Maggi C A, Santicioli P, Geppetti P, Parlani M, Astolfi M, Pradelles P, Patacchini R, Meli A
Pharmacology Department, A. Menarini Pharmaceuticals, Florence, Italy.
Eur J Pharmacol. 1988 Sep 1;154(1):1-10. doi: 10.1016/0014-2999(88)90356-1.
Ruthenium Red, an inorganic dye which blocks transmembrane calcium (Ca) fluxes in neural tissues, reduced the capsaicin-induced release of substance P-like immunoreactivity from muscle strips of the guinea-pig urinary bladder in a concentration-dependent (30 nM - 3 microM) manner, and protected the sensory fibers from capsaicin-induced densensitization. A similar antagonism of the actions of capsaicin was observed in functional experiments (capsaicin-induced contraction of the isolated guinea-pig bladder or inhibition of twitches of the isolated rat vas deferens). In view of its established action on the depolarization-coupled entry of Ca into synaptosomes and the secretion of transmitter, we propose that Ruthenium Red could antagonize the action of capsaicin on the peripheral terminals of sensory nerves by a similar mechanism, thereby suppressing transmitter secretion and preventing the establishment of desensitization.
钌红是一种无机染料,可阻断神经组织中的跨膜钙(Ca)通量,它以浓度依赖性(30 nM - 3 microM)的方式减少了辣椒素诱导的豚鼠膀胱肌条中P物质样免疫反应性的释放,并保护感觉纤维免受辣椒素诱导的脱敏作用。在功能实验(辣椒素诱导的离体豚鼠膀胱收缩或离体大鼠输精管抽搐抑制)中也观察到了对辣椒素作用的类似拮抗作用。鉴于其对Ca进入突触体的去极化偶联进入和递质分泌的既定作用,我们提出钌红可能通过类似机制拮抗辣椒素对感觉神经外周终末的作用,从而抑制递质分泌并防止脱敏的发生。