磷酸修饰的腺嘌呤核苷酸类似物对灌注大鼠胰腺胰岛素分泌的影响。
Effects of phosphate-modified adenine nucleotide analogues on insulin secretion from perfused rat pancreas.
作者信息
Chapal J, Loubatieres-Mariani M M
出版信息
Br J Pharmacol. 1981 May;73(1):105-10. doi: 10.1111/j.1476-5381.1981.tb16778.x.
Abstract
1 The effects of three methylene analogues of adenosine 5'-triphosphate (ATP) or 5'-diphosphate (ADP) have been studied on insulin secretion from the isolated perfused pancreas of the rat: 5'-adenylmethylene diphosphonate or beta, gamma-methylene ATP, adenosine 5'-alpha, beta-methylene triphosphate or alpha, beta-methylene ATP and adenosine 5'-alpha, beta-methylene diphosphonate or alpha, beta-methylene ADP. 2 beta, gamma-Methylene ATP did not elicit any increase of insulin release: alpha, beta-methylene ATP and alpha, beta-methylene ADP induced a biphasic stimulation of insulin secretion; this effect was dose-related between 1.65 and 165 mumol/l. Relative potency ATP/alpha, beta-methylene ATP was 1.2 and ATP/alpha, beta-methylene ADP was 0.31. 3 Our results point to the importance of the steric and electronic characteristics of the polyphosphate chain of the analogues of ATP and ADP in inducing an insulin secretory effect. They support the hypothesis of a purine receptor for ATP and ADP.
摘要
研究了三种腺苷5'-三磷酸（ATP）或5'-二磷酸（ADP）的亚甲基类似物对大鼠离体灌注胰腺胰岛素分泌的影响：5'-腺苷亚甲基二膦酸酯或β，γ-亚甲基ATP、腺苷5'-α，β-亚甲基三磷酸或α，β-亚甲基ATP以及腺苷5'-α，β-亚甲基二膦酸酯或α，β-亚甲基ADP。
β，γ-亚甲基ATP未引起胰岛素释放增加；α，β-亚甲基ATP和α，β-亚甲基ADP诱导胰岛素分泌呈双相刺激；在1.65至165μmol / l之间，这种效应与剂量相关。ATP/α，β-亚甲基ATP的相对效价为1.2，ATP/α，β-亚甲基ADP的相对效价为0.31。
我们的结果表明，ATP和ADP类似物的多磷酸链的空间和电子特性在诱导胰岛素分泌效应中具有重要性。它们支持存在ATP和ADP嘌呤受体的假说。
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Purinergic receptors.嘌呤能受体
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