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NE - 19550和NE - 21610,抗伤害性辣椒素类似物:新生大鼠尾部伤害性纤维的体外研究

NE-19550 and NE-21610, antinociceptive capsaicin analogues: studies on nociceptive fibres of the neonatal rat tail in vitro.

作者信息

Dray A, Bettaney J, Rueff A, Walpole C, Wrigglesworth R

机构信息

Sandoz Institute for Medical Research, London, U.K.

出版信息

Eur J Pharmacol. 1990 Jun 8;181(3):289-93. doi: 10.1016/0014-2999(90)90091-j.

Abstract

When applied to peripheral fibres in a neonatal rat tail/spinal cord preparation in vitro, capsaicin (0.2-50 microM) induced an activation, selective desensitization and reduced responses to other noxious stimuli (heat, bradykinin). Similar concentrations of the antinociceptive analogues NE-19550 and NE-21610, did not affect peripheral fibre responsiveness but induced cross desensitization to capsaicin. At 500 microM both analogues produced similar effects to capsaicin. Capsaicin analogues may induce analgesia without initial activation of nociceptors.

摘要

当应用于新生大鼠尾巴/脊髓体外制备的外周纤维时,辣椒素(0.2 - 50微摩尔)诱导激活、选择性脱敏,并降低对其他有害刺激(热、缓激肽)的反应。抗伤害感受类似物NE - 19550和NE - 21610的类似浓度不影响外周纤维反应性,但诱导对辣椒素的交叉脱敏。在500微摩尔时,两种类似物产生与辣椒素相似的效果。辣椒素类似物可能在不初始激活伤害感受器的情况下诱导镇痛。

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