Pharmacology of the human CGRP 1 receptor in Cos 7 cells

• Published in: Peptides (New York, N.Y. : 1980) Vol. 27; no. 6; pp. 1367 - 1375
• Main Authors: Bailey, Richard J., Hay, Debbie L.
• Format: Journal Article
• Language: English
• Published: Elsevier Inc 2006
• Subjects: BIBN4096BS; Calcitonin receptor-like receptor; CGRP; CGRP 1 receptor; Receptor activity modifying protein; N-[2-[[5amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl); CT; RAMP; CGRP 1 receptor; CL; Receptor activity modifying protein; AM; BIBN4096BS; AMY; CGRP; Calcitonin receptor-like receptor
• ISSN: 0196-9781; 1873-5169
• DOI: 10.1016/j.peptides.2005.11.014

Only limited pharmacological characterization of the CGRP 1 receptor, a heterodimer of the calcitonin (CT) receptor-like receptor (CL) and receptor activity-modifying protein 1 has been performed in cells that do not endogenously express RAMP2. We characterized the receptor in RAMP-deficient Cos 7 cells by measuring cAMP responses following agonist treatment in the absence or presence of antagonists. Potent cAMP responses to human α-and β-CGRP (Cys(Et) 2,7)hαCGRP and human adrenomedullin (AM) were observed. Adrenomedullin 15–52 was also an effective agonist of the CGRP 1 receptor but human and salmon calcitonin and rat amylin were only weak agonists. As expected, BIBN4096BS and CGRP 8–37 were effective antagonists of the CGRP 1 receptor. (Cys(Acm) 2,7)hαCGRP also antagonized CGRP responses. Antagonists of related receptors were only weakly able to inhibit CGRP responses.