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

被引：2

作者：

Takahara, Akira ^{[1
]}

Nozaki, Shuhei ^{[1
]}

Ishiguro, Akane ^{[1
]}

Okamura, Kaori ^{[1
]}

Cao, Xin ^{[1
]}

Aimoto, Megumi ^{[1
]}

Nagasawa, Yoshinobu ^{[1
]}

机构：

[1] Toho Univ, Fac Pharmaceut Sci, Dept Pharmacol & Therapeut, 2-2-1 Miyama, Funabashi, Chiba 2748510, Japan

来源：

JOURNAL OF PHARMACOLOGICAL SCIENCES | 2018年 / 137卷 / 01期

关键词：

Ca2+ channel blockers; Lower esophagus sphincter; Thoracic aorta; NIFEDIPINE; VERAPAMIL; DISEASE;

D O I：

10.1016/j.jphs.2018.01.012

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 KCI-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. (C) 2018 The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society.

引用

页码：98 / 100

页数：3

共 9 条

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