Tetracyclic antidepressant

Class of pharmaceutical drugs

Not to be confused with Tetracycline or Tricyclic antidepressant.

Chemical structure of the TeCA mirtazapine. Notice its four rings fused together.

Tetracyclic antidepressants (TeCAs) are a class of antidepressants that were first introduced in the 1970s. They are named after their tetracyclic chemical structure, containing four rings of atoms, and are closely related to the tricyclic antidepressants (TCAs), which contain three rings of atoms.

## List of TeCAs[edit]

### Marketed[edit]

* Maprotiline (Ludiomil) – can also be classified as a TCA and grouped with the secondary amines
* Mianserin (Tolvon)
* Mirtazapine (Remeron)
* Setiptiline (Tecipul)

Drugs that contain four rings not all fused together but are sometimes still classified as TeCAs include: (Why is this even relevant, these aren’t the same drug classes, should be removed)

* Amoxapine (Asendin) – often classified as a TCA and grouped with the secondary amines
* Quetiapine (Seroquel) - an atypical antipsychotic sometimes used as an adjunct antidepressant

#### Miscellaneous[edit]

* Benzoctamine (Tacitin) – a tetracyclic compound and is closely related to maprotiline, with the two compounds differing only in the length of their side chain, but benzoctamine is not used as an antidepressant and is instead used as an anxiolytic
* Loxapine (Adasuve, Loxitane) – a typical antipsychotic that produces amoxapine as a major metabolite and is said to have antidepressant effects, but it is not usually regarded as a TeCA

Drugs that contain four rings not all fused together but could still be classified as tetracyclic include:

* Mazindol (Mazanor, Sanorex) – a monoamine reuptake inhibitor used as an appetite suppressant and with potential antidepressant effects, but not classified as a TeCA

### Never marketed[edit]

* Aptazapine (CGS-7525A) – a close analogue of mirtazapine
* Esmirtazapine (ORG-50,081) – the (S)-(+) enantiomer of mirtazapine
* Oxaprotiline (C 49-802 BDA) – a close analogue of maprotiline

Drugs that contain four rings not all fused together but could still be classified as tetracyclic include:

* Ciclazindol (WY-23,409) – a close analogue of mazindol

## Pharmacology[edit]

See also: Pharmacology of antidepressants

TeCAs have diverse pharmacology and differ from TCAs in a number of ways. With the exception of amoxapine, TeCAs do not inhibit the reuptake of serotonin[citation needed]. However, aside from mirtazapine, they do inhibit the reuptake of norepinephrine[citation needed]. TeCAs block the serotonin 5-HT2 receptors similarly to TCAs. Besides mirtazapine, they also block the α1-adrenergic receptor[citation needed]. Conversely, whereas TCAs have relatively low affinity for the α2-adrenergic receptor, mianserin and mirtazapine potently antagonize this receptor, and this action is thought to be involved in their antidepressant effects[citation needed]. TeCAs block the histamine H1 receptor similarly to the TCAs, but tend to be even stronger antihistamines than TCAs[citation needed]. On the other hand, in contrast to almost all TCAs, TeCAs have only low affinity for the muscarinic acetylcholine receptors, and for this reason, are associated with few or no anticholinergic side effects[citation needed]. Mianserin and mirtazapine are far less toxic than TCAs in overdose.[1][2]

### Binding profiles[edit]

See also: Tricyclic antidepressant § Binding profiles

The binding profiles of various TeCAs in terms of their affinities (Ki, nM) for various receptors and transporters are as follows:[3]

Compound | SERTTooltip Serotonin transporter | NETTooltip Norepinephrine transporter | DATTooltip Dopamine transporter | 5-HT1A | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT3 | 5-HT6 | 5-HT7 | α1 | α2 | D2 | H1 | H2 | mAChTooltip Muscarinic acetylcholine receptor

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Amoxapine | 58 | 16 | 4,310 | ND | 0.5 | ND | 2.0 | ND | 6.0–50 | 41 | 50 | 2,600 | 3.6–160 | 7.9–25 | ND | 1,000
Maprotiline | 5,800 | 11–12 | 1,000 | ND | 51 | ND | 122 | ND | ND | 50 | 90 | 9,400 | 350–665 | 0.79–2.0 | 776 | 570
Mianserin | 4,000 | 71 | 9,400 | 400–2,600 | 1.6–20 | 1.6–55 | 0.63–6.5 | 5.8–300 | 55–81 | 48–56 | 34 | 3.8–73 | ≥2,100 | 0.30–1.7 | 437 | 820
Mirtazapine | >10,000 | ≥4,600 | >10,000 | ≥3,330 | 6.3–69 | 200 | 8.9–39 | 7.9 | ND | 265 | 316–1,815 | 18–88 | >5,454 | 0.14–1.6 | >10,000 | 670
Setiptiline | >10,000 | 220 | >10,000 | ND | ND | ND | ND | ND | ND | ND | ND | 24 | ND | ND | ND | ND
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. For assay species and references, see the individual drug articles. Most but not all values are for human proteins.

The TeCAs act as antagonists or inverse agonists of the receptors and as inhibitors of the transporters.

## See also[edit]

* List of antidepressants
* Noradrenergic and specific serotonergic antidepressant

## References[edit]

1. ^ Shaw, W. L. (1980-01-01). "The comparative safety of mianserin in overdose". Current Medical Research and Opinion. 6 (sup7): 44–51. doi:10.1185/03007998009114803. ISSN 0300-7995.
2. ^ Waring, W. Stephen; Good, Alison M.; Bateman, D. Nicholas (2007-01-01). "Lack of significant toxicity after mirtazapine overdose: A five-year review of cases admitted to a regional toxicology unit". Clinical Toxicology. 45 (1): 45–50. doi:10.1080/15563650601005837. ISSN 1556-3650. PMID 17357381. S2CID 28546654.
3. ^ Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.

