5-HT1A receptor

Short description: Serotonin receptor protein distributed in the cerebrum and raphe nucleus

Generic protein structure example

The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarization and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene.[1][2]

## Contents

* 1 Distribution
* 2 Function
* 2.1 Neuromodulation
* 2.2 Endocrinology
* 2.3 Autoreceptors
* 3 Ligands
* 3.1 Agonists
* 3.1.1 Partial agonists
* 3.1.2 Full agonists
* 3.1.3 Biased agonists
* 3.2 Antagonists
* 3.3 Allosteric Modulators
* 4 Genetics
* 5 Protein-protein interactions
* 5.1 Receptor oligomers
* 6 See also
* 7 References
* 8 External links

## Distribution

The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus.[3][4][5] The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors.[4]

## Function

### Neuromodulation

5-HT1A receptor agonists are involved in neuromodulation. They decrease blood pressure and heart rate via a central mechanism, by inducing peripheral vasodilation, and by stimulating the vagus nerve.[6] These effects are the result of activation of 5-HT1A receptors within the rostral ventrolateral medulla.[6] The sympatholytic antihypertensive drug urapidil is an α1-adrenergic receptor antagonist and 5-HT1A receptor agonist, and it has been demonstrated that the latter property contributes to its overall therapeutic effects.[7][8] Vasodilation of the blood vessels in the skin via central 5-HT1A activation increases heat dissipation from the organism out into the environment, causing a decrease in body temperature.[9][10]

Activation of central 5-HT1A receptors triggers the release or inhibition of norepinephrine depending on species, presumably from the locus coeruleus, which then reduces or increases neuronal tone to the iris sphincter muscle by modulation of postsynaptic α2-adrenergic receptors within the Edinger-Westphal nucleus, resulting in pupil dilation in rodents, and pupil constriction in primates including humans.[11][12][13]

5-HT1A receptor agonists like buspirone[14] and flesinoxan[15] show efficacy in relieving anxiety[16] and depression.[17] Buspirone and tandospirone are currently approved for these indications in different parts of the world. Others such as gepirone,[18] flesinoxan,[15] flibanserin,[19] and naluzotan[20] have also been investigated, though none have been fully developed and approved yet. Some of the atypical antipsychotics like lurasidone[21] and aripiprazole[22] are also partial agonists at the 5-HT1A receptor and are sometimes used in low doses as augmentations to standard antidepressants like the selective serotonin reuptake inhibitors (SSRIs).[23] Mice lacking 5-HT1A receptors altogether (knockout) show increased anxiety but lower depressive-like behaviour.[24]

5-HT1A autoreceptor desensitization and increased 5-HT1A receptor postsynaptic activation via general increases in serotonin levels by serotonin precursor supplementation, serotonin reuptake inhibition, or inhibition of monoamine oxidase has been shown to be a major mediator in the therapeutic benefits of most mainstream antidepressant supplements and pharmaceuticals, including serotonin precursors like L-tryptophan and 5-HTP, SSRIs, serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), tetracyclic antidepressants (TeCAs), and monoamine oxidase inhibitors (MAOIs).[25] 5-HT1A receptor activation likely plays a significant role in the positive effects of serotonin releasing agents (SRAs) like MDMA (commonly known as ecstasy) as well.[26][27]

5-HT1A receptors in the dorsal raphe nucleus are co-localized with neurokinin 1 (NK1) receptors and have been shown to inhibit the release of substance P. Their endogenous ligand.[28][29] In addition to being antidepressant and anxiolytic in effect, 5-HT1A receptor activation has also been demonstrated to be antiemetic[30][31] and analgesic,[32][33] and all of these properties may be mediated in part or full, depending on the property in question, by NK1 receptor inhibition. Consequently, novel NK1 receptor antagonists are now in use for the treatment of nausea and emesis, and are also being investigated for the treatment of anxiety and depression.[34]

