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  1. World Encyclopedia
  2. 5-HT2 receptor - Wikipedia
5-HT2 receptor - Wikipedia
From Wikipedia, the free encyclopedia
Transmembrane protein

The 5-HT2 receptors are a subfamily of 5-HT receptors that bind the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).[1] The 5-HT2 subfamily consists of three G protein-coupled receptors (GPCRs) which are coupled to Gq/G11 and mediate excitatory neurotransmission,[2] including 5-HT2A, 5-HT2B, and 5-HT2C. For more information, please see the respective main articles of the individual subtypes:

  • 5-HT2A receptor
  • 5-HT2B receptor
  • 5-HT2C receptor

See also

[edit]
  • 5-HT1 receptor
  • 5-HT3 receptor
  • 5-HT4 receptor
  • 5-HT5 receptor
  • 5-HT6 receptor
  • 5-HT7 receptor
  • Category:5-HT2 antagonists

References

[edit]
  1. ^ Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacol. Rev. 46 (2): 157–203. PMID 7938165.
  2. ^ Eison AS, Mullins UL (1996). "Regulation of central 5-HT2A receptors: a review of in vivo studies". Behavioural Brain Research. 73 (1–2): 177–81. doi:10.1016/0166-4328(96)00092-7. PMID 8788498.
  • v
  • t
  • e
Cell surface receptor: G protein-coupled receptors
Class A: Rhodopsin-like
Neurotransmitter
Adrenergic
  • α1 (A
  • B
  • D)
  • α2 (A
  • B
  • C)
  • β1
  • β2
  • β3
Purinergic
  • Adenosine (A1
  • A2A
  • A2B
  • A3)
  • P2Y (1
  • 2
  • 4
  • 5
  • 6
  • 8
  • 9
  • 10
  • 11
  • 12
  • 13
  • 14)
Serotonin
  • (all but 5-HT3) 5-HT1 (A
  • B
  • D
  • E
  • F)
  • 5-HT2 (A
  • B
  • C)
  • 5-HT (4
  • 5A
  • 6
  • 7)
Other
  • Acetylcholine (M1
  • M2
  • M3
  • M4
  • M5)
  • Dopamine
    • D1
    • D2
    • D3
    • D4
    • D5
  • GHB receptor
  • Histamine
    • H1
    • H2
    • H3
    • H4
  • Melatonin (1A
  • 1B
  • 1C)
  • TAAR (1
  • 2
  • 5
  • 6
  • 8
  • 9)
Metabolites and
signaling molecules
Eicosanoid
  • CysLT (1
  • 2)
  • LTB4
    • 1
    • 2
  • FPRL1
  • OXE
  • Prostaglandin
    • DP (1
    • 2), EP (1
    • 2
    • 3
    • 4), FP
  • Prostacyclin
  • Thromboxane
Other
  • Bile acid
  • Cannabinoid (CB1
  • CB2, GPR (18
  • 55
  • 119))
  • EBI2
  • Estrogen
  • Free fatty acid (1
  • 2
  • 3
  • 4)
  • Hydroxycarboxylic acids
    • 1
    • 2
    • 3
  • Lysophosphatidic acid (1
  • 2
  • 3
  • 4
  • 5
  • 6)
  • Lysophospholipid (1
  • 2
  • 3
  • 4
  • 5
  • 6
  • 7
  • 8)
  • Oxoglutarate
  • PAF
  • Sphingosine-1-phosphate (1
  • 2
  • 3
  • 4
  • 5)
  • Succinate
Peptide
Neuropeptide
  • B/W (1
  • 2)
  • FF (1
  • 2)
  • S
  • Y (1
  • 2
  • 4
  • 5)
  • Neuromedin (B
  • U (1
  • 2))
  • Neurotensin (1
  • 2)
Other
  • Anaphylatoxin (C3a
  • C5a (1
  • 2))
  • Angiotensin (1
  • 2)
  • Apelin
  • Bombesin
    • BRS3
    • GRPR
    • NMBR)
    • Bradykinin (B1
    • B2)
  • Chemerin
    • 1
    • 2
  • Chemokine
  • Cholecystokinin (A
  • B)
  • Endothelin
    • A
    • B
  • Formyl peptide (1
  • 2
  • 3)
  • FSH
  • Galanin (1
  • 2
  • 3)
  • Gonadotropin-releasing hormone (1
  • 2)
  • Ghrelin
  • Kisspeptin
  • Luteinizing hormone/choriogonadotropin
  • MAS (1
  • 1L
  • D
  • E
  • F
  • G
  • X1
  • X2
  • X3
  • X4)
  • Melanocortin (1
  • 2
  • 3
  • 4
  • 5)
  • MCHR (1
  • 2)
  • Motilin
  • Opioid (Delta
  • Kappa
  • Mu
  • Nociceptin & Zeta, but not Sigma)
  • Orexin (1
  • 2)
  • Oxytocin
  • Prokineticin (1
  • 2)
  • Prolactin-releasing peptide
  • Relaxin (1
  • 2
  • 3
  • 4)
  • Somatostatin (1
  • 2
  • 3
  • 4
  • 5)
  • Tachykinin (1
  • 2
  • 3)
  • Thyrotropin
