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5-HT1 receptor

In the field of neurochemistry, 5-HT₁ receptors are a subfamily of 5-HT receptors which bind the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine (5-HT).^[1]

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Mode of action

5-HT₁ receptors are G protein coupled receptors that Gi/Go-coupled. This causes a cellular decrease of cAMP.

Subtypes

Although working basically through the same mechanism, there are several 5-HT₁ receptor subtypes (denoted A-F), each encoded by a separate gene. Furthermore each subtype has a somewhat different tissue distribution and binding preference for synthetic 5-HT₁ agonist and antagonist ligands.

5-HT_1A

Main article: 5-HT1A receptor

Gene	Agonists	Antagonists
HTR1A	buspirone (anxiolytic) psilocin (psychedelic ) LSD (psychedelic drug) 5-carboxamidotryptamine (5-CT) 8-OH-DPAT	spiperone methiothepin (antipsychotic) ergotamine (vasoconstrictor in migraine) yohimbine (aphrodisiac)

5-HT_1A acts on the CNS, where it induces neuronal inhibition and controls behaviour, such as sleep, feeding, thermoregulation, aggression, anxiety.

5-HT_1B

Main article: 5-HT1B receptor

Gene	Agonists	Antagonists
HTR1B	ergotamine (vasoconstrictor in migraine) sumatriptan (vasoconstrictor in migraine) 5-carboxamidotryptamine (5-CT)	methiothepin (antipsychotic) yohimbine (aphrodisiac) metergoline

5-HT_1B acts on the CNS, where it induces presynaptic inhibition and behavioural effects. It also has vascular effects, such as pulmonary vasoconstriction.

5-HT_1D

Main article: 5-HT1D receptor

Gene	Agonists	Antagonists
HTR1D	5-(Nonyloxy)tryptamine,^[2] sumatriptan (vasoconstrictor in migraine) 5-carboxamidotryptamine (5-CT)	methiothepin (antipsychotic) yohimbine (aphrodisiac) metergoline ergotamine (vasoconstrictor in migraine)

5-HT_1D acts on the CNS, and affects locomotion and anxiety. It also induces vascular vasoconstriction in the brain. Ergotamine works primarily through the 5-HT1B receptor, since the effect through the 5-HT1D receptor is contrary to the mode of action of ergotamine, i.e. vasoconstriction.

5-HT_1E

Main article: 5-HT1E receptor

Gene	Agonists	Antagonists
HTR1E

5-HT_1F

Main article: 5-HT1F receptor

Gene	Agonists	Antagonists
HTR1F

References

^ 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.
^ Glennon RA, Hong SS, Dukat M, Teitler M, Davis K (1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT_1D beta serotonin receptor agonist". J. Med. Chem. 37 (18): 2828–30. doi:10.1021/jm00044a001. PMID 8071931.

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

Categories: G protein coupled receptors | Signal transduction | Cell signaling

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "5-HT1_receptor". A list of authors is available in Wikipedia.