5-HT receptor

5-HT receptor
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Serotonin

The serotonin receptors also known as 5-hydroxytryptamine receptors or 5-HT receptors are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems.[1][2] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. The serotonin receptors are the target of a variety of pharmaceutical and illicit drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[3]
Contents
[hide]

* 1 Classification
o 1.1 Families
o 1.2 Subtypes
* 2 References
* 3 External links

[edit] Classification

With the exception of the 5-HT3 receptor, a ligand-gated ion channel, all other serotonin receptors are G protein-coupled receptors that activate an intracellular second messenger cascade to produce an excitatory or inhibitory response.
[edit] Families
Family Type Mechanism Potential
5-HT1 Gi/Go-protein coupled. Decreasing cellular levels of cAMP. Inhibitory
5-HT2 Gq/G11-protein coupled. Increasing cellular levels of IP3 and DAG. Excitatory
5-HT3 Ligand-gated Na+ and K+ cation channel. Depolarizing plasma membrane. Excitatory
5-HT4 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT5 Gi/Go-protein coupled.[4] Decreasing cellular levels of cAMP. Inhibitory
5-HT6 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT7 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
[edit] Subtypes

Within these general classes of serotonin receptors, a number of specific types have been characterized:[5][6][7]
Overview of Serotonin Receptors
Receptor Gene(s) Distribution Function Agonists Antagonists
5-HT1A

* HTR1A



* Blood Vessels
* CNS



* Addiction [8][9][10]
* Aggression[11]
* Anxiety[12]
* Appetite[13]
* Blood Pressure[14][15]
* Cardiovascular Function[16]
* Emesis[17]
* Heart Rate[14][15]
* Impulsivity[18]
* Memory[19][20]
* Mood[21]
* Nausea[17]
* Nociception[22]
* Penile Erection[23]
* Pupil Dilation[24]
* Respiration[25]
* Sexual Behavior[26]
* Sleep[27]
* Sociability[28]
* Thermoregulation[29]
* Vasoconstriction[30]



* 5-CT
* 8-OH-DPAT
* Aripiprazole
* Buspirone[31] (anxiolytic and antidepressant)[31]
* Cannabidiol
* Clozapine
* Dihydroergotamine
* Eltoprazine
* Ergotamine
* Flesinoxan
* Flibanserin
* Gepirone
* Ipsapirone
* Methysergide
* Nefazodone
* Quetiapine
* RU 24969
* Tandospirone
* Trazodone
* Urapidil
* Xaliproden
* Yohimbine
* Ziprasidone



* Alprenolol
* Asenapine
* BMY 7378
* Cyanopindolol
* Iodocyanopindolol
* Lecozotan
* Methiothepin
* NAN-190
* Oxprenolol
* Pindolol
* Propanolol
* Robalzotan
* S15535
* Spiperone
* UH-301
* WAY-100,135
* WAY-100,635

5-HT1B

* HTR1B



* Blood Vessels
* CNS



* Addiction [32]
* Aggression[11]
* Anxiety[33][34][35]
* Learning[36]
* Locomotion[37]
* Memory[36]
* Mood[35]
* Penile Erection[23]
* Sexual Behavior[26]
* Vasoconstriction



* 5-CT
* CP-93,129
* CP-94,253
* Dihydroergotamine
* Eltoprazine
* Ergotamine
* Methysergide
* RU 24969
* TFMPP
* Triptans[31] (antimigraine[31])
o Zolmitriptan
o Eletriptan
o Sumatriptan



* Alprenolol
* AR-A000002
* Asenapine
* Cyanopindolol
* GR 127935
* Iodocyanopindolol
* Isamoltane
* Metergoline
* Methiothepin
* Oxprenolol
* Pindolol
* Propanolol
* SB-216,641
* Yohimbine

5-HT1D

* HTR1D



* Blood Vessels
* CNS



* Anxiety[38][39]
* Locomotion[37]
* Vasoconstriction



* 5-CT
* Dihydroergotamine
* Ergotamine
* Methysergide
* Triptans[31] (antimigraine[31])
o Almotriptan
o Eletriptan
o Frovatriptan
o Naratriptan
o Rizatriptan
o Sumatriptan
o Zolmitriptan
* Yohimbine



