5-HT receptor

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Overview

In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT.^[1] 5-HT receptors are located on the cell membrane of nerve cells and other cell types including smooth muscle in animals, and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs. 5-HT receptors affect the release and activity of other neurotransmitters such as glutamate, dopamine and GABA. 5-HT_2A receptors increase the activity of glutamate in many areas of the brain, while some other serotonin receptors have the effect of suppressing glutamate. Increased stimulation of 5-HT_2A receptors seem to oppose the therapeutic actions of increased stimulation of other serotonin receptors in anti-depressant and anxiolytic treatments.^[1]

Classification

With the exception of the 5-HT₃ receptor, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or heptahelical) receptors that activate an intracellular second messenger cascade.

Families

Family	Type	Mechanism
5-HT1	Gi/Go coupled	decreasing cellular levels of cAMP
5-HT2	Gq/G11 coupled	increasing cellular levels of inositol trisphosphate (IP3) and diacylglycerol (DAG)
5-HT3	ligand-gated Na+ and K+ cation channel	depolarizing plasma membrane
5-HT4	Gs coupled	increasing cellular levels of cAMP
5-HT5A	G protein coupled; the primary coupling appears to be through Gi/o	inhibiting adenylate cyclase activity.[1]
5-HT6	Gs coupled	increasing cellular levels of cAMP
5-HT7	Gs coupled	increasing cellular levels of cAMP

Specific proteins/genes

Within these general classes of 5-HT receptors, a number of specific types have been characterized:

Summary of characterized 5-HT receptors, with selected high affinity agonist and antagonist ligands

Receptor	Gene	Actions	Agonists	Antagonists
5-HT1A	HTR1A	CNS: neuronal inhibition, behavioural effects (sleep, feeding, thermoregulation, aggression, anxiety)	buspirone psilocin LSD 8-OH-DPAT	spiperone methiothepin ergotamine yohimbine
5-HT1B	HTR1B	CNS: presynaptic inhibition, behavioural effects vascular: pulmonary vasoconstriction	ergotamine sumatriptan	methiothepin yohimbine metergoline Risperidone
5-HT1D	HTR1D	CNS: locomotion, anxiety; vascular: cerebral vasoconstriction	5-(Nonyloxy)tryptamine,[1] sumatriptan	methiothepin yohimbine metergoline ergotamine
5-HT1E	HTR1E
5-HT1F	HTR1F
5-HT2A	HTR2A	CNS: neuronal excitation, behavioural effects, learning, anxiety smooth muscle: contraction, vasoconstriction / vasodilatation platelets: aggregation	α-methyl-5-HT LSD psilocin DOI	Nefazodone trazodone mirtazapine ketanserin cyproheptadine pizotifen atypical antipsychotics
5-HT2B	HTR2B	stomach: contraction	α-methyl-5-HT LSD DOI Fenfluramine	yohimbine
5-HT2C	HTR2C	CNS: anxiety, choroid plexus: cerebrospinal fluid (CSF) secretion	α-methyl-5-HT agomelatine LSD psilocin DOI	mesulergine agomelatine fluoxetine methysergide[1]
5-HT3	HTR3A, HTR3B	CNS, PNS: neuronal excitation, anxiety, emesis	2-methyl-5-HT	metoclopramide (high doses) renzapride ondansetron alosetron mirtazapine memantine
5-HT4	HTR4	GIT: gastrointestinal motility CNS: neuronal excitation, learning, memory	5-methoxytryptamine metoclopramide renzapride tegaserod RS 67333	GR113808 Piboserod
5-HT5A	HTR5A	CNS (cortex, hippocampus, cerebellum): unknown	5-carboxytryptamine LSD[1]	unknown
5-HT6	HTR6	CNS: unknown	LSD	SB271046[1]
5-HT7	HTR7	CNS, GIT, blood vessels: unknown	5-carboxytryptamine LSD	methiothepin risperidone

Note that there is no 5-HT_1C 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-HT_2C receptor.

Therapeutic modulation

Various drugs are used to modulate the 5-HT system including some antidepressants, anxiolytics, antiemetics, antipsychotics and anti-migraine agents.

External links

• MeSH Serotonin+Receptors
• 5-Hydroxytryptamine Receptors. IUPHAR Receptor Database. International Union of Basic and Clinical Pharmacology. Retrieved on 2008-04-11.
• Glennon RA, Dukat M, Westkaemper RB (2000-01-01). Serotonin Receptor Subtypes and Ligands. American College of Neurophyscopharmacology. Retrieved on 2008-04-11.
• Rubenstein, LA, Lanzara RG (2005-02-16). Activation of G protein-coupled receptors entails cysteine modulation of agonist binding. Cogprints. Retrieved on 2008-04-11.
• Frazer A, Hensler JG (1999). "Chapter 13: Serotonin Receptors", in Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD, editors: Basic Neurochemistry: Molecular, Cellular, and Medical Aspects. Philadelphia: Lippincott-Raven, pages 263-292. ISBN 0-397-51820-X. 
• Wesołowska A (2002). "In the search for selective ligands of 5-HT₅, 5-HT₆ and 5-HT₇ serotonin receptors". Polish Journal of Pharmacology 54 (4): 327-41. PMID 12523486.

v • d • e Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like	Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - 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, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - Neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like	Brain-specific angiogenesis inhibitor (1, 2, 3) - Cadherin (1, 2, 3) - Calcitonin - CD97 - Corticotropin-releasing hormone (1, 2) - EMR (1, 2, 3) - Glucagon (GR, GIPR, GLP1R, GLP2R) - Growth hormone releasing hormone - PACAPR1- GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157) - Latrophilin (1, 2, 3, ELTD1) - Parathyroid hormone (1, 2) - Secretin - Vasoactive intestinal peptide (1, 2)
Class C: Metabotropic glutamate / pheromone	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) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened	Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened

v • d • e Ion channel, receptor: ligand-gated ion channels
Cys-loop receptors	5-HT receptor (5-HT3 serotonin receptor (A)) - GABA receptor (GABA A (α1, α2, α3, α5, α6, β1, β2, β3, γ2, ε), GABA C (ρ1)) - Glycine receptor (α1) - Nicotinic acetylcholine receptor (α1, α2, α3, α4, α5, α7, β2, β3, β4, δ, ε, (α4)2(β2)3, (α7)5, Ganglion type, Muscle type)
Ionotropic glutamate receptors	AMPA (1, 2, 3, 4) - Kainate (1, 2) - NMDA (1, 2A, 2B, 2C, 2D)
ATP-gated channels	Purinergic receptors (P2X (1, 4, 5, 7))

References

de:5-HT-Rezeptor

ja:セロトニン受容体

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