* v
* t
* e

Antidepressants (N06A)

Specific reuptake inhibitors and/or receptor modulators

| SSRIsTooltip Selective serotonin reuptake inhibitors|

* Citalopram
* Escitalopram
* Fluoxetine#
* Fluvoxamine
* Indalpine‡
* Paroxetine
* Sertraline
* Zimelidine‡

|

SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors|

* Desvenlafaxine
* Duloxetine
* Levomilnacipran
* Milnacipran
* Tofenacin
* Venlafaxine

NRIsTooltip Norepinephrine reuptake inhibitors|

* Atomoxetine
* Reboxetine
* Viloxazine

NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors|

* Amineptine‡
* Bupropion
* Nomifensine‡

NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants|

* Mianserin
* Mirtazapine
* Setiptiline

SARIsTooltip Serotonin antagonist and reuptake inhibitors|

* Etoperidone
* Nefazodone
* Trazodone

SMSTooltip Serotonin modulator and stimulators|

* Vilazodone
* Vortioxetine

Others|

* Agomelatine
* Amisulpride
* Dextromethorphan/bupropion
* Esketamine
* Etryptamine‡
* Gepirone
* Indeloxazine
* Flupentixol
* Ketamine§
* Medifoxamine‡
* Metryptamine‡
* Oxaflozane‡
* Pivagabine‡
* Tandospirone
* Teniloxazine
* Tianeptine

Tricyclic and tetracyclic antidepressants

| TCAsTooltip Tricyclic antidepressants|

* Amineptine‡
* Amitriptyline#
* Amitriptylinoxide
* Amoxapine
* Butriptyline‡
* Clomipramine#
* Demexiptiline‡
* Desipramine
* Dibenzepin
* Dimetacrine‡
* Dosulepin
* Doxepin
* Imipramine
* Imipraminoxide‡
* Iprindole‡
* Lofepramine
* Melitracen
* Metapramine‡
* Nitroxazepine
* Nortriptyline
* Noxiptiline
* Opipramol
* Pipofezine
* Propizepine‡
* Protriptyline
* Quinupramine‡
* Tianeptine
* Trimipramine

|

TeCAsTooltip Tetracyclic antidepressants|

* Maprotiline
* Mianserin
* Mirtazapine
* Setiptiline

Others|

* Tiazesim

Monoamine oxidase inhibitors

| Non-selective|

* Irreversible: Benmoxin‡
* Iproclozide‡
* Iproniazid‡
* Isocarboxazid
* Isoniazid#
* Linezolid#
* Mebanazine‡
* Nialamide‡
* Octamoxin‡
* Phenelzine
* Pheniprazine‡
* Phenoxypropazine‡
* Pivhydrazine‡
* Safrazine‡
* Tedizolid
* Tranylcypromine

* Reversible: Caroxazone‡

* Mixed: Bifemelane

|

MAOATooltip Monoamine oxidase A-selective|

* Reversible: Eprobemide
* Metralindole
* Minaprine‡
* Moclobemide
* Pirlindole
* Tetrindole
* Toloxatone

MAOBTooltip Monoamine oxidase B-selective|

* Irreversible: Selegiline

Adjunctive therapies

* Atypical antipsychotics (aripiprazole, brexpiprazole, lurasidone, olanzapine, quetiapine, risperidone)
* Buspirone
* Lithium (lithium carbonate, lithium citrate)
* Thyroid hormones (triiodothyronine (T3), levothyroxine (T4))

Miscellaneous

* Ademetionine (SAMe)
* GABAkine neurosteroids (brexanolone, zuranolone)
* Hypericum perforatum (St. John's Wort)
* Oxitriptan (5-HTP)
* Rubidium chloride (RbCl)
* Tryptophan

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

Pharmacodynamics

* v
* t
* e

Adrenergic receptor modulators

α1|

| Agonists|

* 6-FNE
* Amidephrine
* Buspirone
* Cirazoline
* Corbadrine
* Deoxyepinephrine (epinine, N-methyldopamine)
* Desglymidodrine
* Dexisometheptene
* Dipivefrine
* Dopamine
* Droxidopa (L-DOPS)
* Epinephrine
* Etilefrine
* Etilevodopa
* Ethylnorepinephrine
* Ibopamine
* Indanidine
* Isometheptene
* L-DOPA (levodopa)
* L-Phenylalanine
* L-Tyrosine
* Melevodopa
* Metaraminol
* Methoxamine
* Methyldopa
* Midodrine
* Naphazoline
* Norepinephrine
* Octopamine
* Oxymetazoline
* Phenylephrine
* Phenylpropanolamine
* Synephrine
* Tetryzoline
* Tiamenidine
* XP21279
* Xylometazoline

|

Antagonists|

* Abanoquil
* Ajmalicine
* Alfuzosin
* Anisodamine
* Anisodine
* Atiprosin
* Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone)
* Benoxathian
* Beta blockers (e.g., adimolol, amosulalol, arotinolol, carvedilol, eugenodilol, labetalol)
* Buflomedil
* Bunazosin
* Corynanthine
* Dapiprazole
* Domesticine
* Doxazosin
* Ergolines (e.g., acetergamine, ergotamine, dihydroergotamine, lisuride, nicergoline, terguride)
* Etoperidone
* Fenspiride
* Hydroxyzine
* Indoramin
* Ketanserin
* L-765,314
* mCPP
* Mepiprazole
* Metazosin
* Monatepil
* Moxisylyte
* Naftopidil
* Nantenine
* Neldazosin
* Niaprazine
* Niguldipine
* Pardoprunox
* Pelanserin
* Perlapine
* Phendioxan
* Phenoxybenzamine
* Phentolamine
* Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
* Piperoxan
* Prazosin
* Quinazosin
* Quinidine
* Silodosin
* Spegatrine
* Spiperone
* Talipexole
* Tamsulosin
* Terazosin
* Tiodazosin
* Tolazoline
* Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin)
* Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine)
* Trimazosin
* Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
* Urapidil
* WB-4101
* Zolertine

