Calcitonin gene-related protein (CGRP) (8-37) is a CGRP receptor antagonist.1 It corresponds to amino acids 8-37 of rodent α-CGRP , a neuropeptide. CGRP (8-37) selectively binds to heterotrimeric complexes of calcitonin receptor-like receptor (CRLR) and receptor activity-modifying protein 1 (RAMP1) or RAMP3 (IC50s = 1 and 6.2 nM, respectively) over a complex of CRLR and RAMP2 (IC50 = 219 nM). It prevents CGRP-induced increases in heart rate and decreases in blood pressure in transgenic mice expressing rat CRLR in smooth muscle-containing tissues and sympathetic ganglia when administered at a dose of 2 µmol/kg.2 CGRP (8-37) also inhibits p-phenylquinone-induced writhing (ED50 = 6 µg/animal) and decreases body temperature in a dose-dependent manner in mice.3
1.Husmann, K., Born, W., Fischer, J.A., et al.Three receptor-activity-modifying proteins define calcitonin gene-related peptide or adrenomedullin selectivity of the mouse calcitonin-like receptor in COS-7 cellsBiochem. Pharmacol.66(11)2107-2115(2003) 2.Kunz, T.H., Scott, M., Ittner, L.M., et al.Calcitonin gene-related peptide-evoked sustained tachycardia in calcitonin receptor-like receptor transgenic mice is mediated by sympathetic activityAm. J. Physiol. Heart Circ. Physiol.293(4)H2155-H2160(2007) 3.Saxen, M.A., Smith, F.L., Dunlow, L.D., et al.The hypothermic and antinociceptive effects of intrathecal injection of CGRP (8-37) in miceLife Sci.55(21)1665-1674(1994)
















