The effect of drugs that influence the opioidergic and monoaminergic neuronal systems on the antinociceptive action of tizanidine [5-chloro-4-(2-imidazolin-2-yl-amino)-2,1, 3-benzothiodiazole] was compared with their effect on the action of clonidine. The potency of the clonidine-induced antinociceptive action was 1.83 and 7.75 times greater than that of tizanidine in the tail-flick and acetic acid-induced writhing tests, respectively. The action of tizanidine and clonidine was completely antagonized by pretreatment with yohimbine, an alpha 2-adrenoceptor blocker, but not by prazosin, an alpha 1-adrenoceptor blocker. Other alpha-adrenoceptor blockers, phenoxybenzamine and phentolamine, also attenuated the action of tizanidine and clonidine but the potency of these drugs was less than that of yohimbine. An opioid antagonist (naloxone), drugs influencing the serotonergic neuronal system (p-chlorophenylalanine, 5,6-dihydroxytryptamine, cyproheptadine), and drugs influencing the catecholaminergic system (alpha-methyl-p-tyrosine, diethyl-dithiocarbamate, 6-hydroxydopamine, haloperidol) showed no effect on the action of tizanidine and clonidine. From these results, it appears that alpha 2-adrenoceptors might be of importance in mediating the tizanidine and clonidine antinociceptive action in the tail-flick test.

译文

比较了影响碘化和单胺能神经元系统的药物对替扎尼定 [5-氯-4-(2-咪唑啉-2-基-氨基)-2,1,3-苯并硫二唑] 的抗伤害作用的影响。对可乐定的作用。在甩尾和乙酸诱导的扭动试验中,可乐定诱导的抗伤害感受作用的效力分别是替扎尼定的1.83倍和7.75倍。tizanidine和可乐定的作用通过用 α2-肾上腺素受体阻滞剂育亨宾进行预处理而完全拮抗,而不用 α1-肾上腺素受体阻滞剂哌唑嗪。其他 α-肾上腺素受体阻滞剂苯氧基苯甲胺和酚妥拉明也减弱了替扎尼定和可乐定的作用,但这些药物的效力低于育亨宾。阿片类药物拮抗剂 (纳洛酮),影响5-羟色胺能神经元系统的药物 (对氯苯丙氨酸,5,6-二羟色胺,赛庚啶) 和影响儿茶酚胺能系统的药物 (α-甲基-对-酪氨酸,二乙基-二硫代氨基甲酸,6-羟基多巴胺,氟哌啶醇) 对替扎尼定和可乐定的作用没有影响。从这些结果看来,在甩尾试验中,α2-肾上腺素受体在介导tizanidine和可乐定的抗伤害作用中可能很重要。

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