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• W2020201168 abstract "Effects of the alkylating agent EEDQ (N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline) on levels of dopamine transporter (DAT) and function were examined in caudate-putamen (CPu) tissue from rat brain. EEDQ produced profound, dose-dependent decreases in DAT binding in homogenates (IC50=78 μM) and frozen sections (IC75=200 μM) that were not reversed by washing. EEDQ also blocked uptake of [3H]DA in CPu synaptosomes (IC50=17 μM). However, single (10 mg/kg) or repeated administration of EEDQ in vivo (15 mg/kg/day×3) did not alter DAT levels or DA uptake in CPu. Pretreatment of rats with α-methyl-p-tyrosine and reserpine to deplete endogenous dopamine also failed to lower DAT levels in CPu after injections of EEDQ. EEDQ is an effective alkylating agent for DAT in vitro, but not to evaluate metabolic turnover or function of DAT in vivo. The results encourage development of selective and in vivo-active DAT-alkylating agents." @default.
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• W2020201168 date "2000-10-01" @default.
• W2020201168 modified "2023-09-23" @default.
• W2020201168 title "Alkylation of rat dopamine transporters and blockade of dopamine uptake by EEDQ" @default.
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• W2020201168 doi "https://doi.org/10.1016/s0028-3908(00)00047-2" @default.
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