Ohata K, Murata T, Sakamoto H, Inoue K, Kobayashi M, Kohno S, Nagasaka Y, Kasai H
Nihon Yakurigaku Zasshi. 1982 Dec;80(6):471-80.
The general pharmacological properties of guanabenz (Wy-8678), a new centrally acting antihypertensive agent, on the central nervous system were studied in mice, rats and rabbits, and they were compared with those of clonidine. In mice, guanabenz (1-30 mg/kg, i.p.) showed overt sedation dose-dependently, like clonidine (0.3 or 1 mg/kg, i.p.). At doses (2.5-20 mg/kg, p.o.) not causing muscle relaxant action, guanabenz impaired rotarod performance, inhibited conditioned avoidance responses and maximum electroshock seizure, prolonged thiopental sleeping time, and lowered body temperature in rats. These central depressant effects were observed following oral administration of clonidine at much lower dose levels. In rabbits, neither guanabenz (5-20 mg/kg, p.o.) nor clonidine (0.5 or 1 mg/kg, p.o.) affected body temperature. These findings suggest that the central depressant activities of guanabenz, qualitatively very similar to clonidine, are much less potent than those of clonidine.
对新型中枢性抗高血压药物胍那苄（Wy-8678）在小鼠、大鼠和兔子身上的中枢神经系统一般药理特性进行了研究，并与可乐定的特性进行了比较。在小鼠中，胍那苄（1-30毫克/千克，腹腔注射）剂量依赖性地表现出明显的镇静作用，与可乐定（0.3或1毫克/千克，腹腔注射）相似。在不引起肌肉松弛作用的剂量（2.5-20毫克/千克，口服）下，胍那苄会损害大鼠的转棒性能，抑制条件性回避反应和最大电休克惊厥，延长硫喷妥钠睡眠时间，并降低大鼠体温。在低得多的剂量水平口服可乐定后也观察到了这些中枢抑制作用。在兔子中，胍那苄（5-20毫克/千克，口服）和可乐定（0.5或1毫克/千克，口服）均不影响体温。这些发现表明，胍那苄的中枢抑制活性在性质上与可乐定非常相似，但其效力远低于可乐定。
