Menon M K, Clark W G, Cannon J G
J Pharm Pharmacol. 1979 May;31(5):318-21. doi: 10.1111/j.2042-7158.1979.tb13508.x.
A single intraperitoneal (i.p.) injection in mice of apomorphine (I) and its analogues norapomorphine (II), N-ethylnorapomorphine (III), N-n-propylnorapomorphine (IV) and apocodeine (V), caused dose-related decreases in deep-core body temperature. The neuroleptic agent haloperidol blocked the hypothermia produced by these apomorphines but alpha-methyl-p-tyrosine failed to do so. This indicated a direct post-synaptic stimulation of dopamine receptors. Methysergide potentiated the hypothermic effect of the apomorphine analogues. Taking the amount of apomorphine to produce a 3 degree C fall in temperature at 30 min as unity, the approximate relative potencies were: I 1.00, II 0.06, III 47.50, IV 85.00, V 0.340. The doses of the apomorphines needed to produce hypothermia were much less than those needed to cause stereotypy. The ratios of the minimal doses required to produce hypothermia, to those producing stereotypy were: I 8.82, II 4.00, III 125.00, IV 28.50, V 1.43.
将阿扑吗啡(I)及其类似物去甲阿扑吗啡(II)、N-乙基去甲阿扑吗啡(III)、N-正丙基去甲阿扑吗啡(IV)和阿朴可待因(V)单次腹腔注射给小鼠,会导致深部核心体温出现剂量相关的下降。抗精神病药物氟哌啶醇可阻断这些阿扑吗啡产生的体温过低,但α-甲基对酪氨酸则不能。这表明对多巴胺受体有直接的突触后刺激作用。麦角新碱可增强阿扑吗啡类似物的体温过低效应。以阿扑吗啡在30分钟内使体温下降3摄氏度的量为1,近似相对效价为:I 1.00,II 0.06,III 47.50,IV 85.00,V 0.340。产生体温过低所需的阿扑吗啡剂量远低于引起刻板行为所需的剂量。产生体温过低所需的最小剂量与产生刻板行为所需的最小剂量之比为:I 8.82,II 4.00,III 125.00,IV 28.50,V 1.43。