Target intelligence / Profile preview

Serotonin 5-HT1 Receptor (5-HT1 receptor)

Target
5-HT1 receptor
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The serotonin 5-HT1 receptors are a subfamily of serotonin (5-hydroxytryptamine, 5-HT) receptors that bind the endogenous neurotransmitter serotonin. These receptors are G protein-coupled receptors (GPCRs) coupled to Gi/Go proteins and play a significant role in regulating synaptic levels of serotonin throughout the brain. They inhibit adenylyl cyclase activity, leading to decreased cyclic AMP (cAMP) levels within cells. The 5-HT1 receptor family consists of five main subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-ht1E, and 5-HT1F. Agonists targeting these receptors are used therapeutically for conditions such as depression, migraine headaches, anxiety disorders, and schizophrenia, while genetic variations have been linked with psychiatric conditions like addiction or obsessive-compulsive disorder for certain subtypes.

Other names
5-Hydroxytryptamine receptor 15-HT1 familySerotonin receptor 1
02

Mechanism of action

Gi/Go protein-coupled receptor activation, inhibition of adenylyl cyclase, decreased cAMP levels, hyperpolarization of neurons, modulation of neurotransmitter release.

03

Biological functions

Signal transductionNeurotransmissionMood regulationAnxiety regulationAggression regulationMemory modulationStress response modulationHormone secretion regulation
04

Disease associations

DepressionAnxiety disordersMigraineAddictionObsessive-compulsive disorderSchizophrenia
05

Safety considerations

Variable effects depending on subtype selectivityPotential for drug interactionsSide effects associated with serotonergic modulation
06

Interacting drugs

Buspirone

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