α2|

| Agonists|

* (R)-3-Nitrobiphenyline
* 4-NEMD
* 6-FNE
* Amitraz
* Apraclonidine
* Brimonidine
* Clonidine
* Corbadrine
* Deoxyepinephrine (epinine, N-methyldopamine)
* Detomidine
* Dexmedetomidine
* Dihydroergotamine
* Dipivefrine
* Dopamine
* Droxidopa (L-DOPS)
* Etilevodopa
* Ergotamine
* Epinephrine
* Etilefrine
* Ethylnorepinephrine
* Guanabenz
* Guanfacine
* Guanoxabenz
* L-DOPA (levodopa)
* L-Phenylalanine
* L-Tyrosine
* Ibopamine
* Lofexidine
* Medetomidine
* Melevodopa
* Methyldopa
* Mivazerol
* Moxonidine
* Naphazoline
* Norepinephrine
* Oxymetazoline
* Phenylpropanolamine
* Piperoxan
* PS75
* Rezatomidine
* Rilmenidine
* Romifidine
* Talipexole
* Tasipimidine
* Tetryzoline
* Tiamenidine
* Tizanidine
* Tolonidine
* Urapidil
* Vatinoxan
* XP21279
* Xylazine
* Xylometazoline

|

Antagonists|

* 1-PP
* Adimolol
* Amesergide
* Aptazapine
* Atipamezole
* Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, olanzapine, paliperidone, quetiapine, risperidone, zotepine)
* Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone)
* BRL-44408
* Buflomedil
* Cirazoline
* Efaroxan
* Esmirtazapine
* Fenmetozole
* Fluparoxan
* Idazoxan
* Ketanserin
* Lisuride
* mCPP
* Mianserin
* Mirtazapine
* NAN-190
* Pardoprunox
* Phentolamine
* Phenoxybenzamine
* Piperoxan
* Piribedil
* Rauwolscine
* Rotigotine
* Setiptiline
* Spegatrine
* Spiroxatrine
* Sunepitron
* Terguride
* Tolazoline
* Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
* Yohimbine

| Agonists|

* Abediterol
* Alifedrine
* Amibegron
* Arbutamine
* Arformoterol
* Arotinolol
* BAAM
* Bambuterol
* Befunolol
* Bitolterol
* Broxaterol
* Buphenine
* Carbuterol
* Carmoterol
* Cimaterol
* Clenbuterol
* Colterol
* Corbadrine
* Denopamine
* Deoxyepinephrine (epinine, N-methyldopamine)
* Dipivefrine
* Dobutamine
* Dopamine
* Dopexamine
* Droxidopa (L-DOPS)
* Epinephrine
* Etafedrine
* Etilefrine
* Etilevodopa
* Ethylnorepinephrine
* Eugenodilol
* Fenoterol
* Formoterol
* Hexoprenaline
* Higenamine
* Ibopamine
* Indacaterol
* Isoetarine
* Isoprenaline
* Isoxsuprine
* L-DOPA (levodopa)
* L-Phenylalanine
* L-Tyrosine
* Levosalbutamol
* Lubabegron
* Mabuterol
* Melevodopa
* Methoxyphenamine
* Methyldopa
* Mirabegron
* Norepinephrine
* Orciprenaline
* Oxyfedrine
* PF-610355
* Phenylpropanolamine
* Pirbuterol
* Prenalterol
* Ractopamine
* Procaterol
* Reproterol
* Rimiterol
* Ritodrine
* Salbutamol
* Salmeterol
* Solabegron
* Terbutaline
* Tretoquinol
* Tulobuterol
* Vibegron
* Vilanterol
* Xamoterol
* XP21279
* Zilpaterol
* Zinterol

|

Antagonists|

* Acebutolol
* Adaprolol
* Adimolol
* Afurolol
* Alprenolol
* Alprenoxime
* Amosulalol
* Ancarolol
* Arnolol
* Arotinolol
* Atenolol
* Befunolol
* Betaxolol
* Bevantolol
* Bisoprolol
* Bopindolol
* Bornaprolol
* Brefonalol
* Bucindolol
* Bucumolol
* Bufetolol
* Bufuralol
* Bunitrolol
* Bunolol
* Bupranolol
* Butaxamine
* Butidrine
* Butofilolol
* Capsinolol
* Carazolol
* Carpindolol
* Carteolol
* Carvedilol
* Celiprolol
* Cetamolol
* Cicloprolol
* Cinamolol
* Cloranolol
* Cyanopindolol
* Dalbraminol
* Dexpropranolol
* Diacetolol
* Dichloroisoprenaline
* Dihydroalprenolol
* Dilevalol
* Diprafenone
* Draquinolol
* Ecastolol
* Epanolol
* Ericolol
* Ersentilide
* Esatenolol
* Esprolol
* Eugenodilol
* Exaprolol
* Falintolol
* Flestolol
* Flusoxolol
* Hydroxycarteolol
* Hydroxytertatolol
* ICI-118,551
* Idropranolol
* Indenolol
* Indopanolol
* Iodocyanopindolol
* Iprocrolol
* Isoxaprolol
* Isamoltane
* Labetalol
* Landiolol
* Levobetaxolol
* Levobunolol
* Levomoprolol
* Medroxalol
* Mepindolol
* Metipranolol
* Metoprolol
* Moprolol
* Nadolol
* Nadoxolol
* Nebivolol
* Nifenalol
* Nipradilol
* Oxprenolol
* Pacrinolol
* Pafenolol
* Pamatolol
* Pargolol
* Penbutolol
* Pindolol
* Practolol
* Primidolol
* Procinolol
* Pronethalol
* Propafenone
* Propranolol
* Ridazolol
* Ronactolol
* Soquinolol
* Sotalol
* Spirendolol
* SR 59230A
* Sulfinalol
* Talinolol
* Tazolol
* Tertatolol
* Tienoxolol
* Tilisolol
* Timolol
* Tiprenolol
* Tolamolol
* Toliprolol
* Xibenolol
* Xipranolol

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

* v
* t
* e

Dopamine receptor modulators

D1-like|

| Agonists|

* Benzazepines: 6-Br-APB
* Fenoldopam
* SKF-38,393
* SKF-77,434
* SKF-81,297
* SKF-82,958
* SKF-83,959
* Trepipam
* Zelandopam

* Ergolines: Cabergoline
* CY-208,243
* Dihydroergocryptine
* LEK-8829
* Lisuride
* Pergolide
* Terguride

* Dihydrexidine derivatives: A-77636
* A-86929
* Adrogolide (ABT-431, DAS-431)
* Dihydrexidine
* Dinapsoline
* Dinoxyline
* Doxanthrine

