Involvement of G protein-coupled receptor kinase-6 in desensitization of CGRP receptors.

@article{Aiyar2000InvolvementOG,
  title={Involvement of G protein-coupled receptor kinase-6 in desensitization of CGRP receptors.},
  author={N. Subramanya Aiyar and Jyoti Disa and Ka’ohimanu Dang and Alexey N. Pronin and Jeffrey L. Benovic and P. Azhahia Nambi},
  journal={European journal of pharmacology},
  year={2000},
  volume={403 1-2},
  pages={1-7}
}
This investigation was undertaken to study the mechanisms of calcitonin gene-related peptide (CGRP)-mediated desensitization using recombinant porcine CGRP receptors stably expressed in human embryonic kidney (HEK-293) cells. Pretreatment of these cells with human alphaCGRP resulted in an approximately 60% decrease in CGRP-stimulated adenylyl cyclase activity and an approximately 10-fold rightward shift in the dose-response curve of CGRP. This effect was rapid (t(1/2) approximately 5 min) and… CONTINUE READING
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