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Psychopharmacology
Lobeline is a natural alkaloid found in "Indian tobacco" (Lobelia inflata ), "Devil's tobacco" (Lobelia tupa ), "cardinal flower" (Lobelia cardinalis ), "great lobelia" (Lobelia siphilitica ), and Hippobroma longiflora . In its pure form it is a white amorphous powder which is freely soluble in water.
Lobeline has been used as a smoking cessation aid,[1] [2] [3] and may have application in the treatment of other drug addictions such as addiction to amphetamines[4] [5] , cocaine[6] or alcohol.[7] .
Lobeline has multiple mechanisms of action, acting as a VMAT2 ligand,[8] [9] [10] which stimulates dopamine release to a moderate extent when administered alone, but reduces the dopamine release caused by methamphetamine .[11] [12] It also inhibits the reuptake of dopamine and serotonin ,[13] and acts as a mixed agonist-antagonist at nicotinic acetylcholine receptors [14] [15] and an antagonist at μ-opioid receptors .[16]
References Edit
↑ Stead L, Hughes J (2000). Lobeline for smoking cessation. Cochrane Database Syst Rev (2): CD000124.
↑ Marlow SP, Stoller JK. Smoking cessation. Respiratory Care . 2003 Dec;48(12):1238-56. PMID 14651764
↑ Buchhalter AR, Fant RV, Henningfield JE. Novel pharmacological approaches for treating tobacco dependence and withdrawal : current status. Drugs . 2008;68(8):1067-88. PMID 18484799
↑ Neugebauer NM, Harrod SB, Stairs DJ, Crooks PA, Dwoskin LP, Bardo MT. Lobelane decreases methamphetamine self-administration in rats. European Journal of Pharmacology . 2007 Sep 24;571(1):33-8. PMID 17612524
↑ Eyerman DJ, Yamamoto BK. Lobeline attenuates methamphetamine-induced changes in vesicular monoamine transporter 2 immunoreactivity and monoamine depletions in the striatum. Journal of Pharmacology and Experimental Therapeutics . 2005 Jan;312(1):160-9. PMID 15331654
↑ Polston JE, Cunningham CS, Rodvelt KR, Miller DK. Lobeline augments and inhibits cocaine-induced hyperactivity in rats. Life Sciences . 2006 Aug 1;79(10):981-90. PMID 16765386
↑ Farook JM, Lewis B, Gaddis JG, Littleton JM, Barron S. Lobeline, a nicotinic partial agonist attenuates alcohol consumption and preference in male C57BL/6J mice. Physiology and Behavior . 2009 Jun 22;97(3-4):503-6. PMID:19268674
↑ Zheng G, Dwoskin LP, Crooks PA. Vesicular monoamine transporter 2: role as a novel target for drug development. AAPS Journal . 2006 Nov 10;8(4):E682-92. PMID 17233532
↑ Zheng F, Zheng G, Deaciuc AG, Zhan CG, Dwoskin LP, Crooks PA. Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2. Bioorganic and Medicinal Chemistry . 2007 Apr 15;15(8):2975-92. PMID 17331733
↑ Zheng G, Dwoskin LP, Deaciuc AG, Norrholm SD, Crooks PA. Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter. Journal of Medicinal Chemistry . 2005 Aug 25;48(17):5551-60. PMID 16107155
↑ Wilhelm CJ, Johnson RA, Eshleman AJ, Janowsky A. Lobeline effects on tonic and methamphetamine-induced dopamine release. Biochemical Pharmacology . 2008 Mar 15;75(6):1411-5. PMID 18191815
↑ Wilhelm CJ, Johnson RA, Lysko PG, Eshleman AJ, Janowsky A. Effects of methamphetamine and lobeline on vesicular monoamine and dopamine transporter-mediated dopamine release in a cotransfected model system. Journal of Pharmacology and Experimental Therapeutics . 2004 Sep;310(3):1142-51. PMID 15102929