* Phenethylamines: BCO-001
* Deoxyepinephrine (N-methyldopamine, epinine)
* Dopexamine
* Etilevodopa
* Ibopamine
* L-DOPA (levodopa)
* Melevodopa
* L-Phenylalanine
* L-Tyrosine
* XP21279

* Others: A-68930
* Apomorphine
* Isocorypalmine
* Nuciferine
* PF-6649751
* PF 6669571
* Propylnorapomorphine
* Rotigotine
* SKF-89,145
* SKF-89,626
* Stepholidine
* Tavapadon
* Tetrahydropalmatine

|

PAMs|

* Tetrahydroisoquinolines: DETQ
* DPTQ
* Mevidalen

Antagonists|

* Typical antipsychotics: Butaclamol
* Chlorpromazine
* Chlorprothixene
* Flupentixol (flupenthixol) (+melitracen)
* Fluphenazine
* Loxapine
* Perphenazine (+amitriptyline)
* Pifluthixol
* Thioridazine
* Thiothixene
* Trifluoperazine (+tranylcypromine)
* Zuclopenthixol

* Atypical antipsychotics: Asenapine
* Clorotepine
* Clotiapine
* Clozapine
* DHA-clozapine
* Fluperlapine
* Iloperidone
* Norclozapine
* Norquetiapine
* Olanzapine (+fluoxetine)
* Paliperidone
* Quetiapine
* Risperidone
* Tefludazine
* Zicronapine
* Ziprasidone
* Zotepine

* Others: Berupipam
* Ecopipam
* EEDQ
* Metitepine (methiothepin)
* Odapipam
* Perlapine
* SCH-23390

D2-like|

| Agonists|

* Adamantanes: Amantadine
* Memantine
* Rimantadine

* Aminotetralins: 5-OH-DPAT
* 7-OH-DPAT
* 8-OH-PBZI
* Rotigotine
* UH-232

* Ergolines: Bromocriptine
* Cabergoline
* Chanoclavine
* Dihydroergocryptine
* Epicriptine
* Ergocornine
* Lergotrile
* Lisuride
* LSD
* Pergolide
* Terguride

* Dihydrexidine derivatives: 2-OH-NPA
* Ciladopa
* Dihydrexidine
* Dinoxyline
* N,N-Propyldihydrexidine

* Phenethylamines: Deoxyepinephrine (N-methyldopamine, epinine)
* Dopexamine
* Etilevodopa
* Ibopamine
* L-DOPA (levodopa)
* L-Phenylalanine
* L-Tyrosine
* Melevodopa
* XP21279

* Atypical antipsychotics: Alentemol (U-66444B)
* Aripiprazole (+sertraline)
* Aripiprazole lauroxil
* Bifeprunox
* Brexpiprazole
* Brilaroxazine
* Cariprazine
* F-15063
* Lumateperone
* Norclozapine

* Others: 3-PPP
* A-412997
* ABT-670
* ABT-724
* Adrafinil
* Aplindore
* Apomorphine
* Arketamine
* Armodafinil
* BP-897
* Captodiame
* CP-226,269
* Dizocilpine
* Esketamine
* Flibanserin
* Ketamine
* Mesulergine
* Modafinil
* OSU-6162
* Pardoprunox
* PD-128,907
* PD-168,077
* PF-219,061
* PF-592,379
* Phencyclidine
* Piribedil
* Pramipexole
* Preclamol
* Propylnorapomorphine
* Pukateine
* Quinagolide
* Quinelorane
* Quinpirole
* RDS-127
* Ro10-5824
* Ropinirole
* Roxindole
* Salvinorin A
* SKF-83,959
* Sumanirole
* Talipexole
* Umespirone
* WAY-100,635

|

Antagonists|

* Typical antipsychotics: Acepromazine
* Acetophenazine
* Azaperone
* Benperidol
* Bromperidol
* Butaclamol
* Butaperazine
* Chloracizine
* Chlorproethazine
* Chlorpromazine
* Chlorprothixene
* Ciclindole
* Clopenthixol
* Clothixamide
* Clopimozide
* Droperidol
* Fluacizine
* Fluanisone
* Flucindole
* Fluotracen
* Flupentixol (flupenthixol) (+melitracen)
* Fluphenazine
* Fluprothixene
* Fluspirilene
* Haloperidol
* Homopipramol
* Lenperone
* Levomepromazine (methotrimeprazine)
* Levosulpiride
* Loxapine
* Mesoridazine
* Moperone
* Naranol
* Nemonapride
* Penfluridol
* Perathiepin
* Perazine
* Pericyazine (periciazine)
* Perphenazine (+amitriptyline)
* Piflutixol (pifluthixol)
* Pimozide
* Pipamperone
* Preclamol
* Prochlorperazine
* Promazine
* Prothipendyl
* Spiperone (spiroperidol)
* Sulforidazine
* Sulpiride
* Sultopride
* Teflutixol
* Thiopropazate
* Thioproperazine
* Thioridazine
* Thiothixene
* Timiperone
* Trifluoperazine (+tranylcypromine)
* Triflupromazine
* Trifluperidol
* Zetidoline
* Zuclopenthixol

* Atypical antipsychotics: Amisulpride
* Asenapine
* BL-1020
* Blonanserin
* Carpipramine
* Cinuperone
* Clocapramine
* Clorotepine
* Clotiapine (clothiapine)
* Clozapine
* Cyamemazine
* DHA-clozapine
* Dixyrazine
* Elopiprazole
* Flumezapine
* Fluperlapine
* Gevotroline
* Iloperidone
* Lurasidone
* Mazapertine
* Melperone
* Molindone
* Mosapramine
* Ocaperidone
* Olanzapine (+fluoxetine)
* Paliperidone
* Perospirone
* Piperacetazine
* Pipotiazine
* Piquindone
* Quetiapine
* Remoxipride
* Risperidone
* Sertindole
* Tefludazine
* Tenilapine
* Tiospirone
* Veralipride
* Zicronapine
* Ziprasidone
* Zotepine

* Antiemetics/gastroprokinetics/sedatives: Aceprometazine
* AS-8112
* Alimemazine
* Alizapride
* Benzquinamide
* Bromopride
* Clebopride
* Deudomperidone
* Domperidone
* Eticlopride
* Hydroxyzine
* Itopride
* Metoclopramide
* Metopimazine
* Promethazine
* Thiethylperazine
* Trazpiroben
* Trimethobenzamide

