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  1. World Encyclopedia
  2. AVN-211
AVN-211
From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
AVN-211
Clinical data
Other namesCD-008-0173
Identifiers
IUPAC name
  • 5,7-dimethyl-2-(methylsulfanyl)-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine
CAS Number
  • 1173103-84-8
ChemSpider
  • 26387125
UNII
  • L6B63H3RXJ
ChEMBL
  • ChEMBL1668500
CompTox Dashboard (EPA)
  • DTXSID001032056 Edit this at Wikidata
Chemical and physical data
FormulaC15H15N3O2S2
Molar mass333.42 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • Cc1cc(n2c(n1)c(c(n2)SC)S(=O)(=O)c3ccccc3)C
InChI
  • InChI=1S/C15H15N3O2S2/c1-10-9-11(2)18-14(16-10)13(15(17-18)21-3)22(19,20)12-7-5-4-6-8-12/h4-9H,1-3H3
  • Key:KSAUCBGUWGWPDL-UHFFFAOYSA-N

AVN-211 (CD-008-0173) is a drug which acts as a highly selective 5-HT6 receptor antagonist and is under development by Avineuro Pharmaceuticals for the treatment of schizophrenia.[1][2][3] In early 2011, it successfully completed phase IIa clinical trials,[1][4] with benefits on positive symptoms and some procognitive effects observed,[5] and in mid 2013, phase IIb clinical trials for schizophrenia began.[6] Avineuro Pharmaceuticals also expressed intention to start clinical trials of AVN-211 for Alzheimer's disease in 2015.[6][7][needs update]

See also

[edit]
  • List of investigational antipsychotics
  • AVN-101

References

[edit]
  1. ^ a b Ellenbroek BA, Cesura AM (13 October 2014). "Antipsychotics and the Dopamine-Serotonin Connection". In Celanire S, Poli S (eds.). Small Molecule Therapeutics for Schizophrenia. Springer. pp. 31, 37. ISBN 978-3-319-11502-3.
  2. ^ Pharmacology of 5-HT6 receptors. Academic Press. 7 December 2010. pp. 164–. ISBN 978-0-12-384977-9.
  3. ^ "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595. S2CID 8513976.
  4. ^ "Avineuro Pharmaceuticals, Inc. Reports positive Phase 2a clinical proof of concept trial results on AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.
  5. ^ Morozova MA, Lepilkina TA, Rupchev GE, Beniashvily AG, Burminskiy DS, Potanin SS, et al. (August 2014). "Add-on clinical effects of selective antagonist of 5HT6 receptors AVN-211 (CD-008-0173) in patients with schizophrenia stabilized on antipsychotic treatment: pilot study". CNS Spectrums. 19 (4): 316–323. doi:10.1017/S1092852913000394. PMID 23768250. S2CID 25486838.
  6. ^ a b "Avineuro Pharmaceuticals, Inc. Announces beginning of Phase 2b clinical studies of AVN-211, potent small molecule for treatment of schizophrenia". Avineuro Pharmaceuticals, Inc.
  7. ^ Ivachtchenko AV, Lavrovsky Y, Ivanenkov YA (March 2016). "AVN-211, Novel and Highly Selective 5-HT6 Receptor Small Molecule Antagonist, for the Treatment of Alzheimer's Disease". Molecular Pharmaceutics. 13 (3): 945–963. doi:10.1021/acs.molpharmaceut.5b00830. PMID 26886442.

