Target intelligence / Profile preview

Serotonin 5-hydroxytryptamine receptor 1B (5-HT1B)

Target
5-HT1B
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The serotonin 5-hydroxytryptamine receptor 1B (5-HT1B) is a G protein-coupled receptor (GPCR) for serotonin. It is primarily expressed in the central nervous system and on blood vessel endothelium. In the CNS, it acts as both an autoreceptor on serotonergic neurons to inhibit serotonin release and as a heteroreceptor on non-serotonergic neurons to inhibit the release of other neurotransmitters. In vasculature, it mediates vasoconstriction. It plays a role in mood, memory, aggression, and stress sensitivity, and is implicated in addiction and obsessive-compulsive disorder. Dysfunctions are associated with neuropsychiatric conditions. Triptans, used for migraine treatment, target this receptor subtype.

Other names
5HT1B receptorSerotonin receptor 1BHTR1B5-hydroxytryptamine receptor 1B
02

Mechanism of action

Inhibition of adenylate cyclase activity via Gi/o proteins, leading to reduced cAMP formation and decreased neurotransmitter release at presynaptic sites.

03

Biological functions

Signal transductionRegulation of neurotransmitter releaseVasoconstrictionModulation of neuronal activityAutoreceptor functionHeteroreceptor function
04

Disease associations

MigraineAddiction disordersObsessive-compulsive disorderMood disordersDepression
05

Safety considerations

Potential cardiovascular side effects (vasoconstriction)Overactivation leading to adverse effects
06

Interacting drugs

Sumatriptan

2 more in the full profile.

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