Ochiai T, Yamamura M, Kudo Y, Ishida R
Nihon Yakurigaku Zasshi. 1981 Oct;78(4):347-57.
The general pharmacology of afloqualone, a new centrally acting muscle relaxant, in the CNS was examined in mice and rats and findings compared with those of other central muscle relaxants. Afloqualone showed relatively strong hexobarbital and barbital anesthesia potentiating action. Taking into account the dose ratio of anesthesia potentiating action to the muscle relaxing action, however, the potency of anesthesia potentiating action of afloqualone is lower than that of chlormezanone. At doses producing muscle relaxing action, afloqualone inhibited spontaneous motor activity, methamphetamine-induced hypermotility, pentylenetetrazol-, nicotine-, and maximum electroshock-convulsions, fighting episodes in foot-shocked mice, conditioned avoidance response in rat pole-climbing test, and acetic acid-induced writhing syndrome and lowered normal body temperature. The dose ratios of these pharmacological actions to muscle relaxing action of afloqualone, however, were larger than those of chlormezanone and mephenesin. This suggests that the central depressant activity of afloqualone is less potent and the specificity of muscle relaxing action of afloqualone is higher than those of climbing behaviour, physostigmine-induced death, serotonin-induced heat twitch, and reserpine-induced hypothermia, even at 50 mg/kg. Tolperisone showed neither muscle relaxing action nor other central actions when administered orally.
对新型中枢性肌肉松弛剂阿夫罗喹酮在中枢神经系统的一般药理学进行了小鼠和大鼠实验，并将结果与其他中枢性肌肉松弛剂进行了比较。阿夫罗喹酮表现出相对较强的增强己巴比妥和巴比妥麻醉的作用。然而，考虑到麻醉增强作用与肌肉松弛作用的剂量比，阿夫罗喹酮的麻醉增强作用效力低于氯美扎酮。在产生肌肉松弛作用的剂量下，阿夫罗喹酮抑制自发运动活动、甲基苯丙胺诱导的活动亢进、戊四氮、尼古丁和最大电休克惊厥、足部电击小鼠的打斗行为、大鼠爬杆试验中的条件回避反应以及醋酸诱导的扭体综合征，并降低正常体温。然而，阿夫罗喹酮这些药理作用与肌肉松弛作用的剂量比大于氯美扎酮和甲酚甘油醚。这表明阿夫罗喹酮的中枢抑制活性较弱，且阿夫罗喹酮肌肉松弛作用的特异性高于氯美扎酮和甲酚甘油醚。即使在50mg/kg时，阿夫罗喹酮对攀爬行为、毒扁豆碱诱导的死亡、血清素诱导的热抽搐和利血平诱导的体温过低也没有影响。口服托哌酮既无肌肉松弛作用，也无其他中枢作用。