* Antidepressants: Amoxapine
* Nefazodone
* Opipramol
* Propiomazine
* Trimipramine

* Others: 3-PPP
* Alpiropride
* Azapride
* Bromerguride
* Bromocriptine
* Buspirone
* Desmethoxyfallypride
* EEDQ
* F-15063
* Fallypride
* Fananserin
* Fenfluramine
* Iodobenzamide
* Isocorypalmine
* L-741,626
* L-745,870
* Levofenfluramine
* LEK-8829
* Metergoline
* Metitepine (methiothepin)
* N-Methylspiperone
* Nafadotride
* Nuciferine
* PNU-99,194
* Pridopidine
* Raclopride
* Sarizotan
* SB-277,011-A
* Seridopidine
* Sonepiprazole
* Spiroxatrine
* Stepholidine
* SV-293
* Terguride
* Tetrahydropalmatine
* Tiapride
* UH-232
* Yohimbine

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

* v
* t
* e

Histamine receptor modulators

H1|

| Agonists|

* 2-Pyridylethylamine
* Betahistine
* Histamine
* HTMT
* L-Histidine
* UR-AK49

|

Antagonists|

* First-generation: 4-Methyldiphenhydramine
* Alimemazine
* Antazoline
* Azatadine
* Bamipine
* Benzatropine (benztropine)
* Bepotastine
* Bromazine
* Brompheniramine
* Buclizine
* Captodiame
* Carbinoxamine
* Chlorcyclizine
* Chloropyramine
* Chlorothen
* Chlorphenamine
* Chlorphenoxamine
* Cinnarizine
* Clemastine
* Clobenzepam
* Clocinizine
* Cloperastine
* Cyclizine
* Cyproheptadine
* Dacemazine
* Decloxizine
* Deptropine
* Dexbrompheniramine
* Dexchlorpheniramine
* Dimenhydrinate
* Dimetindene
* Diphenhydramine
* Diphenylpyraline
* Doxylamine
* Embramine
* Etodroxizine
* Etybenzatropine (ethylbenztropine)
* Etymemazine
* Fenethazine
* Flunarizine
* Histapyrrodine
* Homochlorcyclizine
* Hydroxyethylpromethazine
* Hydroxyzine
* Isopromethazine
* Isothipendyl
* Meclozine
* Medrylamine
* Mepyramine (pyrilamine)
* Mequitazine
* Methafurylene
* Methapyrilene
* Methdilazine
* Moxastine
* Orphenadrine
* Oxatomide
* Oxomemazine
* Perlapine
* Phenindamine
* Pheniramine
* Phenyltoloxamine
* Pimethixene
* Piperoxan
* Pipoxizine
* Promethazine
* Propiomazine
* Pyrrobutamine
* Talastine
* Thenalidine
* Thenyldiamine
* Thiazinamium
* Thonzylamine
* Tolpropamine
* Tripelennamine
* Triprolidine

* Second/third-generation: Acrivastine
* Alinastine
* Astemizole
* Azelastine
* Bamirastine
* Barmastine
* Bepiastine
* Bepotastine
* Bilastine
* Cabastinen
* Carebastine
* Cetirizine
* Clemastine
* Clemizole
* Clobenztropine
* Desloratadine
* Dorastine
* Ebastine
* Efletirizine
* Emedastine
* Epinastine
* Fexofenadine
* Flezelastine
* Ketotifen
* Latrepirdine
* Levocabastine
* Levocetirizine
* Linetastine
* Loratadine
* Mapinastine
* Mebhydrolin
* Mizolastine
* Moxastine
* Noberastine
* Octastine
* Olopatadine
* Perastine
* Pibaxizine
* Piclopastine
* Quifenadine (phencarol)
* Rocastine
* Rupatadine
* Setastine
* Sequifenadine (bicarphen)
* Talastine
* Temelastine
* Terfenadine
* Vapitadine
* Zepastine

* Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
* Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
* Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
* Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
* Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)

* Unknown/unsorted: Azanator
* Belarizine
* Elbanizine
* Flotrenizine
* GSK1004723
* Napactadine
* Tagorizine
* Trelnarizine
* Trenizine

H2|

| Agonists|

* Amthamine
* Betazole
* Dimaprit
* Histamine
* HTMT
* Impromidine
* L-Histidine
* UR-AK49

|

Antagonists|

* Bisfentidine
* Burimamide
* Cimetidine
* Dalcotidine
* Donetidine
* Ebrotidine
* Etintidine
* Famotidine
* Isolamtidine
* Lafutidine
* Lamtidine
* Lavoltidine (loxtidine)
* Lupitidine
* Metiamide
* Mifentidine
* Niperotidine
* Nizatidine
* Osutidine
* Oxmetidine
* Pibutidine
* Quisultazine (quisultidine)
* Ramixotidine
* Ranitidine
* Roxatidine
* Sufotidine
* Tiotidine
* Tuvatidine
* Venritidine
* Xaltidine
* Zolantidine

H3|

| Agonists|

* α-Methylhistamine
* Cipralisant
* Histamine
* Imetit
* Immepip
* Immethridine
* L-Histidine
* Methimepip
* Proxyfan

|

Antagonists|

* A-349821
* A-423579
* ABT-239
* ABT-652
* AZD5213
* Bavisant
* Betahistine
* Burimamide
* Ciproxifan
* Clobenpropit
* Conessine
* Enerisant
* GSK-189254
* Impentamine
* Iodophenpropit
* Irdabisant
* JNJ-5207852
* NNC 38-1049
* PF-03654746
* Pitolisant
* SCH-79687
* Thioperamide
* VUF-5681

H4|

| Agonists|

* 4-Methylhistamine
* α-Methylhistamine
* Histamine
* L-Histidine
* OUP-16
* VUF-8430

|

Antagonists|

* JNJ-7777120
* Mianserin
* Seliforant
* Thioperamide
* Toreforant
* VUF-6002

See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors

* v
* t
* e

Monoamine reuptake inhibitors

DATTooltip Dopamine transporter
(DRIsTooltip Dopamine reuptake inhibitors)|

* Piperazines: DBL-583
* GBR-12783
* GBR-12935
* GBR-13069
* GBR-13098
* Nefazodone
* Vanoxerine

