Target intelligence / Profile preview

5-hydroxytryptamine (serotonin) receptor 1D (5-HT1D receptor (also HTR1D))

Target
5-HT1D receptor (also HTR1D)
Molecular classification
G protein-coupled receptor, Receptor, Rhodopsin-like GPCR
01

Overview

The 5-hydroxytryptamine (serotonin) receptor 1D is a member of the G protein-coupled receptor family that binds serotonin as its endogenous ligand. It is encoded by the HTR1D gene located on chromosome 1p34.3–36.3. The receptor is primarily expressed at low levels within regions such as the basal ganglia, hippocampus, and cortex. Functionally, it mediates inhibitory neurotransmission by decreasing cellular cAMP levels upon activation. The main physiological roles include regulation of locomotion and anxiety as well as induction of vasoconstriction within cerebral blood vessels—a property exploited therapeutically for migraine relief using selective agonists like sumatriptan. The target has also been implicated genetically or functionally in neuropsychiatric conditions such as obsessive–compulsive disorder.

Other names
HTR1DSerotonin receptor 1D5-HT₁D receptor
02

Mechanism of action

Agonists activate the 5-hydroxytryptamine (serotonin) receptor 1D, leading to inhibition of adenylate cyclase via Gi/o proteins, resulting in decreased cAMP levels and subsequent physiological effects such as vasoconstriction and modulation of neurotransmitter/hormone release.

03

Biological functions

Signal transductionInhibition of adenylate cyclase activity (decreases cAMP)Modulation of neurotransmitter releaseRegulation of locomotion and anxietyInduction of vasoconstriction in the brain
04

Disease associations

Migraine (therapeutic target for antimigraine drugs)Obsessive–compulsive disorder (implicated by gene association)Other neuropsychiatric disorders, including anxiety and possibly depression, through modulation of serotonin signaling
05

Safety considerations

Potential safety concerns include cardiovascular side effects due to cerebral vasoconstriction when targeted by agonists like sumatriptan.
06

Interacting drugs

Sumatriptan (agonist used in migraine treatment)

1 more in the full profile.

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