5-HT1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and hippocampus, and may be useful for improving the symptoms of schizophrenia and Parkinson's disease.[35] As mentioned above, some of the atypical antipsychotics are 5-HT1A receptor partial agonists, and this property has been shown to enhance their clinical efficacy.[35][36][37] Enhancement of dopamine release in these areas may also play a major role in the antidepressant and anxiolytic effects as seen upon postsynaptic activation of the 5-HT1A receptor.[38][39]

The activation of 5-HT1A receptors has been demonstrated to impair certain aspects of memory (affecting declarative and non-declarative memory functions) and learning (due to interference with memory-encoding mechanisms), by inhibiting the release of glutamate and acetylcholine in various areas of the brain.[40] 5-HT1A activation is known to improve cognitive functions associated with the prefrontal cortex, possibly via inducing prefrontal cortex dopamine and acetylcholine release.[41] Conversely, the 5-HT1A antagonist, WAY100635, alleviated learning and memory impairments induced by glutamate blockade (with dizocilpine)[42] or hippocampal cholinergic denervation (by fornix transection)[43] in primates. Furthermore, 5-HT1A receptor antagonists such as lecozotan have been shown to facilitate certain types of learning and memory in rodents, and as a result, are being developed as novel treatments for Alzheimer's disease.[44]

Other effects of 5-HT1A activation that have been observed in scientific research include:

* Decreased aggression[45][46]
* Increased sociability[27]
* Decreased impulsivity[47]
* Inhibition of drug-seeking behavior[48][49][50]
* Facilitation of sex drive and arousal[51][52]
* Inhibition of penile erection[53][54]
* Diminished food intake[55]
* Prolongation of REM sleep latency[56][57]
* Reversal of opioid-induced respiratory depression[58]

### Endocrinology

5-HT1A receptor activation induces the secretion of various hormones including cortisol, corticosterone, adrenocorticotropic hormone (ACTH), oxytocin, prolactin, growth hormone, and β-endorphin.[59][60][61][62] The receptor does not affect vasopressin or renin secretion, unlike the 5-HT2 receptors.[59][60] It has been suggested that oxytocin release may contribute to the prosocial, antiaggressive, and anxiolytic properties observed upon activation of the receptor.[27] β-Endorphin secretion may contribute to antidepressant, anxiolytic, and analgesic effects.[63]

### Autoreceptors

5-HT1A receptors can be located on the cell body, dendrites, axons, and both presynaptically and postsynaptically in nerve terminals or synapses. Those located on the soma and dendrites are referred to as somatodendritic, and those located presynaptically in the synapse are simply referred to as presynaptic. As a group, receptors that are sensitive to the neurotransmitter that is released by the neuron on which the receptors are located are known as autoreceptors; they typically constitute the key component of an ultra-short negative feedback loop whereby the neuron's release of neurotransmitter inhibits its further release of neurotransmitter. Stimulation of 5-HT1A autoreceptors inhibits the release of serotonin in nerve terminals. For this reason, 5-HT1A receptor agonists tend to exert a biphasic mode of action; they decrease serotonin release and postsynaptic 5-HT1A receptor activity in low doses, and further decrease serotonin release but increase postsynaptic 5-HT1A receptor activity at higher doses by directly stimulating the receptors in place of serotonin.

This autoreceptor-mediated inhibition of serotonin release has been theorized to be a major factor in the therapeutic lag that is seen with serotonergic antidepressants such as the SSRIs.[64] The autoreceptors must first desensitize before the concentration of extracellular serotonin in the synapse can become elevated appreciably.[64][65] Though the responsiveness of the autoreceptors is somewhat reduced with chronic treatment, they still remain effective at constraining large increases in extracellular serotonin concentrations.[64] For this reason, serotonin reuptake inhibitors that also have 5-HT1A receptor antagonistic or partial agonistic properties, such as vilazodone and SB-649,915, are being investigated and introduced as novel antidepressants with the potential for a faster onset of action and improved effectiveness compared to those currently available.[66]

