Nissbrandt H, Pileblad E, Carlsson A
J Pharm Pharmacol. 1985 Dec;37(12):884-9. doi: 10.1111/j.2042-7158.1985.tb04994.x.
In rat substantia nigra a biphasic disappearance curve of dopamine (DA) was seen after tyrosine hydroxylase inhibition by alpha-methyl-p-tyrosine (alpha-MT): the initial phase had a fast turnover and a half life of 0.5 h and the later phase had an extremely slow turnover. In contrast to the effects in striatum, neither haloperidol nor apomorphine influenced alpha-MT-induced DA disappearance in the substantia nigra. Furthermore, inhibition of impulse flow by gamma-butyrolactone prevented DA disappearance in striatum but not in the substantia nigra. Measurements of DA and 3-methoxytyramine following treatment with inhibitors of monoamine oxidase (pargyline) and catechol-O-methyl transferase (tropolone) indicated that O-methylation is a more important metabolic pathway in the substantia nigra than in the striatum. The data are interpreted to indicate that the release and metabolism of DA in the substantia nigra are largely beyond the control of nerve impulses and DA receptors. It is suggested that such an arrangement forms an important feature of autoreceptor-mediated feedback control of DA nerve cell activity.
在大鼠黑质中,用α-甲基-对-酪氨酸(α-MT)抑制酪氨酸羟化酶后,观察到多巴胺(DA)呈现双相消失曲线:初始阶段周转迅速,半衰期为0.5小时,后期阶段周转极其缓慢。与纹状体中的效应相反,氟哌啶醇和阿扑吗啡均不影响α-MT诱导的黑质中DA的消失。此外,γ-丁内酯抑制冲动流可阻止纹状体中DA的消失,但不能阻止黑质中DA的消失。用单胺氧化酶抑制剂(帕吉林)和儿茶酚-O-甲基转移酶抑制剂(托酚酮)处理后对DA和3-甲氧基酪胺的测量表明,O-甲基化在黑质中是比在纹状体中更重要的代谢途径。这些数据被解释为表明黑质中DA的释放和代谢在很大程度上不受神经冲动和DA受体的控制。有人提出,这种安排构成了DA神经细胞活动的自受体介导的反馈控制的一个重要特征。