↑ Zheng G, Horton DB, Deaciuc AG, Dwoskin LP, Crooks PA. Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorganic and Medicinal Chemistry Letters . 2006 Oct 1;16(19):5018-21. PMID 16905316
↑ Damaj MI, Patrick GS, Creasy KR, Martin BR. Pharmacology of lobeline, a nicotinic receptor ligand. Journal of Pharmacology and Experimental Therapeutics . 1997 Jul;282(1):410-9. PMID 9223582
↑ Miller DK, Harrod SB, Green TA, Wong MY, Bardo MT, Dwoskin LP. Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats. Pharmacology, Biochemistry and Behaviour . 2003 Jan;74(2):279-86. PMID 12479946
↑ Miller DK, Lever JR, Rodvelt KR, Baskett JA, Will MJ, Kracke GR. Lobeline, a potential pharmacotherapy for drug addiction, binds to mu opioid receptors and diminishes the effects of opioid receptor agonists. Drug and Alcohol Dependence . 2007 Jul 10;89(2-3):282-91. PMID 17368966
Stimulants (N06B )
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See also Sympathomimetic amines
Cholinergics
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Receptor ligands
Agonists : 77-LH-28-1 • AC-42 • AC-260,584 • Aceclidine • Acetylcholine • AF30 • AF150(S) • AF267B • AFDX-384 • Alvameline • AQRA-741 • Arecoline • Bethanechol • Butyrylcholine • Carbachol • CDD-0034 • CDD-0078 • CDD-0097 • CDD-0098 • CDD-0102 • Cevimeline • cis-Dioxolane • Ethoxysebacylcholine • 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 • Suberylcholine • 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 • Anisodamine • Anisodine • Atropine • Atropine Methonitrate • Benactyzine • Benzatropine (Benztropine) • Benzydamine • BIBN 99 • Biperiden • Bornaprine • CAR-226,086 • CAR-301,060 • CAR-302,196 • CAR-302,282 • CAR-302,368 • CAR-302,537 • CAR-302,668 • CS-27349 • Cyclobenzaprine • Cyclopentolate • Darifenacin • DAU-5884 • Dimethindene • Dexetimide • DIBD • Dicyclomine (Dicycloverine) • Ditran • EA-3167 • EA-3443 • EA-3580 • EA-3834 • Elemicin • Etanautine • Etybenzatropine (Ethylbenztropine) • Flavoxate • Himbacine • HL-031,120 • Ipratropium bromide • J-104,129 • Hyoscyamine • Mamba Toxin 3 • Mamba Toxin 7 • Mazaticol • Mebeverine • Methoctramine • Metixene • Myristicin • N -Ethyl-3-Piperidyl Benzilate • N -Methyl-3-Piperidyl Benzilate • Orphenadrine • Otenzepad • Oxybutynin • PBID • PD-102,807 • Penehyclidine • Phenglutarimide • Phenyltoloxamine • Pirenzepine • Piroheptine • Procyclidine • Profenamine • RU-47,213 • SCH-57,790 • SCH-72,788 • SCH-217,443 • Scopolamine (Hyoscine) • Solifenacin • Telenzepine • Tiotropium bromide • Tolterodine • Trihexyphenidyl • Tripitamine • Tropatepine • Tropicamide • WIN-2299 • Xanomeline • Zamifenacin ; Others : 1st Generation Antihistamines (Brompheniramine , chlorphenamine , cyproheptadine , dimenhydrinate , diphenhydramine , doxylamine , mepyramine /pyrilamine , phenindamine , pheniramine , tripelennamine , triprolidine , etc) • Tricyclic Antidepressants (Amitriptyline , doxepin , trimipramine , etc) • Tetracyclic Antidepressants (Amoxapine , maprotiline , etc) • Typical Antipsychotics (Chlorpromazine , thioridazine , etc) • Atypical Antipsychotics (Clozapine , olanzapine , quetiapine , etc)
