PACAP (Pituitary Adenylate Cyclase-Activating Peptide)

Neuroprotection / Hormonal

Also known as: Pituitary Adenylate Cyclase-Activating Peptide, PACAP-38, PACAP-27, ADCYAP1

VIP/Secretin/Glucagon SuperfamilyResearch phase: Endogenous peptide (migraine antagonists in clinical trials)Regulatory: Endogenous peptide. PAC1R antagonists are in clinical trials for migraine. PACAP itself is not an approved drug.

Mechanism

PACAP is a neuroprotective peptide found throughout the brain and nervous system. It stimulates cAMP production in the pituitary (hence its name) and has broad protective effects on neurons, including defense against oxidative stress and apoptosis. It exists in two forms (27 and 38 amino acids) and is involved in migraine pathology, stress responses, and circadian rhythm regulation.

Technical detail

PACAP exists as PACAP-38 (predominant) and PACAP-27, products of the ADCYAP1 gene. It binds PAC1R (PACAP-specific, Gs/Gq-coupled) and VPAC1R/VPAC2R (shared with VIP). PAC1R activation drives adenylyl cyclase-cAMP-PKA and PLC-PKC pathways, upregulating CREB-mediated neuroprotective gene expression including BDNF and Bcl-2. PACAP is a potent vasodilator implicated in migraine pathogenesis (similar to CGRP), and PAC1R antagonists are under investigation for migraine prevention. Also functions as a hypothalamic hypophysiotropic factor stimulating GH, prolactin, and ACTH release.

Evidence