Janiec W, Piekarska T, Pytlik M, Pałetko Z
Pol J Pharmacol Pharm. 1978 Jul-Aug;30(4):521-7.
We tested the effect of various concentrations (10(-6)--10(-4) M) of dopamine (DA), apomorphine (APM), amantadine (AMD), dimethylaminoadamantane (DMAD) and haloperidol (HP) on in vitro incorporation of 14C/U/adenine to slices of the rat striate body. Two mechanisms participated in this incorporation: one of them (uptake I) of Km = 1.92 micron, the second (uptake II) of Km 434 micron, APM inhibited both uptake I and II, while AMD and DMAD only the uptake I. HP at concentration inhibiting the dopaminergic receptors did not affect the inhibition by APM, AMD or DMAD of incorporation of exogenous adenine to striatal slices. Incorporation of exogenous adenine was not related to stimulation by specific (DA) or unspecific (APM, AMD, DMAD) stimulants of dopaminergic receptors in the rat striate body. The inhibition of the uptake produced by APM, AMD and DMAD may be related to the mechanism of action of these compounds.
我们测试了不同浓度(10⁻⁶ - 10⁻⁴M)的多巴胺(DA)、阿扑吗啡(APM)、金刚烷胺(AMD)、二甲氨基金刚烷(DMAD)和氟哌啶醇(HP)对大鼠纹状体切片中¹⁴C/尿嘧啶/腺嘌呤体外掺入的影响。这种掺入有两种机制参与:其中一种(摄取I)的Km = 1.92微米,另一种(摄取II)的Km为434微米,APM抑制摄取I和摄取II,而AMD和DMAD仅抑制摄取I。在抑制多巴胺能受体的浓度下,HP并不影响APM、AMD或DMAD对外源性腺嘌呤掺入纹状体切片的抑制作用。外源性腺嘌呤的掺入与大鼠纹状体中多巴胺能受体的特异性(DA)或非特异性(APM、AMD、DMAD)刺激剂的刺激无关。APM、AMD和DMAD对摄取的抑制作用可能与其作用机制有关。