Agonists : 5-HIAA • A-84,543 • A-366,833 • A-582,941 • A-867,744 • ABT-202 • ABT-418 • ABT-560 • ABT-894 • Acetylcholine • Altinicline • Anabasine • Anatoxin-a • AR-R17779 • Butyrylcholine • Carbachol • Cotinine • Cytisine • Decamethonium • Desformylflustrabromine • Dianicline • Dimethylphenylpiperazinium • Epibatidine • Epiboxidine • Ethanol • Ethoxysebacylcholine • EVP-4473 • EVP-6124 • Galantamine • GTS-21 • Ispronicline • Lobeline • MEM-63,908 (RG-3487) • Nicotine • NS-1738 • PHA-543,613 • PHA-709,829 • PNU-120,596 • PNU-282,987 • Pozanicline • Rivanicline • Sazetidine A • Sebacylcholine • SIB-1508Y • SIB-1553A • SSR-180,711 • Suberylcholine • TC-1698 • TC-1734 • TC-1827 • TC-2216 • TC-5214 • TC-5619 • TC-6683 • Tebanicline • Tropisetron • UB-165 • Varenicline • WAY-317,538 • XY-4083 Antagonists : 18-Methoxycoronaridine • α-Bungarotoxin • α-Conotoxin • Alcuronium • Amantadine • Anatruxonium • Atracurium • Bupropion (Amfebutamone) • Chandonium • Chlorisondamine • Cisatracurium • Coclaurine • Coronaridine • Dacuronium • Decamethonium • Dextromethorphan • Dextropropoxyphene • Dextrorphan • Diadonium • DHβE • Dimethyltubocurarine (Metocurine) • Dipyrandium • Dizocilpine (MK-801) • Doxacurium • Duador • Esketamine • Fazadinium • Gallamine • Hexafluronium • Hexamethonium (Benzohexonium) • Ibogaine • Isoflurane • Ketamine • Kynurenic acid • Laudexium (Laudolissin) • Levacetylmethadol • Malouetine • Mecamylamine • Memantine • Methadone • Methorphan (Racemethorphan) • Methyllycaconitine • Metocurine • Mivacurium • Morphanol (Racemorphanol) • Neramexane • Nitrous Oxide • Pancuronium • Pempidine • Pentamine • Pentolinium • Phencyclidine • Pipecuronium • Radafaxine • Rapacuronium • Rocuronium • Surugatoxin • Suxamethonium (Succinylcholine) • Thiocolchicoside • Toxiferine • Trimethaphan • Tropeinium • Tubocurarine • Vecuronium • Xenon
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Reuptake inhibitors
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Enzyme inhibitors
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Others
Dopaminergics
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Receptor ligands
Adamantanes : Amantadine • Memantine • Rimantadine ; Aminotetralins : 7-OH-DPAT • 8-OH-PBZI • Rotigotine • UH-232 ; Benzazepines : 6-Br-APB • Fenoldopam • SKF-38,393 • SKF-77,434 • SKF-81,297 • SKF-82,958 • SKF-83,959 ; Ergolines : Bromocriptine • Cabergoline • Dihydroergocryptine • Lisuride • LSD • Pergolide ; Dihydrexidine derivatives : 2-OH-NPA • A-86,929 • Ciladopa • Dihydrexidine • Dinapsoline • Dinoxyline • Doxanthrine ; Others : A-68,930 • A-77,636 • A-412,997 • ABT-670 • ABT-724 • Aplindore • Apomorphine • Aripiprazole • Bifeprunox • BP-897 • CY-208,243 • Dizocilpine • Etilevodopa • Flibanserin • Ketamine • Melevodopa • Modafinil • Pardoprunox • Phencyclidine • PD-128,907 • PD-168,077 • PF-219,061 • Piribedil • Pramipexole • Propylnorapomorphine • Pukateine • Quinagolide • Quinelorane • Quinpirole • RDS-127 • Ro10-5824 • Ropinirole • Rotigotine • Roxindole • Salvinorin A • SKF-89,145 • Sumanirole • Terguride • Umespirone • WAY-100,635
