Theobald R J
Eur J Pharmacol. 1986 Jan 29;120(3):351-4. doi: 10.1016/0014-2999(86)90476-0.
Previously reported work has provided evidence that arylazido aminopropionyl ATP (ANAPP3), a P2-receptor antagonist, blocks the effects of ATP and other purine analogs, in the urinary bladder of the cat. This antagonism appeared limited to those effects mediated by P2-receptors, such as contraction of the urinary bladder. However, it was noted that ANAPP3 did alter the effects of adenosine, mediated through P1-receptors, in some preliminary experiments. A series of experiments was undertaken to determine if ANAPP3 blocks the P1-receptors and/or has effects on inhibition of bladder contractions. The urinary tract of anesthetized cats was exposed by a midline abdominal incision. The pelvic and hypogastric nerves were isolated and prepared for electrical stimulation. Bladder contractions were induced by stimulation of the pelvic nerves every 30 s with square wave pulses. These contractions were inhibited by hypogastric nerves and the exogenous administration of ATP, noradrenaline, adenosine or beta,gamma-methylene ATP (APPCP), a hydrolysis resistant analog of ATP. ANAPP3 (0.5 mumol, i.a.) was administered, but it did not antagonize the inhibition induced by any of the exogenously administered agents or hypogastric nerve stimulation. This study indicates that ANAPP3 is specific for P2-receptors and is not an effective antagonist of P1-receptors, at least in the urinary tract of the cat.
先前报道的研究工作已提供证据表明，P2受体拮抗剂芳基叠氮氨基丙酰ATP（ANAPP3）可阻断ATP及其他嘌呤类似物在猫膀胱中的作用。这种拮抗作用似乎仅限于由P2受体介导的那些效应，如膀胱收缩。然而，在一些初步实验中注意到，ANAPP3确实改变了通过P1受体介导的腺苷的效应。开展了一系列实验以确定ANAPP3是否阻断P1受体和/或对膀胱收缩的抑制有影响。通过腹部中线切口暴露麻醉猫的尿路。分离并准备好盆神经和腹下神经用于电刺激。每隔30秒用方波脉冲刺激盆神经以诱导膀胱收缩。这些收缩可被腹下神经以及外源性给予ATP、去甲肾上腺素、腺苷或β，γ-亚甲基ATP（APPCP，一种ATP的抗水解类似物）所抑制。给予ANAPP3（0.5 μmol，腹腔注射），但它并未拮抗任何外源性给予的药物或腹下神经刺激所诱导的抑制作用。本研究表明，至少在猫的尿路中，ANAPP3对P2受体具有特异性，而不是P1受体的有效拮抗剂。