External links

[edit]
  • Pipeline - Avineuro Pharmaceuticals, Inc.
  • v
  • t
  • e
Antipsychotics (N05A)
Typical
  • Butyrophenones: Benperidol
  • Bromperidol
    • Bromperidol decanoate
  • Droperidol
  • Haloperidol#
    • Haloperidol decanoate
  • Moperone
  • Pipamperone
  • Spiperone
  • Timiperone
  • Trifluperidol
  • Diphenylbutylpiperidines: Fluspirilene
  • Penfluridol
  • Pimozide
  • Phenothiazines: Acepromazine
  • Acetophenazine
  • Butaperazine
  • Carphenazine (carfenazine)‡
  • Chlorpromazine
  • Cyamemazine
  • Dixyrazine
  • Fluphenazine
    • Fluphenazine decanoate
    • Fluphenazine enanthate
  • Levomepromazine (methotrimeprazine)
  • Mesoridazine
  • Perazine
  • Periciazine
  • Perphenazine
    • BL-1020
    • Perphenazine decanoate
    • Perphenazine enanthate
  • Piperacetazine
  • Pipotiazine
    • Pipotiazine palmitate
    • Pipotiazine undecylenate
  • Prochlorperazine
  • Promazine
  • Sulforidazine
  • Thiopropazate
  • Thioproperazine
  • Thioridazine
  • Trifluoperazine
  • Triflupromazine
  • Thioxanthenes: Chlorprothixene
  • Clopenthixol
    • Clopenthixol decanoate
  • Flupentixol
    • Flupentixol decanoate
  • Tiotixene (thiothixene)
  • Zuclopenthixol
    • Zuclopenthixol acetate
    • Zuclopenthixol decanoate
Disputed
  • Benzamides: Amisulpride
  • Levosulpiride
  • Nemonapride
  • Remoxipride‡
  • Sulpiride
  • Sultopride
  • Tiapride
  • Veralipride‡
  • Butyrophenones: Melperone
  • Tricyclics: Carpipramine
  • Clocapramine
  • Clorotepine
  • Clotiapine
  • Loxapine
  • Mosapramine
  • Oxyprothepin decanoate
  • Others: Molindone
Atypical
  • Benzisoxazole/benzisothiazoles: Iloperidone
  • Lurasidone
  • Milsaperidone
  • Paliperidone
    • Paliperidone palmitate
  • Perospirone
  • Risperidone#
  • Ziprasidone
  • Butyrophenones: Lumateperone
  • Phenylpiperazines/quinolinones: Aripiprazole
    • Aripiprazole lauroxil
  • Brilaroxazine†
  • Brexpiprazole
  • Cariprazine
  • Tricyclics: Asenapine
  • Clozapine#
  • Olanzapine (+samidorphan)
  • Quetiapine
  • Zotepine
  • Others: Blonanserin
  • Pimavanserin
  • Sertindole
Others
  • Monoamine-depleting agents: Oxypertine
  • Reserpine
  • Tetrabenazine
  • Muscarinic agonists: Xanomeline/trospium chloride
  • Others/unknown: Azacyclonol
  • #WHO-EM
  • ‡Withdrawn from market
  • Clinical trials:
    • †Phase III
    • §Never to phase III
  • v
  • t
  • e
Serotonin receptor modulators
5-HT1
5-HT1A
  • Agonists: 4-F-5-MeO-pyr-T
  • 5-MeO-pip-T
  • 5-MeO-pyr-T
  • 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 (F-11440), gepirone, perospirone, tandospirone)
  • Bay R 1531
  • Befiradol (NLX-112; F-13640)
  • 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-15599 (NLX-101)
  • Flesinoxan
  • Flibanserin
  • Flumexadol
  • Hypidone
  • Lesopitron
  • LY-293284
  • LY-301317
  • mCPP
  • Naluzotan
  • NBUMP
  • NLX-204
  • NLX-266
  • Osemozotan (MKC-242)
  • Oxaflozane
  • Pardoprunox
  • Piclozotan
  • Rauwolscine
  • Repinotan
  • Roxindole
  • RU-24969
  • S-14506
  • 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
  • TMU4142
  • U-92016-A
  • Urapidil
  • Vilazodone
  • Xaliproden
  • Yohimbine
  • Positive allosteric modulators: Oleamide
  • 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-7378
  • 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-649915
  • 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: Alniditan
  • Anpirtoline
  • AZ10419369
  • Benzofurans (e.g., 5-MAPB, 6-MAPB, BK-5-MAPB, BK-6-MAPB)
  • Benzothiophenes (e.g., 5-MAPBT, 6-MAPBT, BK-5-MAPBT)
  • CGS-12066 (CGS-12066A, CGS-12066B)
  • CP-93129
  • CP-94253
  • CP-122288
  • CP-135807
  • Eltoprazine
  • Ergolines (e.g., bromocriptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)
  • mCPP
  • Methylenedioxyphenethylamines (e.g., MDMA, methylone)
  • PGI-7043
  • PZKKN-94
  • RU-24969
  • Serotonin (5-HT)
  • Triptans (e.g., avitriptan, donitriptan, eletriptan, IS-159, sumatriptan, zolmitriptan)
  • TFMPP
  • Tryptamines (e.g., 5-BT, 5-CT, 5-MT, DMT)
  • Vortioxetine
  • Antagonists: AOP-208 (LB-208)
  • AR-A000002
  • Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, tertatolol)
  • Elzasonan
  • Ergolines (e.g., metergoline)
  • F-14258
  • GR-127935
  • Isamoltane
  • LY-393558
  • Metitepine (methiothepin)
  • SB-216641
  • SB-224289
  • SB-236057
  • SB-616234
  • Trelanserin
  • Yohimbine
  • Negative allosteric modulators: 5-HT-moduline
  • Unknown/unsorted: Ergolines (e.g., cabergoline, ergometrine (ergonovine), lisuride)
5-HT1D
  • Agonists: Alniditan
  • CGS-12066 (CGS-12066A, CGS-12066B)