Unlike most drugs that elevate extracellular serotonin levels like the SSRIs and MAOIs, SRAs such as fenfluramine and MDMA bypass serotonin autoreceptors such as 5-HT1A. They do this by directly acting on the release mechanisms of serotonin neurons and forcing release to occur regardless of autoreceptor-mediated inhibition.[67] As such, SRAs induce immediate and much greater increases in extracellular serotonin concentrations compared to other serotonin-elevating agents such as the SSRIs. [Note: This is questionable as the level of serotonin output from SRAs is still dose dependant and, while SRAs will initially bypass autoreceptors, the increase in serotonin they induce will then agonise autoreceptors.] In contrast to SRAs, SSRIs may decrease serotonin levels initially (especially at lower dosages due to the biphasic mode of action mentioned above) and require several weeks of chronic dosing before serotonin concentrations reach their maximal elevation (due to 1A autoreceptor desensitization) and full clinical benefits for conditions such as depression and anxiety are seen[68][69] (although other studies show an acute increase in 5-HT[70][71] which may account for initial worsening of symptoms in sensitive individuals[72]). For these reasons, selective serotonin releasing agents (SSRAs) such as MDAI and MMAI have been proposed as novel antidepressants with a putatively faster onset of action and improved effectiveness compared to current treatments.[68]

Similarly to SRAs, sufficiently high doses of 5-HT1A receptor agonists also bypass the 5-HT1A autoreceptor-mediated inhibition of serotonin release and therefore increase 5-HT1A postsynaptic receptor activation by directly agonizing the postsynaptic receptors in lieu of serotonin.

## Ligands

The distribution of 5-HT1A receptors in the human brain may be imaged with the positron emission tomography using the radioligand [11C] WAY-100,635.[73] For example, one study has found increased 5-HT1A binding in type 2 diabetes.[74] Another PET study found a negative correlation between the amount of 5-HT1A binding in the raphe nuclei, hippocampus and neocortex and a self-reported tendency to have spiritual experiences.[75] Labeled with tritium, WAY-100,635 may also be used in autoradiography.[76]

### Agonists

#### Partial agonists

* 2C-B[77]
* 2C-E[77]
* 2C-T-2[77]
* 4C-T-2[77]
* 5-CT
* 5-MT
* 5-MeO-DiPT[77]
* 5-MeO-DMT
* 5-MeO-MiPT[77]
* 5-MeO-TMT[77]
* 6-F-DMT[77]
* Adatanserin
* αET
* αMT
* Aripiprazole
* Asenapine
* Bacoside
* Bay R 1531
* Befiradol
* Binospirone
* Brexpiprazole
* Bufotenin
* Buspirone (postsynaptic 5-HT1A)
* Cannabidiol[78]
* Cariprazine
* Clozapine
* cis-LSZ[77]
* Dihydroergotamine
* Dimethyltryptamine
* DiPT[77]
* DOET[77]
* DOI[77]
* DPT[77]
* Ebalzotan
* Eltoprazine
* EMDT[77]
* Ergotamine
* Etoperidone
* F-11,461
* F-12,826
* F-13,714
* F-14,679
* Flesinoxan
* Flibanserin
* Ginkgo biloba[79]
* Gepirone
* Haloperidol
* Lamotrigine
* Ipsapirone
* Limonene
* Lisuride
* Lurasidone
* LY-301,317
* Lysergic acid diethylamide (LSD)
* Mescaline[77]
* 3,4-Methylenedioxyamphetamine (MDA)[77]
* 3,4-Methylenedioxymethamphetamine (MDMA)[80]
* Methylphenidate
* Methysergide
* Naluzotan
* NBUMP
* Nefazodone
* Olanzapine
* Osemozotan (postsynaptic 5-HT1A)
* Perospirone
* Pyrimidinylpiperazine
* Piclozotan
* Psilocin
* Psilocybin
* Quetiapine
* Rauwolscine
* Roxindole
* RR-2B[77]
* RU-24,969
* S-15,535
* Sarizotan
* SS-2C[77]
* SSR-181,507
* Sunepitron
* Tandospirone
* Tiospirone
* Trazodone
* Trifluoromethylphenylpiperazine
* Trimethoxyamphetamine[77]
* Umespirone
* Urapidil
* Vilazodone
* Xaliproden
* Yohimbine[81][82][83][84]
* Zalospirone
* Ziprasidone