* Piperidines: 4-Fluoropethidine
* Benocyclidine (BTCP)
* Desoxypipradrol
* Dexmethylphenidate
* Difemetorex
* Ethylphenidate
* HDMP-28
* Methylphenidate
* Pethidine (meperidine)
* Phencyclidine
* Pipradrol
* Serdexmethylphenidate
* Tenocyclidine

* Pyrrolidines: Diphenylprolinol
* MDPV
* Naphyrone
* Prolintane
* Pyrovalerone

* Tropanes: Altropane
* Benzatropine (benztropine)
* Brasofensine
* CFT
* Cocaine
* Dichloropane
* Difluoropine
* Etybenzatropine (ethybenztropine)
* FE-β-CPPIT
* FP-β-CPPIT
* Ioflupane (123I)
* RTI-55
* RTI-112
* RTI-113
* RTI-121
* RTI-126
* RTI-150
* RTI-177
* RTI-229
* RTI-336
* Tesofensine
* Troparil
* Tropoxane
* WF-11
* WF-23
* WF-31
* WF-33

* Others: Adrafinil
* Amifitadine
* Armodafinil
* Amfonelic acid
* Amineptine
* Ansofaxine
* BTQ
* BTS 74,398
* Bupropion
* Chaenomeles speciosa
* Ciclazindol
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine (BTS-54354)
* Diclofensine
* Didesmethylsibutramine (BTS-54505)
* Dimethocaine
* Diphenylpyraline
* Dizocilpine (MK-801)
* DOV-102,677
* DOV-216,303
* Efavirenz
* Ephenidine
* Esketamine
* EXP-561
* Fencamfamin
* Fezolamine
* Fluorenol
* GYKI-52895
* Hydroxybupropion
* Indatraline
* Ketamine
* Lefetamine
* Levophacetoperane
* Liafensine
* LR-5182
* Manifaxine
* Mazindol
* Medifoxamine
* Mesocarb
* Metaphit
* MIN-117 (WF-516)
* Modafinil
* Nefopam
* Nomifensine
* NS-2359
* O-2172
* Oroxylin A
* Perafensine
* Pridefine
* Radafaxine
* Rimcazole
* Sertraline
* Sibutramine
* Solriamfetol
* Tametraline
* Tedatioxetine
* Threohydrobupropion
* Tripelennamine
* Venlafaxine

NETTooltip Norepinephrine transporter
(NRIsTooltip Norepinephrine reuptake inhibitors)|

* Selective norepinephrine reuptake inhibitors: Amedalin
* Alseroxylon
* Ciclazindol
* Daledalin
* Edivoxetine
* Esreboxetine
* Lortalamine
* Mazindol
* Nisoxetine
* Reboxetine
* Talopram
* Talsupram
* Tandamine
* Teniloxazine
* Viloxazine

* Norepinephrine–dopamine reuptake inhibitors: Amineptine
* Bupropion
* Fencamine
* Fencamfamin
* Hydroxybupropion
* Lefetamine
* Levophacetoperane
* LR-5182
* Manifaxine
* Methylphenidate
* Nomifensine
* O-2172
* Radafaxine
* Serdexmethylphenidate
* Solriamfetol

* Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
* CP-39,332
* Desvenlafaxine
* Duloxetine
* Eclanamine
* Levomilnacipran
* McN5652
* Milnacipran
* N-Methyl-PPPA
* Nafenodone
* PPPA
* Tofenacin
* Venlafaxine

* Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
* Amifitadine
* Ansofaxine
* Bicifadine
* Brasofensine
* Centanafadine
* Cocaine
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine (BTS-54354)
* Diclofensine
* Didesmethylsibutramine (BTS-54505)
* DOV-102677
* DOV-216303
* EXP-561
* Fezolamine
* HDMP-28
* HP-505
* Indatraline
* JNJ-7925476
* JZ-IV-10
* Liafensine
* Mazindol
* Naphyrone
* Nefazodone
* Nefopam
* NS-2359
* Perafensine
* PRC200
* Pridefine
* SEP-228431
* SEP-228432
* Sibutramine
* Tedatioxetine
* Tesofensine
* Threohydrobupropion
* Tropanes (e.g., cocaine)

* Tricyclic antidepressants: Amitriptyline
* Butriptyline
* Cianopramine
* Clomipramine
* Desipramine
* Dosulepin (dothiepin)
* Doxepin
* Imipramine
* Lofepramine
* Melitracen
* Nortriptyline
* Protriptyline
* Trimipramine

* Tetracyclic antidepressants: Amoxapine
* Maprotiline
* Mianserin
* Oxaprotiline
* Setiptiline

* Others: Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine)
* Antipsychotics (e.g., loxapine, ziprasidone)
* Arylcyclohexylamines (e.g., ketamine, phencyclidine)
* Dopexamine
* Ephenidine
* Ginkgo biloba
* Indeloxazine
* Nefazodone
* Opioids (e.g., desmetramadol, methadone, pethidine (meperidine), tapentadol, tramadol, levorphanol)

SERTTooltip Serotonin transporter
(SRIsTooltip Serotonin reuptake inhibitors)|

* Selective serotonin reuptake inhibitors: 6-Nitroquipazine
* Alaproclate
* Centpropazine
* Cericlamine
* Citalopram
* Dapoxetine
* Desmethylcitalopram
* Didesmethylcitalopram
* Escitalopram
* Femoxetine
* Fluoxetine
* Fluvoxamine
* Indalpine
* Ifoxetine
* Norfluoxetine
* Omiloxetine
* Panuramine
* Paroxetine
* PIM-35
* Pirandamine
* RTI-353
* Seproxetine
* Sertraline
* Zimelidine

* Selective serotonin reuptake inhibitors and serotonin receptor modulators: Etoperidone
* Litoxetine
* Lubazodone
* LY-393558
* Quipazine
* SB-649915
* TGBA01AD
* Trazodone
* Vilazodone
* Vortioxetine

* Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
* Bicifadine
* CP-39332
* Desvenlafaxine
* Duloxetine
* Eclanamine
* Levomilnacipran
* McN5652
* Milnacipran
* N-Methyl-PPPA
* PPPA
* Tofenacin
* Venlafaxine

* Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
* Amifitadine
* Ansofaxine
* Bicifadine
* Brasofensine
* Centanafadine
* Cocaine
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine (BTS-54354)
* Diclofensine
* Didesmethylsibutramine (BTS-54505)
* DOV-102677
* DOV-216303
* EXP-561
* Fezolamine
* HDMP-28
* HP-505
* Indatraline
* JNJ-7925476
* JZ-IV-10
* Liafensine
* Mazindol
* Naphyrone
* Nefazodone
* Nefopam
* NS-2359
* Perafensine
* PRC200
* Pridefine
* SEP-228431
* SEP-228432
* Sibutramine
* Tedatioxetine
* Tesofensine
* Threohydrobupropion
* Tropanes (e.g., cocaine)

* Tricyclic antidepressants: Amitriptyline
* Cianopramine
* Clomipramine
* Cyanodothiepin
* Desipramine
* Dosulepin (dothiepin)
* Doxepin
* Imipramine
* Lofepramine
* Nortriptyline
* Pipofezine
* Protriptyline

* Others: A-80426
* Amoxapine
* Antihistamines (e.g., brompheniramine, chlorphenamine, dimenhydrinate, diphenhydramine, mepyramine (pyrilamine), pheniramine, tripelennamine)
* Antipsychotics (e.g., loxapine, ziprasidone)
* Arylcyclohexylamines (e.g., 3-MeO-PCP, esketamine, ketamine, methoxetamine, phencyclidine)
* Cyclobenzaprine
* Delucemine
* Dextromethorphan
* Dextrorphan
* Efavirenz
* Hypidone
* Medifoxamine
* Mesembrine
* Mifepristone
* MIN-117 (WF-516)
* N-Me-5-HT
* Opioids (e.g., dextropropoxyphene, methadone, pethidine (meperidine), levorphanol, tapentadol, tramadol)
* Roxindole

VMATsTooltip Vesicular monoamine transporters|

* Amiodarone
* Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
* APP
* AZIK
* Bietaserpine
* Deserpidine
* Deutetrabenazine
* Dihydrotetrabenazine
* Efavirenz
* GBR-12935
* GZ-793A
* Ibogaine
* Ketanserin
* Lobeline
* Methoxytetrabenazine
* Reserpine
* Rose bengal
* Tetrabenazine
* Valbenazine
* Vanoxerine (GBR-12909)

Others|

* DAT enhancers: Luteolin

* DAT modulators: Agonist-like: SoRI-9804
* SoRI-20040; Antagonist-like: SoRI-20041

See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins

* v
* t
* e

Muscarinic acetylcholine receptor modulators

mAChRsTooltip Muscarinic acetylcholine receptors|

| Agonists|

* 77-LH-28-1
* AC-42
* AC-260,584
* Aceclidine
* Acetylcholine
* AF30
* AF150(S)
* AF267B
* Alvameline
* AQRA-741
* Arecoline
* Bethanechol
* Bevonium
* Butyrylcholine
* Carbachol
* CDD-0034
* CDD-0078
* CDD-0097
* CDD-0098
* CDD-0102
* Cevimeline
* Choline
* cis-Dioxolane
* Clozapine
* Desmethylclozapine (norclozapine)
* Ethoxysebacylcholine
* Itameline
* LY-593,039
* L-689,660
* LY-2,033,298
* McNA343
* Methacholine
* Milameline
* Muscarine
* NGX-267
* Ocvimeline
* Oxotremorine
* PD-151,832
* Pilocarpine
* RS86
* Sabcomeline
* SDZ 210-086
* Sebacylcholine
* Suberyldicholine
* Talsaclidine
* Tazomeline
* Thiopilocarpine
* Vedaclidine
* VU-0029767
* VU-0090157
* VU-0152099
* VU-0152100
* VU-0238429
* WAY-132,983
* Xanomeline
* YM-796

