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α-Calcitonin gene-related peptide (α-CGRP) is a neuropeptide with roles in vasodilation, cardiovascular regulation, and inflammation.1 It belongs to the calcitonin family of peptides, which also includes amylin (Item No. 24274), calcitonin (Item Nos. 24409 | 24410), and adrenomedullin.2 α-CGRP binds selectively to heterotrimeric complexes of calcitonin receptor-like receptor (CRLR) and receptor activity-modifying proteins RAMP 1 or 3 (RAMP1 and 3; IC50s = 7 and 23 nM, respectively) over a complex of CRLR and RAMP2 (IC50 = >1,000 nM).3 It binds to rat brain and spleen membrane preparations (IC50s = 3.9 and 3.5 nM, respectively) and relaxes human cerebral and middle meningeal arterial segments precontracted with prostaglandin F2α (PGF2α; Item No. 16010; IC50s = 0.23 and 2.24 nM, respectively).4,5 In vivo, α-CGRP (0.01-3,000 ng/kg) decreases mean arterial blood pressure (MABP) and increases pial arteriole (PA) and middle meningeal artery (MMA) diameters in rats with closed cranial windows.6 It induces a 50% increase in diameter of arterioles precontracted with human endothelin-1 (ET-1; Item No. 24127) in vivo in hamster cheek pouch at a concentration of 39.8 pM.7
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1. Calcitonin gene-
2. Amylin, calcitonin gene-
3. Three receptor-
4. Structure-
5. In-
6. Inhibitory effect of BIBN4096BS on cephalic vasodilatation induced by CGRP or transcranial electrical stimulation in the rat. Br. J. Pharmacol. 143(6), 697-704 (2004).
7. Interaction of amylin with calcitonin gene-