBOMe)
* 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)
* 2C-B-FLY
* 2CB-Ind
* 5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)
* α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)
* AL-34662
* AL-37350A
* Bromo-DragonFLY
* Dimemebfe
* DMBMPP
* DOx (e.g., DOB, DOC, DOI, DOM)
* Efavirenz
* Ergolines (e.g., 1P-LSD, ALD-52, bromocriptine, cabergoline, ergine (LSA), ergometrine (ergonovine), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, methylergometrine (methylergonovine), pergolide)
* Flumexadol
* IHCH-7113
* Jimscaline
* Lorcaserin
* MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)
* O-4310
* Oxaflozane
* PHA-57378
* PNU-22394
* PNU-181731
* RH-34
* SCHEMBL5334361
* Phenethylamines (e.g., lophophine, mescaline)
* Piperazines (e.g., BZP, quipazine, TFMPP)
* Serotonin (5-HT)
* TCB-2
* TFMFly
* Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)

* Antagonists: 5-I-R91150
* 5-MeO-NBpBrT
* AC-90179
* Adatanserin
* Altanserin
* Antihistamines (e.g., cyproheptadine, hydroxyzine, ketotifen, perlapine)
* AMDA
* Atypical antipsychotics (e.g., amperozide, aripiprazole, asenapine, blonanserin, brexpiprazole, carpipramine, clocapramine, clorotepine, clozapine, fluperlapine, gevotroline, iloperidone, lurasidone, melperone, mosapramine, ocaperidone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, zicronapine, ziprasidone, zotepine)
* Chlorprothixene
* Cinanserin
* CSP-2503
* Deramciclane
* Dotarizine
* Eplivanserin
* Ergolines (e.g., amesergide, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)
* Fananserin
* Flibanserin
* Glemanserin
* Irindalone
* Ketanserin
* KML-010
* Landipirdine
* LY-393558
* mCPP
* Medifoxamine
* Metitepine (methiothepin)
* MIN-117 (WF-516)
* Naftidrofuryl
* Nantenine
* Nelotanserin
* Opiranserin (VVZ-149)
* Pelanserin
* Phenoxybenzamine
* Pimavanserin
* Pirenperone
* Pizotifen
* Pruvanserin
* Rauwolscine
* Ritanserin
* Roluperidone
* S-14671
* Sarpogrelate
* Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, triazoledione, trazodone)
* SR-46349B
* TGBA01AD
* Teniloxazine
* Temanogrel
* Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)
* Tricyclic antidepressants (e.g., amitriptyline)
* Typical antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, loxapine, perphenazine, pimozide, pipamperone, prochlorperazine, setoperone, spiperone, spiramide, thioridazine, thiothixene, trifluoperazine)
* Volinanserin
* Xylamidine
* Yohimbine

* Unknown/unsorted: Ergolines (e.g., dihydroergotamine, nicergoline)

5-HT2B|

* Agonists: 4-Methylaminorex
* Aminorex
* Amphetamines (e.g., chlorphentermine, cloforex, dexfenfluramine, fenfluramine, levofenfluramine, norfenfluramine)
* BW-723C86
* DOx (e.g., DOB, DOC, DOI, DOM)
* Ergolines (e.g., cabergoline, dihydroergocryptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)
* Lorcaserin
* MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)
* Piperazines (e.g., TFMPP)
* PNU-22394
* Ro60-0175
* Serotonin (5-HT)
* Tryptamines (e.g., 5-BT, 5-CT, 5-MT, α-Me-5-HT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)

* Antagonists: Agomelatine
* Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, N-desalkylquetiapine (norquetiapine), N-desmethylclozapine (norclozapine), olanzapine, pipamperone, quetiapine, risperidone, ziprasidone)
* Cyproheptadine
* EGIS-7625
* Ergolines (e.g., amesergide, bromocriptine, lisuride, LY-53857, LY-272015, mesulergine)
* Ketanserin
* LY-393558
* mCPP
* Metadoxine
* Metitepine (methiothepin)
* Pirenperone
* Pizotifen
* Propranolol
* PRX-08066
* Rauwolscine
* Ritanserin
* RS-127445
* Sarpogrelate
* SB-200646
* SB-204741
* SB-206553
* SB-215505
* SB-221284
* SB-228357
* SDZ SER-082
* Tegaserod
* Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)
* Trazodone
* Typical antipsychotics (e.g., chlorpromazine)
* TIK-301
* Yohimbine

* Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine))

5-HT2C|

* Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)
* 5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)
* α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)
* A-372159
* AL-38022A
* Alstonine
* CP-809101
* Dimemebfe
* DOx (e.g., DOB, DOC, DOI, DOM)
* Ergolines (e.g., ALD-52, cabergoline, dihydroergotamine, ergine (LSA), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, pergolide)
* Flumexadol
* Lorcaserin
* MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)
* MK-212
* ORG-12962
* ORG-37684
* Oxaflozane
* PHA-57378
* Phenethylamines (e.g., lophophine, mescaline)
* Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP)
* PNU-22394
* PNU-181731
* Ro60-0175
* Ro60-0213
* Serotonin (5-HT)
* Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
* Vabicaserin
* WAY-629
* WAY-161503
* YM-348

* Antagonists: Adatanserin
* Agomelatine
* Atypical antipsychotics (e.g., asenapine, clorotepine, clozapine, fluperlapine, iloperidone, melperone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, zotepine)
* Captodiame
* CEPC
* Cinanserin
* Cyproheptadine
* Deramciclane
* Desmetramadol
* Dotarizine
* Eltoprazine
* Ergolines (e.g., amesergide, bromocriptine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)
* Etoperidone
* Fluoxetine
* FR-260010
* Irindalone
* Ketanserin
* Ketotifen
* Latrepirdine (dimebolin)
* Medifoxamine
* Metitepine (methiothepin)
* Nefazodone
* Pirenperone
* Pizotifen
* Propranolol
* Ritanserin
* RS-102221
* S-14671
* SB-200646
* SB-206553
* SB-221284
* SB-228357
* SB-242084
* SB-243213
* SDZ SER-082
* Tedatioxetine
* Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)
* TIK-301
* Tramadol
* Trazodone
* Tricyclic antidepressants (e.g., amitriptyline, nortriptyline)
* Typical antipsychotics (e.g., chlorpromazine, loxapine, pimozide, pipamperone, thioridazine)
* Xylamidine

* Unknown/unsorted: Efavirenz
* Ergolines (e.g., ergometrine (ergonovine), methylergometrine (methylergonovine))

5-HT3–7|

| 5-HT3|

* Agonists: Alcohols (e.g., butanol, ethanol (alcohol), trichloroethanol)
* m-CPBG
* Phenylbiguanide
* Piperazines (e.g., BZP, mCPP, quipazine)
* RS-56812
* Serotonin (5-HT)
* SR-57227
* SR-57227A
* Tryptamines (e.g., 2-Me-5-HT, 5-CT, bufotenidine (5-HTQ))
* Volatiles/gases (e.g., halothane, isoflurane, toluene, trichloroethane)
* YM-31636

* Antagonists: Alosetron
* Chemistry:Arazasetron
* AS-8112
* Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine)
* Azasetron
* Batanopride
* Bemesetron (MDL-72222)
* Bupropion
* Cilansetron
* CSP-2503
* Dazopride
* Dolasetron
* Galanolactone
* Granisetron
* Hydroxybupropion
* Lerisetron
* Memantine
* Ondansetron
* Palonosetron
* Ramosetron
* Renzapride
* Ricasetron
* Tedatioxetine
* Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)
* Thujone
* Tropanserin
* Tropisetron
* Typical antipsychotics (e.g., loxapine)
* Volatiles/gases (e.g., nitrous oxide, sevoflurane, xenon)
* Vortioxetine
* Zacopride
* Zatosetron

* Unknown/unsorted: LY-53857
* Piperazines (e.g., naphthylpiperazine)