  • Thyrotropin-releasing hormone
  • Urotensin-II
  • Vasopressin (1A
  • 1B
  • 2)
Miscellaneous
Taste, bitter
  • TAS2R
    • 1
    • 3
    • 4
    • 5
    • 7
    • 8
    • 9
    • 10
    • 13
    • 14
    • 16
    • 19
    • 20
    • 30
    • 31
    • 38
    • 39
    • 40
    • 41
    • 42
    • 43
    • 45
    • 46
    • 50
    • 60
  • Vomeronasal receptor type 1
Orphan
  • GPR (3
  • 4
  • 6
  • 12
  • 15
  • 17
  • 18
  • 19
  • 20
  • 21
  • 22
  • 26
  • 27
  • 31
  • 32
  • 33
  • 34
  • 35
  • 37
  • 39
  • 42
  • 45
  • 50
  • 52
  • 55
  • 61
  • 62
  • 63
  • 65
  • 68
  • 75
  • 78
  • 82
  • 83
  • 84
  • 85
  • 87
  • 88
  • 101
  • 103
  • 109A
  • 119
  • 132
  • 135
  • 137B
  • 139
  • 141
  • 142
  • 146
  • 148
  • 149
  • 150
  • 151
  • 152
  • 153
  • 160
  • 161
  • 162
  • 171
  • 173
  • 174
  • 176
  • 177
  • 182
  • 183)
Other
  • Adrenomedullin
  • Olfactory
  • Opsin (3
  • 4
  • 5
  • 1LW
  • 1MW
  • 1SW
  • RGR
  • RRH)
  • Protease-activated (1
  • 2
  • 3
  • 4)
  • SREB (1
  • 2
  • 3)
Class B: Secretin-like
Adhesion
  • ADGRB
    • Brain-specific angiogenesis inhibitor
      • 1
      • 2
      • 3
  • ADGRC
    • Cadherin
      • 1
      • 2
      • 3
  • ADGRE
    • EMR
      • 1
      • 2
      • 3
    • CD97
  • ADGRG
    • 1
    • 2
    • 3
    • 4
    • 5
    • 6
    • 7
  • ADGRL
    • Latrophilin
      • 1
      • 2
      • 3
    • ELTD1
Orphan
  • GPR (56
  • 64
  • 97
  • 98
  • 110
  • 111
  • 112
  • 113
  • 114
  • 115
  • 116
  • 123
  • 124
  • 125
  • 126
  • 128
  • 133
  • 143
  • 144
  • 155
  • 157)
Other
  • Calcitonin
  • CALCRL
  • Corticotropin-releasing hormone (1
  • 2)
  • Glucagon (GR
  • GIPR
  • GLP1R
  • GLP2R)
  • Growth-hormone-releasing hormone
  • PACAPR1
  • GPR
  • Methuselah-like proteins
  • Parathyroid hormone (1
  • 2)
  • Secretin
  • Vasoactive intestinal peptide (1
  • 2)
Class C: Metabotropic glutamate / pheromone
Taste, sweet
  • TAS1R
    • 1
    • 2
    • 3
  • Vomeronasal receptor, type 2
Other
  • Calcium-sensing receptor
  • GABAB (1
  • 2)
  • Glutamate receptor (Metabotropic glutamate (1
  • 2
  • 3
  • 4
  • 5
  • 6
  • 7
  • 8))
  • GPRC6A
  • GPR (156
  • 158
  • 179)
  • RAIG (1
  • 2
  • 3
  • 4)
Class F: Frizzled & Smoothened
Frizzled
  • Frizzled (1
  • 2
  • 3
  • 4
  • 5
  • 6
  • 7
  • 8
  • 9
  • 10)
Smoothened
  • Smoothened
  • v
  • t
  • e
Cell signaling / Signal transduction
Signaling pathways
  • GPCR
  • Wnt
  • RTK
    • TGF beta
    • MAPK/ERK
  • Notch
  • JAK-STAT
  • Akt/PKB
  • Fas apoptosis
  • Hippo
  • PI3K/AKT/mTOR pathway
  • Integrin receptors
Agents
Receptor ligands
  • Hormones
  • Neurotransmitters/Neuropeptides/Neurohormones
  • Cytokines
  • Growth factors
  • Signaling molecules
Receptors
  • Cell surface
  • Intracellular
  • Co-receptor
Second messenger
  • cAMP-dependent pathway
  • Ca2+ signaling
  • Lipid signaling
Assistants:
  • Signal transducing adaptor protein
  • Scaffold protein
Transcription factors
  • General
  • Transcription preinitiation complex
  • TFIID
  • TFIIH
By distance
  • Juxtacrine
  • Autocrine / Paracrine
  • Endocrine
Other concepts
  • Intracrine action
  • Neurocrine signaling
    • Synaptic transmission
    • Chemical synapse
  • Neuroendocrine signaling
  • Exocrine signalling
    • Pheromones
  • Mechanotransduction
  • Phototransduction
  • Ion channel gating
  • Gap junction
  • v
  • t
  • e
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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