Typical antipsychotics : Acepromazine • Azaperone • Benperidol • Bromperidol • Clopenthixol • Chlorpromazine • Chlorprothixene • Droperidol • Flupentixol • Fluphenazine • Fluspirilene • Haloperidol • Loxapine • Mesoridazine • Methotrimeprazine • Nemonapride • Penfluridol • Perazine • Periciazine • Perphenazine • Pimozide • Prochlorperazine • Promazine • Sulforidazine • Sulpiride • Sultopride • Thioridazine • Thiothixene • Trifluoperazine • Triflupromazine • Trifluperidol • Zuclopenthixol ; Atypical antipsychotics : Amisulpride • Asenapine • Blonanserin • Carpipramine • Clocapramine • Clozapine • Gevotroline • Iloperidone • Lurasidone • Melperone • Molindone • Mosapramine • Ocaperidone • Olanzapine • Paliperidone • Perospirone • Piquindone • Quetiapine • Remoxipride • Risperidone • Sertindole • Tiospirone • Ziprasidone • Zotepine ; Antiemetics : AS-8112 • Alizapride • Bromopride • Clebopride • Domperidone • Metoclopramide • Thiethylperazine ; Others : Amoxapine • Buspirone • Butaclamol • Ecopipam • EEDQ • Eticlopride • Fananserin • L-745,870 • Nafadotride • Nuciferine • PNU-99,194 • Raclopride • Sarizotan • SB-277,011-A • SCH-23,390 • SKF-83,566 • SKF-83,959 • Sonepiprazole • Spiperone • Spiroxatrine • Stepholidine • Tetrahydropalmatine • Tiapride • UH-232 • Yohimbine
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Reuptake inhibitors
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Releasing agents
Morpholines : Fenbutrazate • Morazone • Phendimetrazine • Phenmetrazine ; Oxazolines : 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Cyclazodone • Fenozolone • Fluminorex • Pemoline • Thozalinone ; Phenethylamines (also amphetamines , cathinones , phentermines , etc): 2-Hydroxyphenethylamine (2-OH-PEA) • 4-CAB • 4-Methylamphetamine (4-MA) • 4-Methylmethamphetamine (4-MMA) • Alfetamine • Amfecloral • Amfepentorex • Amfepramone • Amphetamine (Dextroamphetamine , Levoamphetamine ) • Amphetaminil • β-Methylphenethylamine (β-Me-PEA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Benzphetamine • Buphedrone • Butylone • Cathine • Cathinone • Clobenzorex • Clortermine • D-Deprenyl • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylamphetamine • Dimethylcathinone (Dimethylpropion, metamfepramone) • Ethcathinone (Ethylpropion) • Ethylamphetamine • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Famprofazone • Fenethylline • Fenproporex • Flephedrone • Fludorex • Furfenorex • Hordenine • Lophophine (Homomyristicylamine) • Mefenorex • Mephedrone • Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine , Levomethamphetamine ) • Methcathinone (Methylpropion) • Methedrone • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA, tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA, homarylamine) • Methylenedioxyphenethylamine (MDPEA, homopiperonylamine) • Methylone • Ortetamine • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paredrine (Norpholedrine, Oxamphetamine) • Phenethylamine (PEA) • Pholedrine • Phenpromethamine • Prenylamine • Propylamphetamine • Tiflorex (Flutiorex) • Tyramine (TRA) • Xylopropamine • Zylofuramine ; Piperazines : 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine (MeOPP, paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP, piperonylpiperazine); Others : 2-Amino-1,2-dihydronaphthalene (2-ADN) • 2-Aminoindane (2-AI) • 2-Aminotetralin (2-AT) • 4-Benzylpiperidine (4-BP) • 5-IAI • Clofenciclan • Cyclopentamine • Cypenamine • Cyprodenate • Feprosidnine • Gilutensin • Heptaminol • Hexacyclonate • Indanylaminopropane (IAP) • Indanorex • Isometheptene • Methylhexanamine • Naphthylaminopropane (NAP) • Octodrine • Phthalimidopropiophenone • Propylhexedrine (Levopropylhexedrine ) • Tuaminoheptane (Tuamine)