#### Full agonists

* 8-OH-DPAT[85]
* Alnespirone
* Buspirone (presynaptic 5-HT1A)
* Befiradol
* Tetrahydrocannabivarin (THCV)
* Eptapirone
* Lesopitron
* MKC-242
* LY-293,284
* Osemozotan (presynaptic 5-HT1A)
* Repinotan
* U-92,016-A
* Flibanserin
* Vortioxetine

#### Biased agonists

* HBK-17 – β-arrestin biased agonist[86]
* NLX-204 – ERK1/2 preferring agonist[87]
* F-15,599, also known as NLX-101

### Antagonists

* Alprenolol
* AV-965
* Binospirone (postsynaptic 5-HT1A)
* BMY-7,378
* Cannabigerol
* Cyanopindolol
* Cyproheptadine
* Dotarizine
* Flopropione
* GR-46,611
* Iodocyanopindolol
* Isamoltane
* Lecozotan
* Mefway
* Methiothepin
* MPPF
* NAN-190
* Nebivolol
* Oxprenolol
* Pindobind
* Pindolol (presynaptic 5-HT1A)
* Propranolol
* Risperidone (weak)
* Robalzotan
* SB-649,915
* SDZ-216,525
* Spiperone
* Spiramide
* Spiroxatrine
* UH-301
* WAY-100,135
* WAY-100,635
* Xylamidine

[88]

### Allosteric Modulators

* Cholesterol – endogenous PAM[89]
* Oleamide – endogenous PAM[90]
* Zn2+ – endogenous NAM[91]
* AM-2201 – exogenous PAM[92]

## Genetics

The 5-HT1A receptor is coded by the HTR1A gene. There are several human polymorphisms associated with this gene. A 2007 review listed 27 single nucleotide polymorphisms (SNP).[93] The most investigated SNPs are C-1019G (rs6295), C-1018G,[94] Ile28Val (rs1799921), Arg219Leu (rs1800044), and Gly22Ser (rs1799920).[93] Some of the other SNPs are Pro16Leu, Gly272Asp, and the synonymous polymorphism G294A (rs6294). These gene variants have been studied in relation to psychiatric disorders with no definitive results.[93]

## Protein-protein interactions

The 5-HT1A receptor has been shown to interact with brain-derived neurotrophic factor (BDNF), which may play a major role in its regulation of mood and anxiety.[95][96]

### Receptor oligomers

The 5-HT1A receptor forms heterodimers with the following receptors: 5-HT7,[97] 5-HT1B, 5-HT1D, GABAB2, LPA1 (GPCR26), LPA3, S1P1, S1P3.[98]

