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细胞内钙螯合剂喹啉-2(Quin-2)和细胞内钙拮抗剂8-(N,N-二甲基氨基)辛酯(TMB-8)对豚鼠盲肠带对组胺短期脱敏的影响。

Effects of Quin-2, an intracellular Ca chelator, and TMB-8, an intracellular Ca antagonist, on the short-term desensitization to histamine in guinea pig taenia caecum.

作者信息

Uchida M K, Mita M

出版信息

Gen Pharmacol. 1985;16(5):449-53. doi: 10.1016/0306-3623(85)90003-5.

Abstract

The effects of Quin-2-acetoxylmethylester, an intracellular Ca ion chelator, and 8-(N,N-diethylamino)-octyl-3,4,5-trimethoxybenzoate-HCl (TMB-8), an intracellular Ca antagonist, on short-term desensitization to histamine were tested in guinea pig taenia caecum. Desensitization was induced by incubating the muscle with 10(-4) M histamine for 30 min and the recovery from the desensitization needed ca. 90 min. Both Quin-2-acetoxylmethylester (50 microM for 120 min) and TMB-8 (5 microM for 20 min) suppressed the desensitization. Modes of action and structures of both agents are quite different but both may reduce the availability of intracellular Ca ion. It is possible that reduction of intracellular Ca ion suppressed the desensitization.

摘要

在豚鼠盲肠带中测试了细胞内钙离子螯合剂喹-2-乙酰氧基甲酯和细胞内钙拮抗剂8-(N,N-二乙氨基)-辛基-3,4,5-三甲氧基苯甲酸盐酸盐(TMB-8)对组胺短期脱敏的影响。通过将肌肉与10(-4) M组胺孵育30分钟诱导脱敏,脱敏恢复大约需要90分钟。喹-2-乙酰氧基甲酯(50 microM,作用120分钟)和TMB-8(5 microM,作用20分钟)均抑制了脱敏。两种药物的作用方式和结构差异很大,但两者都可能降低细胞内钙离子的可用性。细胞内钙离子的减少可能抑制了脱敏。

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