Serotonin receptor 1B (5-HT1B) and Serotonin receptor 1D (5-HT1D) (5-HT1B, 5-HT1D)

Serotonin receptor 1B (5-HT1B) and serotonin receptor 1D (5-HT1D) are closely related subtypes of serotonin (5-hydroxytryptamine, 5-HT) G protein-coupled receptors. Both are widely expressed in the central nervous system, particularly in the frontal cortex and basal ganglia for 5-HT1B, and in the basal ganglia, hippocampus, and raphe for 5-HT1D. These receptors function as presynaptic inhibitory auto-receptors and heteroreceptors, modulating the release of neurotransmitters such as serotonin, dopamine, glutamate, acetylcholine, noradrenaline, and GABA. In addition to their central role, both are present in vascular tissues, mediating vasoconstriction—especially in the cerebral arteries—making them major therapeutic targets for the acute treatment of migraine. Drugs targeting these receptors (triptans) act as selective agonists, alleviating migraines via vascular and neurogenic mechanisms. However, the associated vasoconstrictive effects impose safety limitations, particularly for patients with existing cardiovascular conditions. Genetic variation in these receptors has also been linked to addiction and psychiatric disorders.

Other names

5-hydroxytryptamine receptor 1B5-HT1B receptorHTR1B5-hydroxytryptamine receptor 1D5-HT1D receptorHTR1D

Agonism of 5-HT1B/1D receptors leading to inhibition of neuropeptide and neurotransmitter release; Vasoconstriction of intracranial blood vessels; Inhibition of plasma protein extravasation