title: Pharmacology of the human CGRP1 receptor in Cos 7 cells.
abstract: Only limited pharmacological characterization of the CGRP1 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 alpha-and beta-CGRP (Cys(Et)2,7)halphaCGRP and human adrenomedullin (AM) were observed. Adrenomedullin15-52 was also an effective agonist of the CGRP1 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 CGRP1 receptor. (Cys(Acm)2,7)halphaCGRP also antagonized CGRP responses. Antagonists of related receptors were only weakly able to inhibit CGRP responses.
authors.affiliation: Proteomics & Biomedicine Research Group, School of Biological Sciences, University of Auckland, 3 Symonds Street, Private Bag 92 019, New Zealand.
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Bailey
authors.forename: Debbie L
authors.initials: DL
authors.lastname: Hay
mesh_terms: D053607:Adrenomedullin; D000818:Animals; D019556:COS Cells; D002116:Calcitonin / Q000737:chemistry* / Q000494:pharmacology*; D015740:Calcitonin Gene-Related Peptide; D002118:Calcium / Q000378:metabolism; D002522:Chlorocebus aethiops; D006801:Humans; D007700:Kinetics; D010455:Peptides / Q000737:chemistry; D011498:Protein Precursors / Q000737:chemistry* / Q000494:pharmacology*; D012313:RNA / Q000378:metabolism; D051381:Rats; D011994:Recombinant Proteins / Q000737:chemistry / Q000494:pharmacology; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012474:Salmon
chemical_list: C000606589:CALCA protein, human; C000606591:Calca protein, rat; D010455:Peptides; D011498:Protein Precursors; D011994:Recombinant Proteins; D053607:Adrenomedullin; D012313:RNA; D002116:Calcitonin; D015740:Calcitonin Gene-Related Peptide; D002118:Calcium