Later, nelotanserin was repurposed for the treatment of Lewy body dementia (LBD) by Axovant Sciences (now Sio Gene Therapies).[6] In late 2018, the company announced that while nelotanserin was generally well-tolerated by LBD patients in a small Phase 2 clinical trial for the treatment of REM sleep behavior disorder (RBD) and there were positive indications on some secondary trial outcomes such as sleep diaries and some polysomnogram sleep parameters, the drug failed to meet its primary endpoint of reducing the frequency of RBD episodes and would be discontinued.[7]
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
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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
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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)
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5-HT1E | |
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5-HT1F | |
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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
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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
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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
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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
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5-HT4 | |
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5-HT5A | |
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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)
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5-HT7 | | - 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
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- See also: Receptor/signaling modulators
- Adrenergics
- Dopaminergics
- Melatonergics
- Monoamine reuptake inhibitors and releasing agents
- Monoamine metabolism modulators
- Monoamine neurotoxins
|