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KRN2391和尼可地尔对非洲爪蟾卵母细胞中格列本脲敏感的钾通道的激活作用。

Activation by KRN2391 and nicorandil of glibenclamide-sensitive K+ channels in Xenopus oocytes.

作者信息

Sakuta H, Okamoto K

机构信息

Department of Pharmacology, National Defense Medical College, Saitama, Japan.

出版信息

Eur J Pharmacol. 1993 Feb 15;244(3):277-83. doi: 10.1016/0922-4106(93)90153-z.

Abstract

KRN2391 (N-cyano-N'-(2-nitroxyethyl)-3-pyridine-carboximidamide methanesulfonate) and nicorandil, a new class of K+ channel openers, each with an NO2 moiety, induced outward K+ currents in follicle-enclosed Xenopus oocytes. These K+ currents were suppressed concentration-dependently and reversibly by glibenclamide, phentolamine and trifluoperazine, all known to inhibit ATP-sensitive K+ channels. The nicorandil-induced K+ current was virtually abolished by defolliculation of oocytes, while the KRN2391 response was little affected by defolliculation. These results suggest that Xenopus oocyte has at least two types of glibenclamide-sensitive K+ channels, one is selectively sensitive to KRN2391 and is probably localized in the oocyte, and the other is sensitive to nicorandil and distributed in the follicle cells surrounding an oocyte.

摘要

KRN2391(N-氰基-N'-(2-硝氧乙基)-3-吡啶甲脒甲烷磺酸盐)和尼可地尔是一类新型的钾通道开放剂,均含有一个NO2基团,它们均可在卵泡包裹的非洲爪蟾卵母细胞中诱导外向钾电流。这些钾电流受到格列本脲、酚妥拉明和三氟拉嗪浓度依赖性且可逆的抑制,这三种物质均已知可抑制ATP敏感性钾通道。卵母细胞去卵泡处理后,尼可地尔诱导的钾电流几乎完全消失,而KRN2391的反应几乎不受去卵泡处理的影响。这些结果表明,非洲爪蟾卵母细胞至少有两种对格列本脲敏感的钾通道,一种对KRN2391具有选择性敏感性,可能定位于卵母细胞中,另一种对尼可地尔敏感,分布在卵母细胞周围的卵泡细胞中。

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