5-HT4|

* Agonists: 5-MT
* BIMU8
* Capeserod
* Cinitapride
* Cisapride
* CJ-033466
* Dazopride
* Metoclopramide
* Minesapride
* Mosapride
* Prucalopride
* PRX-03140
* Renzapride
* RS-67,333
* RS-67,506
* Serotonin (5-HT)
* Tegaserod
* Usmarapride
* Velusetrag
* Zacopride

* Antagonists: GR-113808
* GR-125487
* L-Lysine
* Piboserod
* RS-39604
* RS-67532
* SB-203186
* SB-204070

5-HT5A|

* Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD)
* Serotonin (5-HT)
* Tryptamines (e.g., 5-CT)
* Valerenic acid

* Antagonists: Asenapine
* Latrepirdine (dimebolin)
* Metitepine (methiothepin)
* Ritanserin
* SB-699551

* Unknown/unsorted: Ergolines (e.g., metergoline, methysergide)
* Piperazines (e.g., naphthylpiperazine)

5-HT6|

* Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, methysergide)
* Hypidone
* Serotonin (5-HT)
* Tryptamines (e.g., 2-Me-5-HT, 5-BT, 5-CT, 5-MT, Bufotenin, E-6801, E-6837, EMD-386088, EMDT, LY-586713, N-Me-5-HT, ST-1936, tryptamine)
* WAY-181187
* WAY-208466

* Antagonists: ABT-354
* Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, iloperidone, olanzapine, tiospirone)
* AVN-101
* AVN-211
* AVN-322
* AVN-397
* BGC20-760
* BVT-5182
* BVT-74316
* Cerlapirdine
* EGIS-12,233
* GW-742457
* Idalopirdine
* Ketanserin
* Landipirdine
* Latrepirdine (dimebolin)
* Masupirdine
* Metitepine (methiothepin)
* MS-245
* PRX-07034
* Ritanserin
* Ro 04-6790
* Ro 63-0563
* SB-258585
* SB-271046
* SB-357134
* SB-399885
* SB-742457
* Tetracyclic antidepressants (e.g., amoxapine, mianserin)
* Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, nortriptyline)
* Typical antipsychotics (e.g., chlorpromazine, loxapine)

* Unknown/unsorted: Ergolines (e.g., 2-Br-LSD (BOL-148), bromocriptine, lergotrile, pergolide)
* Piperazines (e.g., naphthylpiperazine)

5-HT7|

* Agonists: 8-OH-DPAT
* AS-19
* Bifeprunox
* E-55888
* Ergolines (e.g., LSD)
* LP-12
* LP-44
* LP-211
* RU-24,969
* Sarizotan
* Serotonin (5-HT)
* Triptans (e.g., frovatriptan)
* Tryptamines (e.g., 5-CT, 5-MT, bufotenin, N-Me-5-HT)

* Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, fluperlapine, olanzapine, risperidone, sertindole, tiospirone, ziprasidone, zotepine)
* Butaclamol
* DR-4485
* EGIS-12,233
* Ergolines (e.g., 2-Br-LSD (BOL-148), amesergide, bromocriptine, cabergoline, dihydroergotamine, ergotamine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)
* JNJ-18038683
* Ketanserin
* LY-215,840
* Metitepine (methiothepin)
* Ritanserin
* SB-258719
* SB-258741
* SB-269970
* SB-656104
* SB-656104A
* SB-691673
* SLV-313
* SLV-314
* Spiperone
* Chemistry:SSR-181507
* Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
* Tricyclic antidepressants (e.g., amitriptyline, clomipramine, imipramine)
* Typical antipsychotics (e.g., acetophenazine, chlorpromazine, chlorprothixene, fluphenazine, loxapine, pimozide)
* Vortioxetine

* Unknown/unsorted: Ergolines (e.g., lisuride, pergolide)
* Piperazines (e.g., naphthylpiperazine)

* See also: Receptor/signaling modulators
* Adrenergics
* Dopaminergics
* Melatonergics
* Monoamine reuptake inhibitors and releasing agents
* Monoamine metabolism modulators
* Monoamine neurotoxins

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