* BRL-15572
* GR 127935
* Ketanserin
* Metergoline
* Methiothepin
* Rauwolscine
* Ritanserin

5-HT1E

* HTR1E



* Blood Vessels
* CNS



* Eletriptan
* Methysergide
* Tryptamine



* Methiothepin

5-HT1F

* HTR1F



* Blood Vessels
* CNS



* Vasoconstriction



* Eletriptan
* Naratriptan
* Sumatriptan



* Methiothepin

5-HT2A

* HTR2A



* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle



* Addiction (potentially modulating) [40]
* Anxiety[41]
* Appetite
* Cognition
* Imagination
* Learning
* Memory
* Mood
* Perception
* Sexual Behavior[42]
* Sleep[43]
* Thermoregulation[44]
* Vasoconstriction[45]



* 2C-B
* 5-MeO-DMT
* BZP
* Bufotenin
* DMT
* DOM
* Ergonovine
* Lisuride
* LSD
* Mescaline
* Myristicin
* Psilocin
* Psilocybin
* TFMPP
* Yohimbine



* Atypical antipsychotics
o Clozapine[31]
o Olanzapine
o Quetiapine
o Risperidone
o Ziprasidone
* Aripiprazole
* Asenapine
* Cyproheptadine
* Eplivanserin
* Etoperidone
* Iloperidone
* Ketanserin[31] (antihypertensive[31])
* Methysergide
* Mianserin
* Mirtazapine
* Nefazodone
* Pimavanserin
* Pizotifen
* Ritanserin
* Trazodone

5-HT2B

* HTR2B



* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle



* Anxiety[46][47][48]
* Appetite[49]
* Cardiovascular Function
* GI Motility[50]
* Sleep[43]
* Vasoconstriction



* BW-723C86
* Fenfluramine
* MDMA
* Norfenfluramine
* Ro60-0175



* Agomelatine
* Asenapine
* BZP
* Ketanserin
* Methysergide
* Ritanserin
* Tegaserod
* Yohimbine

5-HT2C

* HTR2C



* Blood Vessels
* CNS
* GI Tract
* Platelets
* PNS
* Smooth Muscle



* Addiction. (potentially modulating)[40]
* Anxiety[51][52][53]
* Appetite
* GI Motility[54]
* Locomotion
* Mood[53][52]
* Penile Erection[55][56]
* Sexual Behavior[42]
* Sleep[57]
* Thermoregulation[44]
* Vasoconstriction



* A-372,159
* AL-38022A
* Aripiprazole
* Ergonovine
* Lorcaserin
* Ro60-0175
* TFMPP
* Trazodone[31] (hypnotic[31])
* YM-348



* Agomelatine[31] (antidepressant[31])
* Asenapine
* Clozapine[31] (antipsychotic[31])
* Cyproheptadine
* Dimebolin
* Eltoprazine
* Etoperidone
* Fluoxetine
* Iloperidone
* Ketanserin[31] (antihypertensive[31])
* Lisuride
* Methysergide[58]
* Mianserin
* Mirtazapine
* Nefazodone
* Olanzapine
* Quetiapine
* Risperidone
* Ritanserin
* Trazodone
* Ziprasidone

5-HT3

* HTR3A
* HTR3B
* HTR3C
* HTR3D
* HTR3E



* CNS
* GI Tract
* PNS



* Addiction
* Anxiety
* Emesis
* GI Motility
* Learning[59]
* Memory[59]
* Nausea



* 2-Methyl-5-HT
* BZP
* Quipazine
* RS-56812



* Alosetron
* Several antiemetics[31]
o Dolasetron
o Ondansetron[31]
o Granisetron
o Tropisetron
* Clozapine
* Memantine
* Metoclopramide
* Mianserin
* Mirtazapine
* Olanzapine
* Quetiapine

5-HT4

* HTR4



* CNS
* GI Tract
* PNS



* Anxiety[60][61]
* Appetite[62][63]
* GI Motility
* Learning[64][65]
* Memory[66][65][67]
* Mood[68][69]
* Respiration[70][25]



* 5-MT
* BIMU-8
* Cinitapride
* Cisapride[31] (gastroprokinetic)
* Dazopride
* Metoclopramide
* Mosapride
* Prucalopride
* RS-67333
* Renzapride
* Tegaserod
* Zacopride



