Abstract
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.
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