Clark D, Hjorth S, Carlsson A
Eur J Pharmacol. 1984 Oct 30;106(1):185-9. doi: 10.1016/0014-2999(84)90694-0.
Both enantiomers of the dopamine analogue 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP; 0.5-32 mg/kg s.c.) dose dependently reduced the increase in striatal dopamine (DA) synthesis rate produced by gamma-butyrolactone (GBL). Whereas (+)-3-PPP completely prevented the action of GBL, (-)-3-PPP was only partially effective. In addition, (-)-3-PPP partially antagonised the inhibitory action of apomorphine on the GBL-induced increase in DA synthesis rate. These findings suggest that (+)- and (-)-3-PPP act as full and partial agonists respectively, at striatal DA autoreceptors controlling DA synthesis.
多巴胺类似物3-(3-羟基苯基)-N-正丙基哌啶(3-PPP;0.5-32毫克/千克,皮下注射)的两种对映体均剂量依赖性地降低了γ-丁内酯(GBL)所引起的纹状体多巴胺(DA)合成速率的增加。(+)-3-PPP完全阻断了GBL的作用,而(-)-3-PPP仅部分有效。此外,(-)-3-PPP部分拮抗了阿扑吗啡对GBL诱导的DA合成速率增加的抑制作用。这些发现表明,(+)-和(-)-3-PPP分别作为完全激动剂和部分激动剂,作用于控制DA合成的纹状体DA自身受体。