A COMPARISON OF CAPSAZEPINE AND RUTHENIUM RED AS CAPSAICIN ANTAGONISTS IN THE RAT ISOLATED URINARY-BLADDER AND VAS-DEFERENS
A COMPARISON OF CAPSAZEPINE AND RUTHENIUM RED AS CAPSAICIN ANTAGONISTS IN THE RAT ISOLATED URINARY-BLADDER AND VAS-DEFERENS
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DOI：
10.1111/j.1476-5381.1993.tb12881.x
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发表时间：
1993-03-01
影响因子：
7.3
通讯作者：
GIULIANI, S
中科院分区：
文献类型：
--
作者：
MAGGI, CA;BEVAN, S;GIULIANI, S
1 将辣椒素（一种最近开发的辣椒素受体拮抗剂）防止辣椒素对大鼠离体膀胱（收缩）和输精管（抑制电诱发抽搐）的影响的能力与钌红（一种作为辣椒素功能性拮抗剂的染料）进行比较。2 在大鼠膀胱中，辣椒素（3 - 30 mum）产生浓度依赖性曲线右移，辣椒素对激动剂的最大反应没有任何显着抑制。相比之下，钌红（10 - 30 mum）产生非竞争性拮抗作用，其特征是可达到的最大反应明显降低。在大鼠离体输精管中也获得了类似的结果，其中辣椒西平（10μm）产生了对辣椒素的曲线向右移动，而钌红（3μm）抑制了对激动剂的最大反应。 3在用于阻断辣椒素作用的浓度下，辣椒西平和钌红均不影响由神经激肽A或电场刺激或大鼠产生的抽搐抑制产生的大鼠膀胱的收缩反应。输精管中的 α-降钙素基因相关肽 (alphaCGRP)。4 这些发现提供了额外的证据，表明辣椒素和钌红都是探索辣椒素敏感的初级传入神经元功能的宝贵工具。辣椒素对辣椒素作用的拮抗作用与该物质与位于初级传入神经上的香草酸受体的相互作用完全一致，而钌红的作用显然涉及更复杂的非竞争性拮抗作用。
1 The ability of capsazepine, a recently developed capsaicin receptor antagonist, to prevent the effects of capsaicin on the rat isolated urinary bladder (contraction) and vas deferens (inhibition of electrically-evoked twitches) was compared to that of ruthenium red, a dye which behaves as a functional antagonist of capsaicin.2 In the rat bladder, capsazepine (3 - 30 mum) produced a concentration-dependent rightward shift of the curve to capsaicin without any significant depression of the maximal response to the agonist. By contrast, ruthenium red (10 - 30 mum) produced a non-competitive type of antagonism, characterized by marked depression of the maximal response attainable. Similar findings were obtained in the rat isolated vas deferens in which capsazepine (10 mum) produced a rightward shift of the curve to capsaicin while ruthenium red (3 mum) depressed the maximal response to the agonist.3 At the concentrations used to block the effect of capsaicin, neither capsazepine nor ruthenium red affected the contractile response of the rat urinary bladder produced by either neurokinin A or electrical field stimulation or the twitch inhibition produced by rat alpha-calcitonin gene-related peptide (alphaCGRP) in the vas deferens.4 These findings provide additional evidence that both capsazepine and ruthenium red are valuable tools for exploration of the function of capsaicin-sensitive primary afferent neurones. The antagonism of the action of capsaicin by capsazepine is entirely consistent with the proposed interaction of this substance with a vanilloid receptor located on primary afferents, while the action of ruthenium red apparently involves a more complex, non-competitive antagonism.