scholarly journals Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor*

Author(s):  
Eric Moore ◽  
Mark E. Fraley ◽  
Ian M. Bell ◽  
Christopher S. Burgey ◽  
Rebecca B. White ◽  
...  
Biochemistry ◽  
2010 ◽  
Vol 49 (9) ◽  
pp. 1862-1872 ◽  
Author(s):  
Christopher M. Koth ◽  
Norzehan Abdul-Manan ◽  
Christopher A. Lepre ◽  
Peter J. Connolly ◽  
Sanghee Yoo ◽  
...  

1992 ◽  
Vol 70 (12) ◽  
pp. 1571-1575 ◽  
Author(s):  
L. W. Kline ◽  
P. K. T. Pang

Calcitonin gene related peptide has been shown to relax vascular and intestinal smooth muscle. This study examines the effects of calcitonin gene related peptide on cholecystokinin-induced contraction of guinea pig gallbladder strips in vitro. Calcitonin gene related peptide was found to cause a dose-dependent relaxation of cholecystokinin-induced tension, which was blocked by the calcitonin gene related peptide receptor antagonist human calcitonin gene related peptide8–37. Previous studies demonstrated that calcitonin gene related peptide acted directly on guinea pig gallbladder smooth muscle to inhibit acetylcholine- or KCl-induced contraction. The present results further confirm that calcitonin gene related peptide acts directly on the smooth muscle. In addition, the use of L-NG-nitroarginine methyl ester, glibenclamide, and other agents strongly suggests that calcitonin gene related peptide also acts by way of the nonadrenergic noncholinergic nervous system, to induce the relaxation of cholecystokinin-induced contraction observed in the guinea pig gallbladder strips.Key words: calcitonin gene related peptide, gallbladder, cholecystokinin.


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