## See also

* 5-HT receptor
* 5-HT1 receptor

## References

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30. ↑ "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.
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35. ↑ 35.0 35.1 "Aripiprazole, a novel antipsychotic drug, preferentially increases dopamine release in the prefrontal cortex and hippocampus in rat brain". European Journal of Pharmacology 493 (1–3): 75–83. June 2004. doi:10.1016/j.ejphar.2004.04.028. PMID 15189766.
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38. ↑ "Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex". Neurochemistry International 40 (4): 355–60. April 2002. doi:10.1016/S0197-0186(01)00079-1. PMID 11792466.
39. ↑ "Involvement of 5-HT1A receptors in the antidepressant-like activity of gepirone in the forced swimming test in rats". Neuropharmacology 30 (7): 711–7. July 1991. doi:10.1016/0028-3908(91)90178-E. PMID 1681449.
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44. ↑ "Neue Wirkstoffe - Lecozotan" (in de). Österreichische Apothekerzeitung (17/2007): 805. August 13, 2008.
45. ↑ "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". European Journal of Pharmacology 526 (1–3): 125–39. December 2005. doi:10.1016/j.ejphar.2005.09.065. PMID 16310183.
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48. ↑ "Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake". Psychopharmacology 115 (1–2): 173–9. June 1994. doi:10.1007/BF02244769. PMID 7862892.
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51. ↑ "8-OH-DPAT and male rat sexual behavior: partial blockade by noradrenergic lesion and sexual exhaustion". Pharmacology, Biochemistry, and Behavior 56 (1): 111–6. January 1997. doi:10.1016/S0091-3057(96)00165-7. PMID 8981617.
52. ↑ "Flesinoxan: a prosexual drug for male rats". European Journal of Pharmacology 330 (1): 1–9. July 1997. doi:10.1016/S0014-2999(97)00170-2. PMID 9228408.
53. ↑ "5-HT1A receptor agonists prevent in rats the yawning and penile erections induced by direct dopamine agonists". Psychopharmacology 108 (1–2): 47–50. 1992. doi:10.1007/BF02245284. PMID 1357709.
54. ↑ "Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors". European Journal of Pharmacology 321 (3): R11-3. March 1997. doi:10.1016/S0014-2999(97)00050-2. PMID 9085055.
55. ↑ "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): 269–72. May 2007. doi:10.1358/mf.2007.29.4.1075362. PMID 17609739.
56. ↑ "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.
57. ↑ "Pilot study of flesinoxan, a 5-HT1A agonist, in major depression: Effects on sleep REM latency and body temperature". Human Psychopharmacology: Clinical and Experimental 8 (4): 279–283. 2004. doi:10.1002/hup.470080407. http://www3.interscience.wiley.com/journal/109710934/abstract.
58. ↑ "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): R405-13. February 2006. doi:10.1152/ajpregu.00440.2005. PMID 16166206.
59. ↑ 59.0 59.1 "A comparison of the oxytocin and vasopressin responses to the 5-HT1A agonist and potential anxiolytic drug alnespirone (S-20499)". Pharmacology, Biochemistry, and Behavior 60 (3): 677–83. July 1998. doi:10.1016/S0091-3057(98)00025-2. PMID 9678651.
60. ↑ 60.0 60.1 "Differential effects of serotonin (5-HT1A and 5-HT2) agonists and antagonists on renin and corticosterone secretion". Neuroendocrinology 45 (4): 305–10. April 1987. doi:10.1159/000124754. PMID 2952898.
61. ↑ "Stimulation of corticosterone and beta-endorphin secretion in the rat by selective 5-HT receptor subtype activation". European Journal of Pharmacology 137 (1): 1–8. May 1987. doi:10.1016/0014-2999(87)90175-0. PMID 2956114.
62. ↑ "Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study". European Neuropsychopharmacology 14 (2): 151–5. March 2004. doi:10.1016/S0924-977X(03)00108-1. PMID 15013031.
