%0 Journal Article %1 Klotz1986a %A Klotz, K. N. %A Lohse, M. J. %A Schwabe, U. %D 1986 %J J Neurochem %K *Brain Animals Binding, Calcium/pharmacology Cations, Cell Chemistry Competitive Divalent GTP Guanosine Kinetics Magnesium/pharmacology Manganese/pharmacology Membrane/analysis Phenylisopropyladenosine/metabolism Phosphohydrolases/metabolism Purinergic Rats Surface/drug Triphosphate/pharmacology Xanthines/pharmacology effects/*metabolism Receptor %N 5 %P 1528-34 %T Characterization of the solubilized A1 adenosine receptor from rat brain membranes %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=3007672 %V 46 %X 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)-N6-3Hphenylisopropyladenosine(3HPIA) 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 3HPIA but also with the antagonist 1,3-diethyl-8-3Hphenylxanthine. 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.

@article{Klotz1986a, 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.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Klotz, K. N. and Lohse, M. J. and Schwabe, U.}, biburl = {https://www.bibsonomy.org/bibtex/2aefddfd4c90d12f656a01ddc3ee5d9cc/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {d7903605268aacda39b38cb8b1f31be5}, intrahash = {aefddfd4c90d12f656a01ddc3ee5d9cc}, issn = {0022-3042 (Print) 0022-3042 (Linking)}, journal = {J Neurochem}, keywords = {*Brain Animals Binding, Calcium/pharmacology Cations, Cell Chemistry Competitive Divalent GTP Guanosine Kinetics Magnesium/pharmacology Manganese/pharmacology Membrane/analysis Phenylisopropyladenosine/metabolism Phosphohydrolases/metabolism Purinergic Rats Surface/drug Triphosphate/pharmacology Xanthines/pharmacology effects/*metabolism Receptor}, month = May, note = {Klotz, K N Lohse, M J Schwabe, U Comparative Study Research Support, Non-U.S. Gov't United states Journal of neurochemistry J Neurochem. 1986 May;46(5):1528-34.}, number = 5, pages = {1528-34}, shorttitle = {Characterization of the solubilized A1 adenosine receptor from rat brain membranes}, timestamp = {2010-12-14T18:20:05.000+0100}, title = {Characterization of the solubilized A1 adenosine receptor from rat brain membranes}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=3007672}, volume = 46, year = 1986 }