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Enzyme inhibitors
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Others
Serotonergics
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5-HT1 receptor ligands
Agonists : Azapirones : Alnespirone • Binospirone • Buspirone • Enilospirone • Eptapirone • Gepirone • Ipsapirone • Perospirone • Revospirone • Tandospirone • Tiospirone • Umespirone • Zalospirone ; Antidepressants : Etoperidone • Nefazodone • Trazodone ; Antipsychotics : Aripiprazole • Asenapine • Clozapine • Quetiapine • Ziprasidone ; Ergolines : Dihydroergotamine • Ergotamine • Lisuride • Methysergide • LSD ; Tryptamines : 5-CT • 5-MeO-DMT • 5-MT • Bufotenin • DMT • Indorenate • Psilocin • Psilocybin ; Others : 8-OH-DPAT • Adatanserin • Befiradol • BMY-14802 • Cannabidiol • Dimemebfe • Ebalzotan • Eltoprazine • F-11,461 • F-12,826 • F-13,714 • F-14,679 • F-15,063 • F-15,599 • Flesinoxan • Flibanserin • Lesopitron • Lu AA21004 • LY-293,284 • LY-301,317 • MKC-242 • NBUMP • Osemozotan • Oxaflozane • Pardoprunox • Piclozotan • Rauwolscine • Repinotan • Roxindole • RU-24,969 • S 14,506 • S-14,671 • S-15,535 • Sarizotan • SSR-181,507 • Sunepitron • U-92,016-A • Urapidil • Vilazodone • Xaliproden • Yohimbine Antagonists : Antipsychotics : Iloperidone • Risperidone • Sertindole ; Beta blockers : Alprenolol • Cyanopindolol • Iodocyanopindolol • Oxprenolol • Pindobind • Pindolol • Propranolol • Tertatolol ; Others : AV965 • BMY-7,378 • CSP-2503 • Dotarizine • Flopropione • GR-46611 • Isamoltane • Lecozotan • Mefway • Metitepine/Methiothepin • MPPF • NAN-190 • PRX-00023 • Robalzotan • S-15535 • SB-649,915 • SDZ 216-525 • Spiperone • Spiramide • Spiroxatrine • UH-301 • WAY-100,135 • WAY-100,635 • Xylamidine
Agonists : Lysergamides : Dihydroergotamine • Ergotamine • Methysergide ; Piperazines : Eltoprazine • TFMPP ; Triptans : Avitriptan • Eletriptan • Sumatriptan • Zolmitriptan ; Tryptamines : 5-CT • 5-MT ; Others : CGS-12066A • CP-93,129 • CP-94,253 • CP-135,807 • RU-24,969 Antagonists : Lysergamides : Metergoline ; Others : AR-A000002 • Elzasonan • GR-127,935 • Isamoltane • Metitepine/Methiothepin • SB-216,641 • SB-224,289 • SB-236,057 • Yohimbine
Agonists : Lysergamides : Dihydroergotamine • Methysergide ; Triptans : Almotriptan • Avitriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan ; Tryptamines : 5-CT • 5-Ethyl-DMT • 5-MT • 5-(Nonyloxy)tryptamine ; Others : CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonists : Lysergamides : Metergoline ; Others : Alniditan • BRL-15,572 • Elzasonan • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Metitepine/Methiothepin • Ritanserin • Yohimbine • Ziprasidone
Agonists : Lysergamides : Methysergide ; Triptans : Eletriptan ; Tryptamines : BRL-54443 • Tryptamine Antagonists : Metitepine/Methiothepin
Agonists : Triptans : Eletriptan • Naratriptan • Sumatriptan ; Tryptamines : 5-MT ; Others : BRL-54443 • Lasmiditan • LY-334,370 Antagonists : Metitepine/Methiothepin
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5-HT2 receptor ligands