* L-Lysine[60]
* Piboserod

5-HT5A

* HTR5A



* CNS



* Locomotion[71]
* Sleep[72]



* 5-CT
* Ergotamine
* Valerenic Acid[72]



* Asenapine
* Dimebolin
* Methiothepin
* Ritanserin
* SB-699,551
* SB-699,551-A

5-HT6

* HTR6



* CNS



* Anxiety[73][74]
* Cognition[75]
* Learning[76]
* Memory[76]
* Mood[74][77]



* EMD-386,088
* EMDT



* Aripiprazole
* Asenapine
* Clozapine
* Dimebolin
* EGIS-12233
* Iloperidone
* MS-245
* Olanzapine
* Ro04-6790
* SB-258,585
* SB-271,046[78]
* SB-357,134
* SB-399,885

5-HT7

* HTR7



* Blood Vessels
* CNS
* GI Tract



* Anxiety[79][80]
* Memory[81][82]
* Mood[79][80]
* Respiration[25][83]
* Sleep[79][83][84]
* Thermoregulation
* Vasoconstriction



* 5-CT
* 8-OH-DPAT
* AS-19



* Aripiprazole
* Asenapine
* Clozapine
* EGIS-12233
* Iloperidone
* Ketanserin
* Olanzapine
* Ritanserin
* SB-269,970

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor. Note that there is also no 5-HT5B receptor, as it exists only in mice and rats and not in humans or monkeys.

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[31] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.[31]
[edit] References

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[edit] External links

* MeSH Serotonin+Receptors
* "5-Hydroxytryptamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288.
* Rubenstein, LA, Lanzara RG (2005-02-16). "Activation of G protein-coupled receptors entails cysteine modulation of agonist binding". Cogprints. http://cogprints.org/4095/. Retrieved 2008-04-11.


[show]
v • d • e
Transmembrane 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) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 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) · Lactate · Lysophosphatidic acid (1, 2, 3, 4, 5, 6) · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · 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) · Angiotensin (1, 2) · Apelin · Bombesin (BRS3, GRPR, NMBR) · Bradykinin (B1, B2) · Chemokine · Cholecystokinin (A, B) · Endothelin (A, B) · Formyl peptide (1, 2, 3) · FSH · Galanin (1, 2, 3) · GHB receptor · 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

Orphan

GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 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
Class B: Secretin like
Orphan

GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other

Brain-specific angiogenesis inhibitor (1, 2, 3) · Cadherin (1, 2, 3) · Calcitonin · CALCRL · CD97 · Corticotropin-releasing hormone (1, 2) · EMR (1, 2, 3) · Glucagon (GR, GIPR, GLP1R, GLP2R) · Growth hormone releasing hormone · PACAPR1 · GPR · Latrophilin (1, 2, 3, ELTD1) · Methuselah-like proteins · Parathyroid hormone (1, 2) · Secretin · Vasoactive intestinal peptide (1, 2)
Class C: Metabotropic
glutamate / pheromone
Taste

TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other

Calcium-sensing receptor · GABA B (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
[show]
v • d • e
Ion channel, receptor: ligand-gated ion channels
Cys-loop receptors
5-HT/serotonin

5-HT3 (A, B, C, D, E)
GABA

GABAA (α1, α2, α3, α4, α5, α6, β1, β2, β3, γ1, γ2, γ3, δ, ε, π, θ) · GABAA-ρ (ρ1, ρ2, ρ3)
Glycine

α1 · α2 · α3 · α4 · β
Nicotinic acetylcholine

monomers: α1 · α2 · α3 · α4 · α5 · α6 · α7 · α9 · α10 · β1 · β2 · β3 · β4 · δ · ε
pentamers: (α3)2(β4)3 · (α4)2(β2)3 · (α7)5 · (α1)2(β4)3 - Ganglion type · (α1)2β1δε - Muscle type
Zinc

Zinc-activated
Ionotropic glutamates
Ligand-gated only

AMPA (1, 2, 3, 4) · Kainate (1, 2, 3, 4, 5)
Voltage- and ligand-gated

NMDA (1, 2A, 2B, 2C, 2D, 3A, 3B, L1A, L1B)
‘Orphan’

