We are analyzing https://link.springer.com/article/10.1007/bf00178977.

Title:
Autoradiographic evidence for G-protein coupled A2-receptors in rat neostriatum using [3H]-CGS 21680 as a ligand | Naunyn-Schmiedeberg's Archives of Pharmacology
Description:
Recently [3H]-CGS 21680 (2-[p-(2-carbonylethyl)-phenylethylamino]-5′-N-ethylcarboxamidoadeno-sine) has been identified as a selective adenosine A2-receptor agonist. In this study the binding of [3H]-CGS 21680 to 10 μm sections of rat neostriatum was investigated with quantitative autoradiography. Specific, saturable binding was detectable, and Scatchard analysis of saturation experiments gave estimates for K D and B max of 1.7 nM and 322 fmol/mg protein, respectively. The rank order of potency for inhibition of [3H]-CGS 21680 binding was 5′-N-ethylcarboxamidoadenosine (1.9 nM) > 2-chloroadenosine (18 nM) > R-N6-phenylisoprop-yladenosine (59 nM) > S-N6-phenylisoprophyladeno sine (460 nM) > 1,3-dipropyl-8-cyclopentylxanthine (700 nM). The binding of [3H]-CGS 21680 was sensitive to GTP, since 1 μM GTP reduced binding to 4.7% of control. These data support the identity of CGS 21680 as an agonist at high affinity adenosine A2-receptors and indicate these receptors in rat striatum are coupled to guanine nucleotide binding proteins.
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Keywords {🔍}

adenosine, receptors, google, scholar, rat, brain, article, binding, pharmacol, hcgs, autoradiographic, agonist, receptor, naunynschmiedebergs, access, privacy, cookies, content, fredholm, guanine, data, information, publish, search, areceptors, neostriatum, parkinson, selective, autoradiography, membranes, characterization, localization, williams, jarvis, schwabe, arch, analysis, log, journal, research, pharmacology, gprotein, coupled, ligand, study, quantitative, inhibition, affinity, nucleotide, open,

Topics {✒️}

g-protein coupled a2-receptors month download article/chapter n6-cyclohexyl[3h]adenosine a2 selective agonist adenosine a2 receptors a2 receptor labeled phenylethylamino]-5′-n-ethylcarboxamidoadeno-sine 322 fmol/mg protein adenosine receptor subtypes adenosine a1-receptors adenosine a1 receptors ri adenosine receptors inhibitory adenosine receptors privacy choices/manage cookies quantitative autoradiography quantitative autoradiographic study full article pdf [3h]n6-phenylisopropyladenosine related subjects article naunyn-schmiedeberg' ligand autoradiography 3-diethyl-8-[3h]phenylxanthine rat fat cells [3h]-cgs 21680 binding adenosine receptors european economic area stabilized native gpcr hippocampal synaptic transmission equilibrative nucleoside transporters preferential hypotensive activity conditions privacy policy check access instant access rat striatal membranes receptor localization accepting optional cookies rat neostriatum cultured brain cells main content log journal finder publish daly jw direct autoradiographic localization ligand published [3h]-neca [3h]-cgs 21680 coupled fredholm bb article log adenosine regulates data support

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      description:Recently [3H]-CGS 21680 (2-[p-(2-carbonylethyl)-phenylethylamino]-5′-N-ethylcarboxamidoadeno-sine) has been identified as a selective adenosine A2-receptor agonist. In this study the binding of [3H]-CGS 21680 to 10 μm sections of rat neostriatum was investigated with quantitative autoradiography. Specific, saturable binding was detectable, and Scatchard analysis of saturation experiments gave estimates for K D and B max of 1.7 nM and 322 fmol/mg protein, respectively. The rank order of potency for inhibition of [3H]-CGS 21680 binding was 5′-N-ethylcarboxamidoadenosine (1.9 nM) > 2-chloroadenosine (18 nM) > R-N6-phenylisoprop-yladenosine (59 nM) > S-N6-phenylisoprophyladeno sine (460 nM) > 1,3-dipropyl-8-cyclopentylxanthine (700 nM). The binding of [3H]-CGS 21680 was sensitive to GTP, since 1 μM GTP reduced binding to 4.7% of control. These data support the identity of CGS 21680 as an agonist at high affinity adenosine A2-receptors and indicate these receptors in rat striatum are coupled to guanine nucleotide binding proteins.
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