calcitonin gene-related peptide 8-38

Calcitonin gene-related peptide 8-38 (CGRP 8-38) is a truncated peptide fragment consisting of amino acids 8 through 38 of the full-length CGRP molecule. It functions as a potent and competitive antagonist at the CGRP receptor, which is a heterodimeric G protein-coupled receptor complex comprising the calcitonin receptor-like receptor (CLR) and the receptor activity-modifying protein 1 (RAMP1). By binding to the receptor's orthosteric site without inducing signal transduction, CGRP 8-38 effectively blocks the vasodilatory and pro-nociceptive actions of endogenous CGRP. Although it has been a fundamental pharmacological tool for decades in characterizing CGRP-mediated pathways in migraine, pain, and cardiovascular research, its therapeutic development was hindered by rapid enzymatic degradation and poor oral bioavailability. These limitations eventually led to the clinical development of more stable small-molecule antagonists (gepants) and monoclonal antibodies targeting the CGRP pathway.

Other names

CGRP fragment 8-38Calcitonin gene-related peptide (8-38) human8-38-Calcitonin gene-related peptide