GluD (δ1, δ2)
ATP-gated channels
Purinergic receptors

P2X (1, 2, 3, 4, 5, 6, 7)
[show]
v • d • e
Serotonergics
[show]

5-HT1 receptor ligands
5-HT1A

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 • 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-92016A • Urapidil • Vilazodone • Xaliproden • Yohimbine
Antagonists: Antipsychotics: Iloperidone • Risperidone • Sertindole; Beta blockers: Alprenolol • Cyanopindolol • Iodocyanopindolol • Oxprenolol • Pindobind • Pindolol • Propranolol • Tertatolol; Others: AV965 • BMY-7378 • CSP-2503 • Dotarizine • Flopropione • GR-46611 • Isamoltane • Lecozotan • Metitepine/Methiothepin • MPPF • NAN-190 • PRX-00023 • Robalzotan • S-15535 • SB-649915 • SDZ 216-525 • Spiperone • Spiramide • Spiroxatrine • UH-301 • WAY-100,135 • WAY-100,635 • Xylamidine
5-HT1B

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-24969
Antagonists: Lysergamides: Metergoline; Others: AR-A000002 • Elzasonan • GR-127,935 • Isamoltane • Metitepine/Methiothepin • SB-216,641 • SB-224,289 • SB-236,057 • Yohimbine
5-HT1D

Agonists: Lysergamides: Dihydroergotamine • Methysergide; Triptans: Almotriptan • Avitriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; 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-15572 • Elzasonan • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Metitepine/Methiothepin • Ritanserin • Yohimbine • Ziprasidone
5-HT1E

Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: BRL-54443 • Tryptamine
Antagonists: Metitepine/Methiothepin
5-HT1F

Agonists: Triptans: Eletriptan • Naratriptan • Sumatriptan; Tryptamines: 5-MT; Others: BRL-54443 • Lasmiditan • LY-334,370
Antagonists: Metitepine/Methiothepin
[show]

5-HT2 receptor ligands
5-HT2A

Agonists: Lysergamides: ALD-52 • Ergonovine • Lisuride • LA-SS-Az • LSD • LSD-Pip • Lysergic acid 2-butyl amide • Methysergide; Phenethylamines: 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2CB-Ind • 2C-E • 2C-I • 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 • Clozapine • Gevotroline • Iloperidone • Melperone • 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
5-HT2B

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 • 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
5-HT2C

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-37,684 • Oxaflozane • PNU-22394 • Ro60-0175 • 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
[show]

5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7 ligands
5-HT3

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
5-HT4

Agonists: Gastroprokinetic Agents: Cinitapride • Cisapride • Dazopride • Metoclopramide • Mosapride • Prucalopride • Renzapride • Tegaserod • Zacopride; Others: 5-MT • BIMU-8 • CJ-033,466 • PRX-03140 • RS-67333 • RS-67506 • SL65.0155 • TD-5108
Antagonists: GR-113,808 • GR-125,487 • L-Lysine • Piboserod • RS-39604 • RS-67532 • SB-203,186
5-HT5A

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.
5-HT6

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-12233 • GW-742,457 • Ketanserin • Latrepirdine • Lu AE58054 • Metitepine/Methiothepin • MS-245 • PRX-07034 • Ritanserin • Ro 04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 • SB-742,457
5-HT7

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-12233 • 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
[show]