  • CP-122288
  • 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, IS-159, naratriptan, rizatriptan, sumatriptan, zolmitriptan)
  • Tryptamines (e.g., 5-BT, 5-CT, 5-Et-DMT, 5-MT, 5-(nonyloxy)tryptamine, DMT)
  • Antagonists: BRL-15572
  • Elzasonan
  • Ergolines (e.g., metergoline)
  • F-14258
  • GR-127935
  • Ketanserin
  • LY-310762
  • LY-367642
  • LY-393558
  • LY-456219
  • LY-456220
  • Metitepine (methiothepin)
  • Mianserin
  • Ritanserin
  • Yohimbine
  • Ziprasidone
  • Negative allosteric modulators: 5-HT-moduline
  • 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-122288
  • Ergolines (e.g., bromocriptine, lysergol, methylergometrine (methylergonovine) methysergide)
  • Lasmiditan
  • LY-334370
  • LY-344864
  • 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)
  • Positive allosteric modulators: AB0124
  • CTW0404
  • CTW0419
  • JPC0323
  • (R)-Glaucine
  • Oleamide
  • 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)
  • Butanserin
  • Chlorprothixene
  • Cinanserin
  • CSP-2503
  • Deramciclane
  • Dotarizine
  • Eplivanserin
  • Ergolines (e.g., amesergide, LY-53857, LY-215840, mesulergine, metergoline, methysergide, sergolexole)
  • Fananserin
  • Flibanserin
  • Glemanserin
  • Irindalone
  • Ketanserin
  • KML-010
  • Landipirdine
  • LY03017
  • LY-393558
  • mCPP
  • Medifoxamine
  • Metitepine (methiothepin)
  • Metrenperone
  • MIN-117 (WF-516)
  • MT-1207
  • Naftidrofuryl
  • Nantenine
  • Nelotanserin
  • NH130
  • Opiranserin (VVZ-149)
  • Pelanserin
  • Phenoxybenzamine
  • Pimavanserin
  • Pirenperone
  • Pizotifen
  • Pruvanserin
  • Rauwolscine
  • Ritanserin
  • Roluperidone
  • S-14671
  • Sarpogrelate
  • Seganserin
  • Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, triazoledione, trazodone)
  • Temanogrel
  • Teniloxazine
  • Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)
  • TGBA01AD
  • Trelanserin
  • 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
  • ATHX-105
  • Centhaquine
  • 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
  • PRX-00933 (BVT-933; GW-876167)
  • Ro60-0175
  • Ro60-0213
  • Serotonin (5-HT)
  • Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
  • Vabicaserin
  • VR-1065
  • WAY-629
  • WAY-161503
  • YM-348
  • Positive allosteric modulators: CTW0415
  • CYD-1-79
  • JPC0323
  • Oleamide
  • PNU-69176E
  • VA012
  • VA240
  • 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-215840, mesulergine, metergoline, methysergide, sergolexole)
  • Etoperidone
  • Fluoxetine
  • FR260010
  • Irindalone
  • Ketanserin
  • Ketotifen
  • Latrepirdine (dimebolin)
  • LY03017
  • Medifoxamine
  • Metitepine (methiothepin)
  • Nefazodone
  • Pirenperone
  • Pizotifen
  • Propranolol
  • Ritanserin
  • RS-102221
  • S-14671
  • SB-200646
  • SB-206553
  • SB-221284
  • SB-228357
  • SB-242084
  • SB-243213
  • SB-247853
  • SDZ SER-082
  • Seganserin
  • 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
  • Positive allosteric modulators: 5-Aminoindole
  • 5-Chloroindole
  • 5-Hydroxyindole
  • Catechol
  • Chloroform
  • meta-Chlorophenylbiguanide (mCPBG)
  • Colchicine
  • Ethanol (alcohol)
  • Halothane
  • Indole
  • Isoflurane
  • TMPPAA
  • Antagonists: Alosetron
  • Anpirtoline
  • Arazasetron
  • AS-8112
  • Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine)
  • Azasetron
  • Batanopride
  • Bemesetron (MDL-72222)
  • Cilansetron
  • CSP-2503
  • Dazopride
  • Dolasetron
  • Galanolactone
  • Granisetron
  • 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
  • Negative allosteric modulators: Bupropion
  • Colchicine
  • Hydroxybupropion
  • 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-67333
  • RS-67506
  • 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)
  • UCSF648
  • 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-12233
  • GW-742457
  • Idalopirdine
  • Ketanserin
  • Landipirdine
  • Latrepirdine (dimebolin)
  • Masupirdine
  • Metitepine (methiothepin)
  • MS-245
  • PRX-07034
  • PZKKN-94
  • 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-24969
  • 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-12233
  • Ergolines (e.g., 2-Br-LSD (BOL-148), amesergide, bromocriptine, cabergoline, dihydroergotamine, ergotamine, LY-53857, LY-215840, mesulergine, metergoline, methysergide, sergolexole)
  • JNJ-18038683
  • Ketanserin
  • LY-215840
  • 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
  • Negative allosteric modulators: Oleamide
  • 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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