安非他命的影响比较,苯乙胺和相关药物对多巴胺流出,多巴胺吸收和马吲哚绑定。

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帕克EM, Cubeddu LX

安非他命的影响比较,苯乙胺和相关药物对多巴胺流出,多巴胺吸收和马吲哚绑定。

J Exp其他杂志》1988年4月,245 (1):199 - 210。

PubMed ID

3129549 (在PubMed

]

文摘

我们量化影响安非他命(两栖的),苯乙胺(豌豆),酪胺(酪氨酸)、章鱼胺(10月)和DA, DA的初始利率吸收(饰纹状体),绑定[3 h]马吲哚的神经元摄取(ν)网站(纹状体膜)和DA和dihydroxyphenylacetic酸(DOPAC)流出(纹状体片)。一般来说,效力三范式的顺序是:两栖的小于DA =酪氨酸=豌豆小于10月吸收的Km值与抑制的Ki值呈正相关,马吲哚绑定(r = 0.91;P . 01)和效能诱导DA流出(r = 0.96;不到.005页)。效能为马吲哚绑定和抑制诱发DA流出也高度相关(r = 0.92;P小于. 01)。相关性是丢失数据nomifensine(笔名),ν抑制剂,包括在分析中。尽管有显著的相关性,两栖的,酪氨酸,豌豆和10月尽管显著相关性,两栖的,酪氨酸,豌豆,10月10到20倍更有效抑制ν比诱发流出或抑制马吲哚绑定。相反,笔名抑制马吲哚绑定的效力10到800倍,需要抑制ν或引起DA版本,分别。笔名抑制竞争性AMPH-induced DA释放。 These results suggest that: 1) AMPH-like drugs bind to and are likely to be transported by the NU carrier, and 2) inward transport of these agents appears to have multiple effects (e.g., an increase in intracellular Na+ and Cl-) that act cooperatively to increase Vmax and reduce Km for the outward, carrier-mediated DA transport. AMPH, TYR, PEA and OCT had qualitatively similar effects on endogenous DA and [3H]DA release. Monoamine oxidase inhibition potentiated these effects. All these agents released more endogenous DA from control than from reserpine-treated slices. In control slices, TYR and OCT increased DA and DOPAC efflux; whereas AMPH and PEA increased DA and reduced DOPAC efflux, except at high concentrations in which DOPAC efflux also was increased. After reserpine, these agents reduced DOPAC efflux in proportion to the increased DA efflux. In summary, we propose that AMPH-like drugs increase DA efflux from a single cytoplasmic pool maintained by DA synthesis and spontaneous and drug-induced efflux of DA from storage vesicles.(ABSTRACT TRUNCATED AT 400 WORDS)

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