A neuropeptide with diverse biological activities
α-Calcitonin gene-related peptide (α-CGRP) is a neuropeptide with diverse biological activities. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin , and adrenomedullin. α-CGRP binds selectively to a heteromeric complex of calcitonin receptor-like receptor (CRLR) and receptor activity-modifying protein 1 (RAMP1; IC50 = 0.1 nM) over a complex of CLCR and RAMP2 (IC50 = 1,300 nM). It also binds selectively to complexes of human calcitonin receptor 2 (CTR2) and RAMP1 (IC50 = 43.7 nM) compared to CTR2 and RAMP2 complexes (IC50 = 141.3 nM) in amylin radioligand displacement assays. α-CGRP induces cAMP-activated currents in Xenopus oocytes with endogenous Cgrp receptors that overexpress RAMP1 (EC50 = 9 nM). It also induces cAMP accumulation in COS-7 cells transfected with both CTR2 and RAMP1 (EC50 = 8.32 nM).
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