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• W2000648746 abstract "Binding of the non-selective adenosine receptor agonist, [3H]NECA (5′-N-Ethylcar☐amidoadenosine) was evaluated in sections of rat brain using quantitative receptor autoradiography. [3H]NECA bound specifically to a variety of different brain regions including striatum, cerebellum and thalamus. In the presence of the selective adenosine A1 receptor agonist, cyclopentyladenosine (CPA; 50 nM), [3H]NECA binding was exclusively localized to the striatum and olfactory tubercle. Binding in rat striatum occured at a single site (Kd=9nM) with limited capacity (apparent Bmax = 230fmol/mg tissue). Competition experiments in both striatum and olfactory tubercle with various adenosine agonists and antagonists indicated that the sites labeled by [3H]NECA in the presence of 50 nM CPA were A2 in nature, the rank order of activity for agonists being NECA> 2-chloroadenosine(2-CADO), >R-N6-phenylisopropyladenosine(R-PIA) >CPA>S-N6-phenylisopropyladenosine(S-PIA). For xanthine antagonists the order was 1,3-dipropyl-8(2-amino-4-chloro)phenylxanthine(PACPX) >xanthine amino acid congener(XAC) >xanthine car☐ylic acid congener(XCC) > 1,3-diethyl-8-phenylxanthine(DPX). The localization of A2 receptors to discrete regions of rat brain indicates that the purine may have a selective role in modulating basal ganglia function." @default.
• W2000648746 created "2016-06-24" @default.
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• W2000648746 date "1989-04-01" @default.
• W2000648746 modified "2023-10-06" @default.
• W2000648746 title "Autoradiographic characterization of high-affinity adenosine A2 receptors in the rat brain" @default.
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• W2000648746 doi "https://doi.org/10.1016/0006-8993(89)90353-3" @default.
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