The sensory neuropeptide calcitonin gene-related peptide 1 (CALCA, aka CGRP) plays an important role in primary headaches. The CALC1 gene produces a prepropeptide from which calcitonin (CALCA(83-119)) is a cleavage product (Nelkin BD et al, 1984). CALCA(83-119) is a polypeptide hormone that is produced in the thyroid gland. It acts to reduce blood calcium, opposing the effects of parathyroid hormone. It also induces vasodilation of coronary, cerebral and systemic vasculature. The CALCA(83-119) receptor (CALCR) (Gorn AH et al, 1992) binds CALCA(83-119) and mediates its actions. The ligand:receptor complex couples to the G protein alpha s subunit, which stimulates adenylyl cyclase and increases intracellular cAMP levels (Gorn AH et al, 1992). CALCA(83-119) antagonists are effective in migraine treatment.
Leong, SS, de Bustros, A, Rosenfeld, KI, Baylin, SB, Roos, BA, Nelkin, BD
Yamin, M, Lodish, HF, Flannery, MR, Auron, PE, Tapp, DR, Gorn, AH, Manning, CA, Goldring, SR, Krane, SM, Lin, HY
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