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腺苷5'-(2-氟二磷酸)是一种选择性激动剂,作用于介导平滑肌舒张的P2嘌呤受体。

Adenosine 5'-(2-fluorodiphosphate) is a selective agonist at P2-purinoceptors mediating relaxation of smooth muscle.

作者信息

Hourani S M, Welford L A, Loizou G D, Cusak N J

机构信息

Department of Biochemistry, University of Surrey, Guildford, U.K.

出版信息

Eur J Pharmacol. 1988 Feb 16;147(1):131-6. doi: 10.1016/0014-2999(88)90642-5.

Abstract

The pharmacological effects of ATP and of an adenine nucleotide analogue, adenosine 5'-(2-fluorodiphosphate) (ADP-beta-F) on various guinea-pig isolated smooth muscle preparations were investigated. ATP relaxed the taenia coli and the aorta, and contracted the urinary bladder and vas deferens. ADP-beta-F mimicked the effects of ATP on the taenia coli and aorta, but did not contract the bladder or vas deferens. The lack of potency of ADP-beta-F on the bladder was not due to its rapid degradation by ectonucleotidases, as it was degraded more slowly than ATP by both the bladder and the taenia coli. These results are consistent with the suggestion that the P2-purinoceptors mediating contraction of smooth muscle (P2X) are different from those mediating inhibitory effects (P2Y), and suggest that ADP-beta-F is a specific agonist at the P2Y-purinoceptor.

摘要

研究了三磷酸腺苷(ATP)及一种腺嘌呤核苷酸类似物5'-(2-氟二磷酸)腺苷(ADP-β-F)对多种豚鼠离体平滑肌标本的药理作用。ATP使结肠带和主动脉舒张,使膀胱和输精管收缩。ADP-β-F模拟了ATP对结肠带和主动脉的作用,但不使膀胱或输精管收缩。ADP-β-F对膀胱无作用并非因其被外核苷酸酶快速降解,因为它在膀胱和结肠带中的降解速度均比ATP慢。这些结果与以下观点一致,即介导平滑肌收缩的P2嘌呤受体(P2X)与介导抑制作用的受体(P2Y)不同,提示ADP-β-F是P2Y嘌呤受体的特异性激动剂。

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