Target intelligence / Profile preview

Serotonin Receptor 5-HT1 Family (5-HT1 Family)

Target
5-HT1 Family
Molecular classification
G protein-coupled receptor
01

Overview

The serotonin 5-HT1 receptor family comprises a group of five G protein-coupled receptors (GPCRs): 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. These receptors are primarily coupled to Gi/Go proteins, inhibiting adenylyl cyclase and reducing cAMP formation. They are widely distributed throughout the central nervous system and play crucial roles in regulating mood, anxiety, aggression, and neurotransmitter release. Specific subtypes like 5-HT1A and 5-HT1B function as autoreceptors, controlling serotonin neuron firing and serotonin release, respectively. Drugs targeting these receptors, such as buspirone (5-HT1A partial agonist) and triptans (5-HT1B/1D/1F agonists), are used in the treatment of anxiety, depression, and migraine.

Other names
5-Hydroxytryptamine Receptor 1 FamilySerotonin 1 Receptor Family
02

Mechanism of action

Agonism or antagonism at 5-HT1 receptor subtypes, leading to modulation of adenylyl cyclase activity and downstream signaling pathways.

03

Biological functions

NeurotransmissionMood regulationAnxiety modulationRegulation of neurotransmitter releaseVasoconstriction/vasodilation
04

Disease associations

MigraineAnxiety disordersDepressionAggression
05

Safety considerations

Potential for off-target effects due to sequence similarity between subtypes.Cardiovascular effects associated with some agonists (e.g., ergots).
06

Interacting drugs

Buspirone

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