Kohli J D, Glock D, Goldberg L I
Eur J Pharmacol. 1985 Aug 27;114(3):305-10. doi: 10.1016/0014-2999(85)90374-7.
The (+)- and (-)-enantiomers of 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP) were studied for their effects on DA1 and DA2 dopamine receptors in pentobarbital anesthetized dogs. 3-PPP enantiomers were administered into the renal artery after phenoxybenzamine pretreatment to determine possible DA1 activity; dopamine was also injected for comparison. DA2 activity was determined by injection of the enantiomers into the femoral vascular bed with intact nerve supply and without phenoxybenzamine; dipropyl dopamine (DPDA) or apomorphine were used as standard DA2 agonists. Antagonist activity of the enantiomers on DA1 or DA2 receptors was determined by simultaneous administration of the enantiomer with DA in the renal vascular bed and with DPDA or apomorphine in the femoral vascular bed. Neither enantiomer was active as a DA1 agonist, but both exhibited antagonist activity. Both enantiomers were found to be agonists of the DA2 receptor; in addition, both showed DA2 antagonist activity. In all actions the (-)-enantiomer was approximately 4 times more potent than the (+)-enantiomer.
研究了3-(3-羟基苯基)-N-正丙基哌啶(3-PPP)的(+)-和(-)-对映体对戊巴比妥麻醉犬的DA1和DA2多巴胺受体的影响。在酚苄明预处理后，将3-PPP对映体注入肾动脉以确定其可能的DA1活性；还注射多巴胺作为对照。通过将对映体注入神经供应完整且未用酚苄明处理的股血管床来测定DA2活性；使用二丙基多巴胺(DPDA)或阿扑吗啡作为标准DA2激动剂。通过在肾血管床中将对映体与多巴胺同时给药，以及在股血管床中将对映体与DPDA或阿扑吗啡同时给药，来测定对映体对DA1或DA2受体的拮抗活性。两种对映体均无DA1激动剂活性，但均表现出拮抗活性。发现两种对映体均为DA2受体激动剂；此外，两者均表现出DA2拮抗活性。在所有作用中，(-)-对映体的效力约为(+)-对映体的4倍。
