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首页> 外文期刊>Life sciences >CAPSAICIN-INDUCED BIPHASIC OXYGEN UPTAKE IN RAT MUSCLE - ANTAGONISM BY CAPSAZEPINE AND RUTHENIUM RED PROVIDES FURTHER EVIDENCE FOR PERIPHERAL VANILLOID RECEPTOR SUBTYPES (VN1/VN2)
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CAPSAICIN-INDUCED BIPHASIC OXYGEN UPTAKE IN RAT MUSCLE - ANTAGONISM BY CAPSAZEPINE AND RUTHENIUM RED PROVIDES FURTHER EVIDENCE FOR PERIPHERAL VANILLOID RECEPTOR SUBTYPES (VN1/VN2)

机译：辣椒素诱导的大鼠肌肉中的双氧吸收-卡帕西汀和钌红的拮抗作用提供了进一步的证据，证实了周围香草受体亚型（VN1 / VN2）

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Previous studies with the vanilloid spice principle capsaicin have demonstrated a biphasic VO2 response, with vasoconstriction, in the perfused rat hindlimb that has led to suggestions of vanilloid receptor subtypes (VN1/VN2) in this preparation (1). In the present study, the known competitive vanilloid antagonist capsazepine inhibited the above capsaicin-mediated effects in a manner that was indicative of binding at specific vanilloid recognition sites. Low concentrations of capsazepine selectively inhibited the increased VO2 produced by the putative VN1 receptor at submicromolar concentrations of capsaicin, while the inhibition of VO2 produced by high concentrations of capsaicin (putative VN2) was enhanced. These observations, showing different susceptibilities to blockade by capsazepine, further support the presence of two vanilloid receptor subtypes in the rat hindlimb. Schild plots of the data yielded variable slopes that approach unity at greater responses to capsaicin (mean K-B = 8.44 +/- 2.08 mu M and 7.28 +/- 0.78 mu M for VO2 and perfusion pressure curves, respectively). Low concentrations of the capsaicin antagonist ruthenium red selectively blocked the putative VN2 receptor-mediated effects produced by high concentrations of capsaicin. The noncompetitive nature of this inhibitor suggests an operation through separate receptor-coupled ion channel complexes at high and low concentrations of the vanilloid. Tetrodotoxin failed to attenuate any changes produced by capsaicin, suggesting that the mechanism of action of capsaicin in the rat hindlimb may differ from other tissues. [References: 36]
机译：先前使用香草类香料原理辣椒素的研究表明，在灌注的大鼠后肢中有血管收缩的双相VO2反应，从而提示该制剂中含有香草类受体亚型（VN1 / VN2）（1）。在本研究中，已知的竞争性类香草酸拮抗剂辣椒素以某种方式抑制上述辣椒素介导的作用，这表明在特定类香草酸识别位点的结合。在辣椒素的亚微摩尔浓度下，低浓度的辣椒素选择性抑制假定的VN1受体产生的VO2增加，而对高浓度的辣椒素（假定的VN2）产生的VO2抑制作用增强。这些观察结果显示出不同的易受卡塞平阻滞作用的敏感性，进一步支持了大鼠后肢中两种类香草素受体亚型的存在。数据的希尔德图产生了对辣椒素的更大响应时趋近于统一的可变斜率（VO2和灌注压力曲线的平均K-B分别为8.44 +/- 2.08μM和7.28 +/- 0.78μM）。低浓度的辣椒素拮抗剂钌红选择性地阻断了高浓度的辣椒素产生的假定的VN2受体介导的作用。该抑制剂的非竞争性性质表明，在高和低浓度的类香草素中，需要通过单独的受体偶联离子通道复合物进行操作。河豚毒素不能减弱辣椒素产生的任何变化，表明辣椒素在大鼠后肢中的作用机制可能不同于其他组织。 [参考：36]

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