Pharmacological Differences between Human and Rat CGRP Receptors Are Determined by RAMP1 | Zendy

Stefanie A. Kane | Zendy; John Mallee | Zendy; Christopher Salvatore | Zendy; Beatrice LeBourdellès | Zendy; Ken S. Koblan | Zendy

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Pharmacological Differences between Human and Rat CGRP Receptors Are Determined by RAMP1

Author(s) -

Stefanie A. Kane,

John Mallee,

Christopher Salvatore,

Beatrice LeBourdellès,

Ken S. Koblan

Publication year - 2001

Publication title -

the scientific world journal

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.453

H-Index - 93

eISSN - 2356-6140

pISSN - 1537-744X

DOI - 10.1100/tsw.2001.422

Subject(s) - calcitonin gene related peptide , receptor , computer science , pharmacology , medicine , neuropeptide

Several small molecule CGRP receptor antagonists have now been reported and their effects profiled in a variety of in vivo assays. Of particular interest is the observation that some antagonists display marked species selectivity. Doods and coworkers[1] reported that BIBN4096BS exhibited 200-fold higher affinity for human and marmoset CGRP receptors, than for receptors from rat, dog, guinea pig and rabbit. In addition, Edvinsson and colleagues[2] reported that compound 1 was a significantly more potent antagonist on human cerebral arteries than on guinea pig arteries. In the present study, we sought to identify the molecular basis for this profound species selectivity.

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