Target intelligence / Profile preview

Pituitary adenylate cyclase-activating polypeptide receptor (PAC1R)

Target
PAC1R
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The pituitary adenylate cyclase-activating polypeptide receptor (PAC1R) is a class B GPCR and the primary high-affinity receptor for PACAP. It plays important roles in neuronal function and various physiological processes. Dysregulation has been implicated in disorders such as PTSD, migraine, and metabolic syndromes. Therapeutics targeting either the peptide or receptor are under investigation.

Other names
PAC1ADCYAP1R1
02

Mechanism of action

Ligand binding activates Gαs and Gαq pathways, leading to increased cAMP/PKA and IP3/DAG/Ca²⁺/PKC signaling respectively.

03

Biological functions

NeurotransmissionNeuroprotectionHormone secretionEnergy homeostasisMetabolic homeostasisSignal transduction
04

Disease associations

PTSDMigraineMetabolic syndromes
05

Safety considerations

Elevated cAMP in trigeminal neurons may sensitize neurons

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