Davies J, Johnston S E, Hill D R, Quinlan J E
Neurosci Lett. 1984 Jul 27;48(2):197-202. doi: 10.1016/0304-3940(84)90019-3.
The effects of microiontophoretic ejection of tizanidine were compared with those of adrenoceptor agonists on responses of single laminae IV and V neurones to noxious and innocuous cutaneous stimuli. Tizanidine, noradrenaline and clonidine depressed neuronal responses to noxious but not innocuous stimuli. Spontaneous activity was also depressed by these three substances. By contrast, beta- and alpha 1-adrenoceptor agonists had no consistent effect on neuronal responses to cutaneous stimuli. The selective actions of tizanidine, noradrenaline and clonidine were reversibly antagonized by the alpha 2-adrenoceptor antagonist RX781094 but not by WB4101 (alpha 1 antagonist). The binding of an alpha 2-adrenoceptor ligand to rat brain membranes was preferentially displaced by tizanidine. These results indicate an interaction of tizanidine with central alpha 2-adrenoceptors.
将替扎尼定微量离子导入与肾上腺素能受体激动剂对IV和V层单神经元对有害和无害皮肤刺激反应的影响进行了比较。替扎尼定、去甲肾上腺素和可乐定抑制神经元对有害刺激而非无害刺激的反应。这三种物质也抑制自发活动。相比之下，β-和α1-肾上腺素能受体激动剂对神经元对皮肤刺激的反应没有一致的影响。替扎尼定、去甲肾上腺素和可乐定的选择性作用可被α2-肾上腺素能受体拮抗剂RX781094可逆性拮抗，但不能被WB4101（α1拮抗剂）拮抗。替扎尼定优先取代α2-肾上腺素能受体配体与大鼠脑膜的结合。这些结果表明替扎尼定与中枢α2-肾上腺素能受体存在相互作用。
