Pharmacology of the human CGRP1 receptor in Cos 7 cells

Peptides. 2006 Jun;27(6):1367-75. doi: 10.1016/j.peptides.2005.11.014. Epub 2005 Dec 20.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenomedullin
  • Animals
  • COS Cells
  • Calcitonin / chemistry*
  • Calcitonin / pharmacology*
  • Calcitonin Gene-Related Peptide
  • Calcium / metabolism
  • Chlorocebus aethiops
  • Humans
  • Kinetics
  • Peptides / chemistry
  • Protein Precursors / chemistry*
  • Protein Precursors / pharmacology*
  • RNA / metabolism
  • Rats
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / pharmacology
  • Reverse Transcriptase Polymerase Chain Reaction
  • Salmon


  • CALCA protein, human
  • Calca protein, rat
  • Peptides
  • Protein Precursors
  • Recombinant Proteins
  • Adrenomedullin
  • RNA
  • Calcitonin
  • Calcitonin Gene-Related Peptide
  • Calcium