Pharmacological characterization of a receptor for calcitonin gene-related peptide on rat, L6 myocytes

D.R. Poyner, D.P. Andrew, D. Brown, C. Bose, M.R. Hanley

Research output: Contribution to journalArticlepeer-review


1 The L6 myocyte cell line expresses high affinity receptors for calcitonin gene-related peptide (CGRP) which are coupled to activation of adenylyl cyclase. The biochemical pharmacology of these receptors has been examined by radioligand binding or adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation. 2 In intact cells at 37 degrees C, human and rat alpha- and beta-CGRP all activated adenylyl cyclase with EC50s of about 1.5 nM. A number of CGRP analogues containing up to five amino acid substitutions showed similar potencies. In membrane binding studies at 22 degrees C in 1 mM Mg2+, the above all bound to a single site with IC50s of 0.1-0.4 nM. 3 The fragment CGRP(8-37) acted as a competitive antagonist of CGRP stimulation of adenylyl cyclase with a calculated Kd of 5 nM. The Kd determined in membrane binding assays was lower (0.5 nM). 4 The N-terminal extended human alpha-CGRP analogue Tyro-CGRP activated adenylyl cyclase and inhibited [125I]-iodohistidyl-CGRP binding less potently than human alpha-CGRP (EC50 for cyclase = 12 nM, IC50 for binding = 4 nM). 5 The pharmacological profile of the L6 CGRP receptor suggests that it most closely resembles sites on skeletal muscle, cardiac myocytes and hepatocytes. The L6 cell line should be a stable homogeneous model system in which to study CGRP mechanisms and pharmacology."
Original languageEnglish
Pages (from-to)441-447
Number of pages7
JournalBritish Journal of Pharmacology
Issue number2
Publication statusPublished - 8 May 1992


  • adenylyl cyclase
  • calcitonin
  • gene-related peptide
  • cell
  • line cells
  • cultured cyclic
  • AMP
  • inosine
  • triphosphate
  • iodine
  • radioisotopes
  • kinetics
  • muscles
  • radioligand
  • assay
  • rats receptors
  • calcitonin receptors
  • cell surface
  • amylin
  • calcitonin gene-related peptide receptors
  • ligand binding


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