Agonists : Lysergamides : ALD-52 • Ergometrine • Lisuride • LA-SS-Az • LSD • LSD-Pip • Lysergic acid 2-butyl amide • Lysergic acid 3-pentyl amide • Methysergide ; Phenethylamines : 25I-NBF • 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2CB-Ind • 2C-C-NBOMe • 2C-E • 2C-I • 2C-TFM-NBOMe • 2C-T-2 • 2C-T-7 • 2C-T-21 • 2CBCB-NBOMe • 2CBFly-NBOMe • Bromo-DragonFLY • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline • TCB-2 • TFMFly ; Piperazines : BZP • Quipazine • TFMPP ; Tryptamines : 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin ; Others : AL-34662 • AL-37350A • Dimemebfe • Medifoxamine • Oxaflozane • PNU-22394 • RH-34 Antagonists : Atypical antipsychotics : Amperozide • Aripiprazole • Carpipramine • Clocapramine • Clozapine • Gevotroline • Iloperidone • Melperone • Mosapramine • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine ; Typical antipsychotics : Loxapine • Pipamperone ; Antidepressants : Amitriptyline • Amoxapine • Aptazapine • Etoperidone • Mianserin • Mirtazapine • Nefazodone • Trazodone ; Others : 5-I-R91150 • AC-90179 • Adatanserin • Altanserin • AMDA • APD-215 • Blonanserin • Cinanserin • CSP-2503 • Cyproheptadine • Deramciclane • Dotarizine • Eplivanserin • Esmirtazapine • Fananserin • Flibanserin • Ketanserin • KML-010 • Lubazodone • Mepiprazole • Metitepine/Methiothepin • Nantenine • Pimavanserin • Pizotifen • Pruvanserin • Rauwolscine • Ritanserin • S-14,671 • Sarpogrelate • Setoperone • Spiperone • Spiramide • SR-46349B • Volinanserin • Xylamidine • Yohimbine
Agonists : Oxazolines : 4-Methylaminorex • Aminorex ; Phenethylamines : Chlorphentermine • Cloforex • DOB • DOC • DOI • DOM • Fenfluramine • MDA • MDMA • Norfenfluramine ; Tryptamines : 5-CT • 5-MT • α-Methyl-5-HT ; Others : BW-723C86 • Cabergoline • mCPP • Pergolide • PNU-22394 • Ro60-0175 Antagonists : Agomelatine • Asenapine • EGIS-7625 • Ketanserin • Lisuride • LY-272,015 • Metitepine/Methiothepin • PRX-08066 • Rauwolscine • Ritanserin • RS-127,445 • Sarpogrelate • SB-200,646 • SB-204,741 • SB-206,553 • SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082 • Tegaserod • Yohimbine
Agonists : Phenethylamines : 2C-B • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • DOB • DOC • DOI • DOM • MDA • MDMA • Mescaline ; Piperazines : Aripiprazole • mCPP • TFMPP ; Tryptamines : 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin ; Others : A-372,159 • AL-38022A • CP-809,101 • Dimemebfe • Lorcaserin • Medifoxamine • MK-212 • Org 12,962 • ORG-37,684 • Oxaflozane • PNU-22394 • Ro60-0175 • Ro60-0213 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348 Antagonists : Atypical antipsychotics : Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine ; Typical antipsychotics : Chlorpromazine • Loxapine • Pipamperone ; Antidepressants : Agomelatine • Amitriptyline • Amoxapine • Aptazapine • Etoperidone • Fluoxetine • Mianserin • Mirtazapine • Nefazodone • Nortriptyline • Trazodone ; Others : Adatanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine • Eltoprazine • Esmirtazapine • FR-260,010 • Ketanserin • Ketotifen • Latrepirdine • Lu AA24530 • Metitepine/Methiothepin • Methysergide • Pizotifen • Ritanserin • RS-102,221 • S-14,671 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Xylamidine
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5-HT3 , 5-HT4 , 5-HT5 , 5-HT6 , 5-HT7 ligands