Reuptake inhibitors
SERT

Selective serotonin reuptake inhibitors (SSRIs): Alaproclate • Citalopram • Dapoxetine • Desmethylcitalopram • Desmethylsertraline • Escitalopram • Femoxetine • Fluoxetine • Fluvoxamine • Indalpine • Ifoxetine • Litoxetine • Lu AA21004 • Lubazodone • Panuramine • Paroxetine • Pirandamine • RTI-353 • Seproxetine • Sertraline • Vilazodone • Zimelidine; Serotonin-norepinephrine reuptake inhibitors (SNRIs): Bicifadine • Desvenlafaxine • Duloxetine • Eclanamine • Levomilnacipran • Milnacipran • Sibutramine • Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors (SNDRIs): Brasofensine • Diclofensine • DOV-102,677 • DOV-21,947 • DOV-216,303 • NS-2359 • SEP-225,289 • SEP-227,162 • Tesofensine; Tricyclic antidepressants (TCAs): Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Pipofezine • Protriptyline • Trimipramine; Tetracyclic antidepressants (TeCAs): Amoxapine; Piperazines: Nefazodone • Trazodone; Antihistamines: Brompheniramine • Chlorpheniramine • Diphenhydramine • Mepyramine/Pyrilamine • Pheniramine • Tripelennamine; Opioids: Meperidine (Pethidine) • Methadone • Propoxyphene; Others: Cocaine • CP-39,332 • Cyclobenzaprine • Dextromethorphan • Dextrorphan • EXP-561 • Fezolamine • Mesembrine • Nefopam • PIM-35 • Pridefrine • Roxindole • SB-649,915 • Ziprasidone
VMAT

Ibogaine • Reserpine • Tetrabenazine
[show]

Releasing agents
Aminoindanes: 5-IAI • ETAI • MDAI • MDMAI • MMAI • TAI; Aminotetralins: 6-CAT • 8-OH-DPAT • MDAT • MDMAT; Oxazolines: 4-Methylaminorex • Aminorex • Clominorex • Fluminorex; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Methyl-MDA • 4-CAB • 4-FA • 4-FMA • 4-HA • 4-MTA • 5-APDB • 5-Methyl-MDA • 6-APDB • 6-Methyl-MDA • Amiflamine • BDB • BOH • Brephedrone • Butylone • Chlorphentermine • Cloforex • Diethylcathinone • Dimethylcathinone • DMA • DMMA • EBDB • EDMA • Ethylone • Etolorex • Fenfluramine (Dexfenfluramine) • Flephedrone • IAP • IMP • Lophophine • MBDB • MDA • MDEA • MDHMA • MDMA • MDMPEA • MDOH • MDPEA • Mephedrone • Methedrone • Methylone • MMA • MMDA • MMDMA • NAP • Norfenfluramine • pBA • pCA • pIA • PMA • PMEA • PMMA • TAP; Piperazines: 2C-B-BZP • BZP • MBZP • mCPP • MDBZP • MeOPP • Mepiprazole • pFPP • TFMPP; Tryptamines: 4-Methyl-αET • 4-Methyl-αMT • 5-CT • 5-MeO-αET • 5-MeO-αMT • 5-MT • αET • αMT • DMT • Tryptamine (itself); Others: Indeloxazine • Tramadol • Viqualine
[show]

Enzyme inhibitors
Anabolism

TPH

AGN-2979 • Fenclonine
AAAD

Benserazide • Carbidopa • Genistein • Methyldopa
Catabolism

MAO

Nonselective: Benmoxin • Caroxazone • Echinopsidine • Furazolidone • Hydralazine • Indantadol • Iproclozide • Iproniazid • Isocarboxazid • Isoniazid • Linezolid • Mebanazine • Metfendrazine • Nialamide • Octamoxin • Paraxazone • Phenelzine • Pheniprazine • Phenoxypropazine • Pivalylbenzhydrazine • Procarbazine • Safrazine • Tranylcypromine; MAO-A Selective: Amiflamine • Bazinaprine • Befloxatone • Befol • Brofaromine • Cimoxatone • Clorgiline • Esuprone • Harmala alkaloids (Harmine, Harmaline, Tetrahydroharmine, Harman, Norharman, etc) • Methylene Blue • Metralindole • Minaprine • Moclobemide • Pirlindole • Sercloremine • Tetrindole • Toloxatone • Tyrima
[show]

Others
Precursors

L-Tryptophan → 5-HTP
Cofactors

Ferrous iron (Fe2+) • Magnesium (Mg2+) • Tetrahydrobiopterin • Vitamin B3 (Niacin, Nicotinamide → NADPH) • Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal phosphate) • Vitamin B9 (Folic Acid → Tetrahydrofolic acid) • Vitamin C (Ascorbic acid) • Zinc (Zn2+)
Others

Activity enhancers: BPAP • PPAP; Reuptake enhancers: Tianeptine
Retrieved from "http://en.wikipedia.org/wiki/5-HT_receptor"
Categories: G protein coupled receptors | Ionotropic receptors
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