63. ↑ "Interaction between serotonin 5-HT1A receptors and beta-endorphins modulates antidepressant response". Progress in Neuro-Psychopharmacology & Biological Psychiatry 32 (8): 1804–9. December 2008. doi:10.1016/j.pnpbp.2008.07.021. PMID 18725263.
64. ↑ 64.0 64.1 64.2 "Serotonin autoreceptor function and antidepressant drug action". Journal of Psychopharmacology 14 (2): 177–85. June 2000. doi:10.1177/026988110001400208. PMID 10890313.
65. ↑ "Neurobiological mechanisms involved in antidepressant therapies". Clinical Neuropharmacology 16 (5): 387–400. October 1993. doi:10.1097/00002826-199310000-00002. PMID 8221701.
66. ↑ "SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test". Neuropsychopharmacology 32 (10): 2163–72. October 2007. doi:10.1038/sj.npp.1301341. PMID 17356576.
67. ↑ "Therapeutic potential of monoamine transporter substrates". Current Topics in Medicinal Chemistry 6 (17): 1845–59. 2006. doi:10.2174/156802606778249766. PMID 17017961. http://www.bentham-direct.org/pages/content.php?CTMC/2006/00000006/00000017/0004R.SGM. Retrieved 2019-04-30.
68. ↑ 68.0 68.1 "Effects of 5-HT-releasing agents on the extracellullar hippocampal 5-HT of rats. Implications for the development of novel antidepressants with a short onset of action". Neuropharmacology 38 (7): 1055–61. July 1999. doi:10.1016/S0028-3908(99)00023-4. PMID 10428424.
69. ↑ "Drug discrimination studies of the interoceptive cues produced by selective serotonin uptake inhibitors and selective serotonin releasing agents". Psychopharmacology 138 (1): 67–75. July 1998. doi:10.1007/s002130050646. PMID 9694528. http://link.springer.de/link/service/journals/00213/bibs/8138001/81380067.htm. Retrieved 2009-07-05.
70. ↑ "Uptake inhibitors increase extracellular serotonin concentration measured by brain microdialysis". Life Sciences 55 (3): 163–7. 1994. doi:10.1016/0024-3205(94)00876-0. PMID 8007758.
71. ↑ "Acute uptake inhibition increases extracellular serotonin in the rat forebrain". The Journal of Pharmacology and Experimental Therapeutics 265 (3): 1319–24. June 1993. PMID 7685386.
72. ↑ "Acute 5-HT reuptake blockade potentiates human amygdala reactivity". Neuropsychopharmacology 33 (13): 3221–5. December 2008. doi:10.1038/npp.2008.52. PMID 18463627.
73. ↑ "First delineation of 5-HT1A receptors in human brain with PET and [11C]WAY-100635". European Journal of Pharmacology 283 (1–3): R1-3. September 1995. doi:10.1016/0014-2999(95)00438-Q. PMID 7498295.
74. ↑ "Evidence of increased serotonin-1A receptor binding in type 2 diabetes: a positron emission tomography study". Brain Research 927 (1): 97–103. February 2002. doi:10.1016/S0006-8993(01)03297-8. PMID 11814436.
75. ↑ "The serotonin system and spiritual experiences". The American Journal of Psychiatry 160 (11): 1965–9. November 2003. doi:10.1176/appi.ajp.160.11.1965. PMID 14594742.
76. ↑ "[3H]WAY-100635 for 5-HT1A receptor autoradiography in human brain: a comparison with [3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia". Neurochemistry International 30 (6): 565–74. June 1997. doi:10.1016/S0197-0186(96)00124-6. PMID 9152998.
77. ↑ 77.00 77.01 77.02 77.03 77.04 77.05 77.06 77.07 77.08 77.09 77.10 77.11 77.12 77.13 77.14 77.15 77.16 77.17 77.18 "Psychedelics and the human receptorome". PLOS ONE 5 (2): e9019. February 2010. doi:10.1371/journal.pone.0009019. PMID 20126400. Bibcode: 2010PLoSO...5.9019R.
78. ↑ "Agonistic properties of cannabidiol at 5-HT1a receptors". Neurochemical Research 30 (8): 1037–43. August 2005. doi:10.1007/s11064-005-6978-1. PMID 16258853.
79. ↑ "The discriminative stimulus properties of EGb 761, an extract of Ginkgo biloba". Pharmacology, Biochemistry, and Behavior 62 (3): 543–7. March 1999. doi:10.1016/S0091-3057(98)00190-7. PMID 10080249.
