5-Hydroxytryptamine receptor 1B, 1D, 1E, 2B, 5, 6, and 7 (5-HT1B/1D/1E/2B/5/6/7)

The serotonin receptors 5-HT1B, 5-HT1D, 5-HT1E, 2B, 5, 6, and 7 represent a diverse group of G protein-coupled receptors (GPCRs) that mediate the physiological effects of serotonin (5-hydroxytryptamine) across the central and peripheral nervous systems [Source: IUPHAR/BPS Guide to Pharmacology]. The 5-HT1 subtypes (1B, 1D, 1E) are primarily Gi/o-coupled and are major targets for migraine therapy, where their activation leads to cranial vasoconstriction and inhibition of trigeminal pain signaling [Source: UniProt P28222, P28221]. The 5-HT2B receptor is Gq-coupled and plays a role in cardiac development and gut motility; however, its unintended activation is a significant safety concern due to its association with drug-induced cardiac valvulopathy and pulmonary hypertension [Source: PubMed PMID: 10846167]. The 5-HT5 (specifically 5-HT5A in humans), 5-HT6, and 5-HT7 receptors are involved in complex neurological processes including cognition, mood regulation, and circadian rhythms, making them subjects of intense research for treating schizophrenia, depression, and cognitive impairment [Source: UniProt P50406, P34969]. Drugs targeting these receptors often exhibit broad polypharmacology, such as ergot alkaloids (e.g., dihydroergotamine) and atypical antipsychotics (e.g., clozapine), which interact with multiple subtypes to achieve their therapeutic effects [Source: PubChem].

Other names

5-HT1B5-HT1D5-HT1E5-HT2B5-HT5A5-HT65-HT7Serotonin receptors5-Hydroxytryptamine receptors

Agonism of 5-HT1B and 5-HT1D receptors for acute migraine treatment; Antagonism of 5-HT6 and 5-HT7 receptors for potential cognitive and antipsychotic effects; Agonism of 5-HT2B receptors is generally avoided due to cardiovascular toxicity.