Ponzio F, Achilli G, Perego C, Algeri S
Neurosci Lett. 1981 Nov 18;27(1):61-7. doi: 10.1016/0304-3940(81)90206-8.
Studies were undertaken to evaluate the effect of certain dopamine (DA) agonists and antagonists on DA metabolite concentrations in rat striatum, with special regard to 3-methoxytyramine (3-MT). Quipazine, nomifensine and piribedil act as dopaminergic agonist drugs. However piribedil, which is a dopaminergic receptor agonist, reduced the concentrations of all 3 metabolites considered, while nomifensine produced an increase, and quipazine caused an early rise in 3-MT followed by a lowering of the concentration of dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA). Haloperidol and clozapine are both DA antagonists. Haloperidol, which blocks DA receptors, caused an increase in the formation of all 3 metabolites while clozapine raised DOPA and HAV but not 3-MT. The importance of simultaneous determination of these 3 metabolites is discussed with relation to evaluation of the mechanism of action of these drugs and - more generally - of drugs acting on the dopaminergic system.
开展了多项研究,以评估某些多巴胺(DA)激动剂和拮抗剂对大鼠纹状体中DA代谢物浓度的影响,尤其关注3-甲氧基酪胺(3-MT)。喹哌嗪、诺米芬辛和匹莫齐特作为多巴胺能激动剂药物。然而,作为多巴胺能受体激动剂的匹莫齐特降低了所考虑的所有3种代谢物的浓度,而诺米芬辛则使其升高,喹哌嗪导致3-MT早期升高,随后二羟基苯乙酸(DOPAC)和高香草酸(HVA)浓度降低。氟哌啶醇和氯氮平均为DA拮抗剂。阻断DA受体的氟哌啶醇导致所有3种代谢物的生成增加,而氯氮平使多巴和高香草酸升高,但不影响3-MT。结合这些药物以及更普遍地作用于多巴胺能系统的药物的作用机制评估,讨论了同时测定这3种代谢物的重要性。