In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.

@article{Hostetler2013InVQ,
  title={In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.},
  author={Eric D. Hostetler and Aniket D. Joshi and Sandra M. Sanabria-Boh{\'o}rquez and Hong Fan and Zhizhen Zeng and Mona Purcell and Liza Gantert and Kerry Riffel and Mangay Williams and Stacey O'Malley and Patricia Miller and Harold G. Selnick and Steven N. Gallicchio and Ian Mac Bell and Christopher A. Salvatore and Stefanie A. Kane and Chi-Chung Li and Richard J. Hargreaves and Tjibbe J de Groot and Guy Bormans and Anne van Hecken and Inge Derdelinckx and Jan N.J.M. de Hoon and Tom Reynders and Ruben Declercq and Inge de Lepeleire and Walter P. Kennedy and Rebecca Blanchard and Eugene E. Marcantonio and Cyrille Sur and Jacquelynn J. Cook and Koen Van Laere and Jeffrey L. Evelhoch},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2013},
  volume={347 2},
  pages={
          478-86
        }
}
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes vasodilation, neurogenic inflammation and trigeminovascular sensory activation. This process is implicated in the cause of migraine headaches, and CGRP-R antagonists in clinical development have proven effective in treating migraine-related pain in humans. CGRP-R is expressed on blood vessel smooth muscle and sensory trigeminal neurons and fibers in… CONTINUE READING

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