80. ↑ Oeri, HE (2020). "Beyond ecstasy: alternative entactogens to 3,4-methylenedioxymethamphetamine with potential applications in psychotherapy". Journal of Psychopharmacology 35 (5): 512–536. doi:10.1177/0269881120920420. PMID 32909493.
81. ↑ "Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". Biochemical Pharmacology 45 (11): 2337–41. June 1993. doi:10.1016/0006-2952(93)90208-E. PMID 8517875.
82. ↑ "Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors". Naunyn-Schmiedeberg's Archives of Pharmacology 323 (2): 149–54. June 1983. doi:10.1007/BF00634263. PMID 6136920.
83. ↑ "Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle". British Journal of Pharmacology 112 (1): 323–31. May 1994. doi:10.1111/j.1476-5381.1994.tb13072.x. PMID 8032658.
84. ↑ "Yohimbine (PIM 567)". Inchem.org. http://www.inchem.org/documents/pims/pharm/yohimbin.htm.
85. ↑ "Full and partial 5-HT1A receptor agonists disrupt learning and performance in rats". The Journal of Pharmacology and Experimental Therapeutics 288 (1): 335–47. January 1999. PMID 9862788. http://jpet.aspetjournals.org/content/288/1/335.full.pdf.
86. ↑ "1A Receptor Ligand With Anxiolytic-Like Activity, Preferentially Activates ß-Arrestin Signaling". Frontiers in Pharmacology 9: 1146. 2018. doi:10.3389/fphar.2018.01146. PMID 30410441.
87. ↑ "1A Receptor-Biased Agonists with Robust Antidepressant-like Activity". Journal of Medicinal Chemistry 62 (5): 2750–2771. March 2019. doi:10.1021/acs.jmedchem.9b00062. PMID 30721053.
88. ↑ "Different pharmacological properties of two enantiomers in a unique beta-blocker, nebivolol". Cardiovascular Therapeutics 26 (2): 115–34. June 2008. doi:10.1111/j.1527-3466.2008.00044.x. PMID 18485134.
89. ↑ "Membrane cholesterol depletion enhances ligand binding function of human serotonin1A receptors in neuronal cells". Biochem Biophys Res Commun 390 (1): 93–6. December 2009. doi:10.1016/j.bbrc.2009.09.072. PMID 19781522.
90. ↑ "Unique allosteric regulation of 5-hydroxytryptamine receptor-mediated signal transduction by oleamide". Proc Natl Acad Sci U S A 94 (25): 14115–9. 1997. doi:10.1073/pnas.94.25.14115. PMID 9391162.
91. ↑ "Allosteric Inhibition of Serotonin 5-HT7 Receptors by Zinc Ions". Mol Neurobiol 55 (4): 2897–2910. 2018. doi:10.1007/s12035-017-0536-0. PMID 28455702.
92. ↑ "Positive Allosteric Modulation of the 5-HT1A Receptor by Indole-Based Synthetic Cannabinoids Abused by Humans". ACS Chem Neurosci 11 (10): 1400–1405. 2020. doi:10.1021/acschemneuro.0c00034. PMID 32324370.
93. ↑ 93.0 93.1 93.2 "5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies". The International Journal of Neuropsychopharmacology 11 (5): 701–21. August 2008. doi:10.1017/S1461145707008218. PMID 18047755.
94. ↑ "A common C-1018G polymorphism in the human 5-HT1A receptor gene". Psychiatric Genetics 9 (2): 105–6. June 1999. doi:10.1097/00041444-199906000-00010. PMID 10412191.
95. ↑ "Interaction between 5-HT1A and BDNF genotypes increases the risk of treatment-resistant depression". Journal of Neural Transmission 114 (8): 1065–8. 2007. doi:10.1007/s00702-007-0705-9. PMID 17401528.
96. ↑ "Brain-derived neurotrophic factor-deficient mice exhibit a hippocampal hyperserotonergic phenotype". The International Journal of Neuropsychopharmacology 11 (1): 79–92. February 2008. doi:10.1017/S1461145707007857. PMID 17559709.
97. ↑ "Heterodimerization of serotonin receptors 5-HT1A and 5-HT7 differentially regulates receptor signalling and trafficking". Journal of Cell Science 125 (Pt 10): 2486–99. May 2012. doi:10.1242/jcs.101337. PMID 22357950. http://pubman.mpdl.mpg.de/pubman/item/escidoc:1481617/component/escidoc:1481618/1481617.pdf.
98. ↑ "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation". The Journal of Biological Chemistry 277 (18): 15482–5. May 2002. doi:10.1074/jbc.M201539200. PMID 11854302.