Agonists : Piperazines : BZP • Quipazine ; Tryptamines : 2-Methyl-5-HT • 5-CT ; Others : Chlorophenylbiguanide • Butanol • Ethanol • Halothane • Isoflurane • RS-56812 • SR-57,227 • SR-57,227-A • Toluene • Trichloroethane • Trichloroethanol • Trichloroethylene • YM-31636 Antagonists : Antiemetics : AS-8112 • Alosetron • Azasetron • Batanopride • Bemesetron • Cilansetron • Dazopride • Dolasetron • Granisetron • Lerisetron • Ondansetron • Palonosetron • Ramosetron • Renzapride • Tropisetron • Zacopride • Zatosetron ; Atypical antipsychotics : Clozapine • Olanzapine • Quetiapine ; Tetracyclic antidepressants : Amoxapine • Mianserin • Mirtazapine ; Others : CSP-2503 • ICS-205,930 • Lu AA21004 • Lu AA24530 • MDL-72,222 • Memantine • Nitrous Oxide • Ricasetron • Sevoflurane • Thujone • Xenon
Agonists : Gastroprokinetic Agents : Cinitapride • Cisapride • Dazopride • Metoclopramide • Mosapride • Prucalopride • Renzapride • Tegaserod • Velusetrag • Zacopride ; Others : 5-MT • BIMU8 • CJ-033,466 • PRX-03140 • RS-67333 • RS-67506 • SL65.0155 • Antagonists : GR-113,808 • GR-125,487 • L-Lysine • Piboserod • RS-39604 • RS-67532 • SB-203,186
Agonists : Lysergamides : Ergotamine • LSD ; Tryptamines : 5-CT ; Others : Valerenic Acid Antagonists : Asenapine • Latrepirdine • Metitepine/Methiothepin • Ritanserin • SB-699,551 * Note that the 5-HT5B receptor is not functional in humans.
Agonists : Lysergamides : Dihydroergotamine • Ergotamine • Lisuride • LSD • Mesulergine • Metergoline • Methysergide ; Tryptamines : 2-Methyl-5-HT • 5-BT • 5-CT • 5-MT • Bufotenin • E-6801 • E-6837 • EMD-386,088 • EMDT • LY-586,713 • N -Methyl-5-HT • Tryptamine ; Others : WAY-181,187 • WAY-208,466 Antagonists : Antidepressants : Amitriptyline • Amoxapine • Clomipramine • Doxepin • Mianserin • Nortriptyline ; Atypical antipsychotics : Aripiprazole • Asenapine • Clozapine • Fluperlapine • Iloperidone • Olanzapine • Tiospirone ; Typical antipsychotics : Chlorpromazine • Loxapine ; Others : BGC20-760 • BVT-5182 • BVT-74316 • EGIS-12,233 • GW-742,457 • Ketanserin • Latrepirdine • Lu AE58054 • Metitepine/Methiothepin • MS-245 • PRX-07034 • Ritanserin • Ro04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 • SB-742,457
Agonists : Lysergamides : LSD ; Tryptamines : 5-CT • 5-MT • Bufotenin ; Others : 8-OH-DPAT • AS-19 • Bifeprunox • LP-12 • LP-44 • RU-24,969 • Sarizotan Antagonists : Lysergamides : 2-Bromo-LSD • Bromocriptine • Dihydroergotamine • Ergotamine • Mesulergine • Metergoline • Methysergide ; Antidepressants : Amitriptyline • Amoxapine • Clomipramine • Imipramine • Maprotiline • Mianserin ; Atypical antipsychotics : Amisulpride • Aripiprazole • Clozapine • Olanzapine • Risperidone • Sertindole • Tiospirone • Ziprasidone • Zotepine ; Typical antipsychotics : Chlorpromazine • Loxapine ; Others : Butaclamol • EGIS-12,233 • Ketanserin • LY-215,840 • Metitepine/Methiothepin • Pimozide • Ritanserin • SB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperone • SSR-181,507
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Reuptake inhibitors
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Enzyme inhibitors
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Others
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