Maxwell D R, Read M A, Sumpter E A
Br J Pharmacol. 1974 Jan;50(1):35-45. doi: 10.1111/j.1476-5381.1974.tb09590.x.
1 (+/-)-10-(3-Dimethylamino-2-methylpropyl)-2-valeroylphenothiazine hydrochloride (M & B 18,706) has been compared with dimethothiazine, chloropromazine, diazepam and baclofen for potency in reducing decerebrate rigidity in the cat and rat and for activity in causing ataxia or sedation.2 When given intravenously M & B 18,706 had seven times the potency of dimethothiazine and one-half the potency of chlorpromazine in reducing the rigidity of the intercollicular decerebrate cat. When administered orally M & B 18,706 and chlorpromazine were equi-potent in reducing rigidity but M & B 18,706 was less effective than chlorpromazine in producing ataxia in this species.3 In the rat, M & B 18,706 had one-quarter the potency of chlorpromazine for reducing decerebrate rigidity but had from 1/20th to 1/200th its potency in tests for sedative or tranquillizing activity.4 M & B 18,706, like dimethothiazine and chlorpromazine, had little effect on the rigidity of ischaemic decerebrate cats and failed to inhibit polysynaptic spinal reflexes.5 M & B 18,706 had intravenous potency comparable to chlorpromazine in reducing the pressor action of noradrenaline in the spinal cat.
已将(±)-10-(3-二甲基氨基-2-甲基丙基)-2-戊酰基吩噻嗪盐酸盐(M&B 18,706)与二甲硫嗪、氯丙嗪、地西泮和巴氯芬在降低猫和大鼠去大脑僵直方面的效力以及引起共济失调或镇静的活性进行了比较。
静脉注射时,M&B 18,706在降低中脑间去大脑猫的僵直方面,效力是二甲硫嗪的7倍,是氯丙嗪的一半。口服时,M&B 18,706和氯丙嗪在降低僵直方面效力相当,但在该物种中,M&B 18,706在产生共济失调方面比氯丙嗪效果差。
在大鼠中,M&B 18,706降低去大脑僵直的效力是氯丙嗪的四分之一,但在镇静或安定活性测试中的效力仅为氯丙嗪的1/20至1/200。
M&B 18,706与二甲硫嗪和氯丙嗪一样,对缺血性去大脑猫的僵直几乎没有影响,也不能抑制多突触脊髓反射。
M&B 18,706在降低脊髓猫去甲肾上腺素的升压作用方面,静脉注射效力与氯丙嗪相当。