5-hydroxytryptamine receptor 1B

Definition:

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.

References:

[1]. H Jin, et al. Characterization of the human 5-hydroxytryptamine1B receptor. J Biol Chem. 1992 Mar 25;267(9):5735-8. [Content Brief]

[2]. Chong Wang, et al. Structural basis for molecular recognition at serotonin receptors. Science. 2013 May 3;340(6132):610-4. [Content Brief]

[3]. Daniel Wacker, et al. Structural features for functional selectivity at serotonin receptors. Science. 2013 May 3;340(6132):615-9. [Content Brief]

[4]. D Mochizuki, et al. Cloning and expression of the human 5-HT1B-type receptor gene. Biochem Biophys Res Commun. 1992 Jun 15;185(2):517-23. [Content Brief]

[5]. S A Veldman, et al. Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype. Mol Pharmacol. 1992 Sep;42(3):439-44. [Content Brief]

[6]. Z Xie, et al. Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. 1999 Jul 30;456(1):63-7. [Content Brief]

[7]. L Demchyshyn, et al. A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5522-6. [Content Brief]

[8]. G Y Ng, et al. Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition. Biochemistry. 1993 Nov 2;32(43):11727-33. [Content Brief]

[9]. R L Weinshank, et al. Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4. [Content Brief]

[10]. F O Levy, et al. Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype. J Biol Chem. 1992 Apr 15;267(11):7553-62. [Content Brief]

[11]. Lars Edvinsson, et al. Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: relationship to clinical effect. Clin Sci (Lond). 2005 Sep;109(3):335-42. [Content Brief]

[12]. M W Hamblin, et al. Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity. Biochem Biophys Res Commun. 1992 Apr 30;184(2):752-9. [Content Brief]

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