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猪离体直肠动脉对咪唑啉衍生物的非肾上腺素能受体反应的证据。

Evidence for nonadrenoceptor responses to imidazoline derivatives in the porcine isolated rectal artery.

作者信息

Wang Minyan, Dunn W R, Chan S L, Garfield B, Wilson V G

机构信息

School of Biomedical Sciences, University of Nottingham, Nottingham, UK.

出版信息

Ann N Y Acad Sci. 2003 Dec;1009:386-91. doi: 10.1196/annals.1304.052.

Abstract

High concentrations of phentolamine, efaroxan, and idazoxan were found to produce nonadrenoceptor contractions of the porcine isolated rectal artery previously exposed to U46619 and forskolin. These responses were insensitive to the putative imidazoline I(3) receptor antagonist KU-14R, unlike those previously reported in this preparation for oxymetazoline. The pharmacologic nature of this response and the obligate requirement for preconstriction suggests that these imidazoline derivatives modulate ion channel function through a novel nonadrenergic site.

摘要

研究发现,高浓度的酚妥拉明、依发洛新和咪唑克生可使先前暴露于U46619和福斯高林的猪离体直肠动脉产生非肾上腺素能受体收缩。与先前在该制剂中报道的去氧肾上腺素的反应不同,这些反应对假定的咪唑啉I(3)受体拮抗剂KU-14R不敏感。这种反应的药理学性质以及预收缩的必然要求表明,这些咪唑啉衍生物通过一个新的非肾上腺素能位点调节离子通道功能。

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