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Characterization of the Solubilized A1 Adenosine Receptor from Rat Brain Membranes
Authors:Karl-Norbert Klotz  Martin J Lohse  Ulrich Schwabe
Institution:Pharmakologisches Institut der Universität Heidelberg, Heidelberg, F.R.G.
Abstract:A1 adenosine receptors from rat brain membranes were solubilized with the zwitterionic detergent 3-3-(cholamidopropyl)dimethylammonio]-1-propanesulfonate. The solubilized receptors retained all the characteristics of membrane-bound A1 adenosine receptors. A high and a low agonist affinity state for the radiolabelled agonist (R)-N6-3H]phenylisopropyladenosine(3H]PIA) with KD values of 0.3 and 12 nM, respectively, were detected. High-affinity agonist binding was regulated by guanine nucleotides. In addition agonist binding was still modulated by divalent cations. The solubilized A1 adenosine receptors could be labelled not only with the agonist 3H]PIA but also with the antagonist 1,3-diethyl-8-3H]phenylxanthine. Guanine nucleotides did not affect antagonist binding as reported for membrane-bound receptors. These results suggest that the solubilized receptors are still coupled to the guanine nucleotide binding protein Ni and that all regulatory functions are retained on solubilization.
Keywords:A1 adenosine receptors  Solubilization  Rat brain membranes
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