Selectivity of Ca2+ channel blockers for dilator actions on the isolated lower esophageal sphincter and aorta from rats

• Main Authors: Akira Takahara (Author), Shuhei Nozaki (Author), Akane Ishiguro (Author), Kaori Okamura (Author), Xin Cao (Author), Megumi Aimoto (Author), Yoshinobu Nagasawa (Author)
• Format: Book
• Published: Elsevier, 2018-05-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

We compared dilator actions of representative four Ca2+ channel blockers on the isolated lower esophagus sphincter (LES) and thoracic aorta from rats. Verapamil, diltiazem, nifedipine and cilnidipine suppressed KCl-induced contractions of LES and thoracic aorta in a concentration-dependent manner. The order of selectivity for LES, which was calculated as ratio of IC50 value for thoracic aorta divided by that for LES, was diltiazem > verapamil > nifedipine > cilnidipine. These results suggest that diltiazem more preferentially dilates the LES whereas cilnidipine is expected to have lower potential risk of gastroesophageal dysfunction during the antihypertensive therapy. Keywords: Ca2+ channel blockers, Lower esophagus sphincter, Thoracic aorta

Item Description

1347-8613
10.1016/j.jphs.2018.01.012