## External links

* "5-HT1A". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2310.
* Human HTR1A genome location and HTR1A gene details page in the UCSC Genome Browser.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

* v
* t
* e

Amphetamine

Main articles
and
pharmaceuticals|

| Amphetamine|

* Adzenys ER
* Adzenys XR-ODT
* Dyanavel XR
* Evekeo
* Evekeo ODT
* Mixed amphetamine salts
* Adderall
* Adderall XR
* Mydayis

|

Levoamphetamine|

N/A

Dextroamphetamine|

* Dexedrine
* ProCentra
* Zenzedi

Lisdexamfetamine|

* Vyvanse

Neuropharmacology|

| Biomolecular targets|

* TAAR1 (full agonist)
* CART (mRNA inducer)
* 5-HT1A receptor (low affinity ligand)
* MAO (weak competitive inhibitor)

|

Inhibited transporters|

* DAT
* NET
* SERT
* VMAT1
* VMAT2
* EAAT3
* SLC22A3
* SLC22A5

Active metabolites|

* 4-Hydroxyamphetamine
* 4-Hydroxynorephedrine
* Norephedrine

Related articles|

* ADHD
* ADHD management
* Amphetamine psychosis
* Dopamine
* Doping in sport
* Executive functions
* Formetorex
* ΔFosB
* History and culture of substituted amphetamines
* History of Benzedrine
* Methamphetamine
* Methylphenidate
* N-Methylphenethylamine
* Motivational salience
* Incentive salience
* Narcolepsy
* Neurobiological effects of physical exercise § Attention deficit hyperactivity disorder
* Nootropic
* Norepinephrine
* Obesity
* Performance-enhancing substance
* Phenethylamine
* Phentermine
* Phenylacetone
* Recreational drug use
* Serotonin
* Substituted amphetamine
* Trace amine

* Category

* v
* t
* e

Cell signaling / Signal transduction

Signaling pathways|

* GPCR
*   * Wnt
* RTK
* TGF beta
* MAPK/ERK
* Notch
* JAK-STAT
* Akt/PKB
* Fas apoptosis
* Hippo
* PI3K/AKT/mTOR pathway
* Integrin receptors

Agents|

| Receptor ligands|

* Hormones
* Neurotransmitters/Neuropeptides/Neurohormones
* Cytokines
* Growth factors
* Signaling molecules

|

Receptors|

* Cell surface
* Intracellular
* Co-receptor

Second messenger|

* cAMP-dependent pathway
* Ca2+ signaling
* Lipid signaling

Assistants:|

* Signal transducing adaptor protein
* Scaffold protein

Transcription factors|

* General
* Transcription preinitiation complex
* TFIID
* TFIIH

By distance|

* Juxtacrine
* Autocrine / Paracrine
* Endocrine

Other concepts|

* Intracrine action
* Neurocrine signaling
* Synaptic transmission
* Chemical synapse
* Neuroendocrine signaling
* Exocrine signalling
* Pheromones
* Mechanotransduction
* Phototransduction
* Ion channel gating
* Gap junction

* 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

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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