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

Abstract:

: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.

journal_name

J Pharmacol Sci

authors

Takahara A,Nozaki S,Ishiguro A,Okamura K,Cao X,Aimoto M,Nagasawa Y

doi

10.1016/j.jphs.2018.01.012

subject

Has Abstract

pub_date

2018-05-01 00:00:00

pages

98-100

issue

1

eissn

1347-8613

issn

1347-8648

pii

S1347-8613(18)30070-7

journal_volume

137

pub_type

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