|

Antagonists|

* 3-Quinuclidinyl benzilate
* 4-DAMP
* Aclidinium bromide (+formoterol)
* Abediterol
* AF-DX 250
* AF-DX 384
* Ambutonium bromide
* Anisodamine
* Anisodine
* Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, dimetindene, diphenhydramine, doxylamine, meclizine, mequitazine, perlapine, phenindamine, pheniramine, phenyltoloxamine, promethazine, propiomazine, triprolidine)
* AQ-RA 741
* Atropine
* Atropine methonitrate
* Atypical antipsychotics (e.g., clozapine, fluperlapine, olanzapine (+fluoxetine), rilapine, quetiapine, tenilapine, zotepine)
* Benactyzine
* Benzatropine (benztropine)
* Benzilone
* Benzilylcholine mustard
* Benzydamine
* BIBN 99
* Biperiden
* Bornaprine
* Camylofin
* CAR-226,086
* CAR-301,060
* CAR-302,196
* CAR-302,282
* CAR-302,368
* CAR-302,537
* CAR-302,668
* Caramiphen
* Cimetropium bromide
* Clidinium bromide
* Cloperastine
* CS-27349
* Cyclobenzaprine
* Cyclopentolate
* Darifenacin
* DAU-5884
* Desfesoterodine
* Dexetimide
* DIBD
* Dicycloverine (dicyclomine)
* Dihexyverine
* Difemerine
* Diphemanil metilsulfate
* Ditran
* Drofenine
* EA-3167
* EA-3443
* EA-3580
* EA-3834
* Emepronium bromide
* Etanautine
* Etybenzatropine (ethybenztropine)
* Fenpiverinium
* Fentonium bromide
* Fesoterodine
* Flavoxate
* Glycopyrronium bromide (+beclometasone/formoterol, +indacaterol, +neostigmine)
* Hexahydrodifenidol
* Hexahydrosiladifenidol
* Hexbutinol
* Hexocyclium
* Himbacine
* HL-031,120
* Homatropine
* Imidafenacin
* Ipratropium bromide (+salbutamol)
* Isopropamide
* J-104,129
* Hyoscyamine
* Mamba toxin 3
* Mamba toxin 7
* Mazaticol
* Mebeverine
* Meladrazine
* Mepenzolate
* Methantheline
* Methoctramine
* Methylatropine
* Methylhomatropine
* Methylscopolamine
* Metixene
* Muscarinic toxin 7
* N-Ethyl-3-piperidyl benzilate
* N-Methyl-3-piperidyl benzilate
* Nefopam
* Octatropine methylbromide (anisotropine methylbromide)
* Orphenadrine
* Otenzepad (AF-DX 116)
* Otilonium bromide
* Oxapium iodide
* Oxitropium bromide
* Oxybutynin
* Oxyphencyclimine
* Oxyphenonium bromide
* PBID
* PD-102,807
* PD-0298029
* Penthienate
* Pethidine
* pFHHSiD
* Phenglutarimide
* Phenyltoloxamine
* Pipenzolate bromide
* Piperidolate
* Pirenzepine
* Piroheptine
* Pizotifen
* Poldine
* Pridinol
* Prifinium bromide
* Procyclidine
* Profenamine (ethopropazine)
* Propantheline bromide
* Propiverine
* Quinidine
* 3-Quinuclidinyl thiochromane-4-carboxylate
* Revefenacin
* Rociverine
* RU-47,213
* SCH-57,790
* SCH-72,788
* SCH-217,443
* Scopolamine (hyoscine)
* Scopolamine butylbromide (hyoscine butylbromide)
* Silahexacyclium
* Sofpironium bromide
* Solifenacin
* SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., femoxetine, paroxetine)
* Telenzepine
* Terodiline
* Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
* Tiemonium iodide
* Timepidium bromide
* Tiotropium bromide
* Tiquizium bromide
* Tofenacin
* Tolterodine
* Tricyclic antidepressants (e.g., amitriptyline (+perphenazine), amitriptylinoxide, butriptyline, cidoxepin, clomipramine, desipramine, desmethyldesipramine, dibenzepin, dosulepin (dothiepin), doxepin, imipramine, lofepramine, nitroxazepine, northiaden (desmethyldosulepin), nortriptyline, protriptyline, quinupramine, trimipramine)
* Tridihexethyl
* Trihexyphenidyl
* Trimebutine
* Tripitamine (tripitramine)
* Tropacine
* Tropatepine
* Tropicamide
* Trospium chloride
* Typical antipsychotics (e.g., chlorpromazine, chlorprothixene, cyamemazine (cyamepromazine), loxapine, mesoridazine, thioridazine)
* Umeclidinium bromide (+vilanterol)
* WIN-2299
* Xanomeline
* Zamifenacin

Precursors
(and prodrugs)|

* Acetyl-coA
* Adafenoxate
* Choline (lecithin)
* Citicoline
* Cyprodenate
* Dimethylethanolamine
* Glycerophosphocholine
* Meclofenoxate (centrophenoxine)
* Phosphatidylcholine
* Phosphatidylethanolamine
* Phosphorylcholine
* Pirisudanol

See also
Receptor/signaling modulators
Nicotinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators

* 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-11,461
* 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)
* GR-46611
* L-694247
* L-772405
* mCPP
* PNU-109291
* PNU-142633
* Serotonin (5-HT)
* TGBA01AD
* Triptans (e.g., almotriptan, avitriptan, donitriptan, eletriptan, 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: Ergolines (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
* Anpirtoline
* 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
* 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

* v
* t
* e

Tetracyclics

Classes|

* Polyketides
* Tetracenes

Steroids

Antibiotics|

* Tetracyclines
* Tetracycline
* Chlortetracycline
* Demeclocycline
* Doxycycline
* Eravacycline
* Lymecycline
* Minocycline
* Omadacycline
* Oxytetracycline
* Rolitetracycline
* Sarecycline
* Glycylcycline
* Tigecycline
* Triterpenes
* Fusidanes
* Fusidic acid
* Helvolic acid
* Cephalosporin P1

Antidepressants
(TeCAs)|

* Azipramine
* Ciclopramine
* Esmirtazapine
* Mianserin
* Mirtazapine
* Naranol
* Oxaprotiline
* Setiptiline (teciptiline)

Steroids|

* Sex hormones
* Progestogens
* Acetomepregenol
* Chlormadinone acetate
* Danazol
* Delmadinone acetate
* Etonogestrel
* Gestodene
* Hydroxyprogesterone caproate
* Levonorgestrel
* Norethisterone
* Norgestrel
* Progesterone
* Segesterone acetate
* Tibolone
* Sterane
* Cholane
* Cholestane
* Ergostane
* Gonanes
* Androstane
* Estrane
* Pregnane
* Allopregnane
* Norpregnane
* Retropregnane
* Triterpenes
* Cycloartane
* Cucurbitacins
* Cucurbitane
* Dammarane
* Euphane
* Lanostane
* Protostane
* Sterols
* Phytosterols
* Campesterol
* beta-Sitosterol
* Cholesterol
* Stanol esters

*[Ki]: inhibitory constant
*[nM]: nanomolar
*[SERT]: Serotonin transporter
*[NET]: Norepinephrine transporter
*[DAT]: Dopamine transporter
*[mACh]: Muscarinic acetylcholine receptor
*[ND]: No data
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*[SSRIs]: Selective serotonin reuptake inhibitors
*[SNRIs]: Serotonin–norepinephrine reuptake inhibitors
*[NRIs]: Norepinephrine reuptake inhibitors
*[NDRIs]: Norepinephrine–dopamine reuptake inhibitors
*[NaSSAs]: Noradrenergic and specific serotonergic antidepressants
*[SARIs]: Serotonin antagonist and reuptake inhibitors
*[SMS]: Serotonin modulator and stimulators
*[TCAs]: Tricyclic antidepressants
*[TeCAs]: Tetracyclic antidepressants
*[MAOA]: Monoamine oxidase A
*[MAOB]: Monoamine oxidase B
*[SAMe]: S-adenosyl-L-methionine
*[5-HTP]: 5-hydroxytryptophan
*[DRIs]: Dopamine reuptake inhibitors
*[SRIs]: Serotonin reuptake inhibitors
*[VMATs]: Vesicular monoamine transporters
*[mAChRs]: Muscarinic acetylcholine receptors