DOI: 10.1111/j.1471-4159.1988.tb01129.x. A<sub>1</sub> Adenosine Receptor‐G Protein Coupling in Bovine Brain Membranes: Effects of Guanine Nucleotides, Salt, and Solubilization

A1 Adenosine Receptor‐G Protein Coupling in Bovine Brain Membranes: Effects of Guanine Nucleotides, Salt, and Solubilization

10.1111/j.1471-4159.1988.tb01129.x

Crossref journal-article

Wiley

Journal of Neurochemistry (311)

Abstract

Abstract: The effects of guanine nucleotides, NaCl, and solubilization on the interaction of antagonists and agonists with the A1 adenosine receptor of bovine brain membranes were studied using the high‐affinity antagonist radioligand [3H]xanthine amine congener ([3H]XAC). In membranes, guanine nucleotides and NaCl had no effect on [3H]XAC saturation curves. Using agonist (R)‐phenylisopropyladenosine (R‐PIA) competition curves versus [3H]XAC, it was demonstrated that agonists could differentiate two affinity states having high and low affinity for agonist and that guanine nucleotides shifted the equilibrium to an all‐low‐affinity state that was indistinguishable from the low‐affinity state in the absence of guanine nucleotides. In contrast, NaCl decreased agonist affinity by a distinctly different mechanism characterized by a parallel rightward shifted agonist curve such that R‐PIA still recognized two affinity states albeit of lower affinity than in the absence of salt. R‐PIA competition curves in the presence of both guanine nucleotides and salt were still shallow but were shifted far to the right, and two very low affinity states were discerned. On solubilization, guanine nucleotides in a reversible, concentration‐dependent manner increased antagonist ([3H]XAQ but not agonist (R‐N6‐−[3H]phenyl‐isopropyladenosine) binding. This was consequent to a change in maximal binding capacity. R‐PIA competition curves (versus [3H]XAC) in solubilized preparations demonstrated that agonist could still differentiate two agonist specific affinity states which were modulated by guanine nucleotides. In the presence of guanine nucleotides all the receptors were shifted to a uniform low‐affinity state. In contrast, NaCl had no effect on agonist affinity as determined by agonist competition curves in a solubilized receptor preparation. This is firm evidence that guanine nucleotides and NaCl must decrease agonist affinity by distinct mechanisms.

Bibliography

Stiles, G. L. (1988). A1 Adenosine ReceptorâG Protein Coupling in Bovine Brain Membranes: Effects of Guanine Nucleotides, Salt, and Solubilization. Journal of Neurochemistry, 51(5), 1592â1598. Portico.

Authors 1

Gary L. Stiles (first)

References 16 Referenced 56

10.1016/0003-2697(76)90527-3
10.1016/0003-2697(83)90427-X
10.1152/ajpcell.1978.235.3.C97
{'key': 'e_1_2_2_5_1', 'first-page': '5', 'article-title': 'Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes', 'volume': '21', 'author': 'DeLean A.', 'year': '1982', 'journal-title': 'Mol. Pharmacol'} / Mol. Pharmacol / Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes by DeLean A. (1982)
10.1126/science.6280275
10.1146/annurev.bi.56.070187.003151
{'key': 'e_1_2_2_8_1', 'first-page': '329', 'article-title': 'Guanine nucleotide and cation regulation of [3H]cyclo‐hexyladenosine and [3H]diethyl phenylxanthine to adenosine A1 receptors in brain membranes.', 'volume': '21', 'author': 'Goodman R. A.', 'year': '1982', 'journal-title': 'Mol. Pharmacol'} / Mol. Pharmacol / Guanine nucleotide and cation regulation of [3H]cyclo‐hexyladenosine and [3H]diethyl phenylxanthine to adenosine A1 receptors in brain membranes. by Goodman R. A. (1982)
10.1016/0165-6147(87)90042-3
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{'key': 'e_1_2_2_11_1', 'first-page': '173', 'article-title': 'Inhibition of adenylate cyclase by hormones and neurotransmitters', 'volume': '14', 'author': 'Jacobs K. H.', 'year': '1981', 'journal-title': 'Adv. Cyclic Nucleotide Res'} / Adv. Cyclic Nucleotide Res / Inhibition of adenylate cyclase by hormones and neurotransmitters by Jacobs K. H. (1981)
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10.1111/j.1471-4159.1986.tb01772.x
10.1016/S0021-9258(18)88840-8 / J. Biol. Chem / The A1 adenosine receptor: solubilization of a guanine nucleotide‐sensitive form of the receptor by Stiles G. L. (1985)
10.1016/0165-6147(86)90434-7
10.1152/physrev.1984.64.2.661
10.1016/S0021-9258(18)32928-4 / J. Biol Chem / Agonist and antagonist affinities for inhibitory adenosine receptors are reciprocally affected by 5′‐guanylylimidodiphosphate or N‐ethylmaleimide by Yeung S. H. (1983)

Dates

Type	When
Created	18 years, 11 months ago (Oct. 5, 2006, 6:20 p.m.)
Deposited	1 year, 10 months ago (Oct. 20, 2023, 11:54 p.m.)
Indexed	1 year, 3 months ago (May 12, 2024, 5 p.m.)
Issued	36 years, 10 months ago (Nov. 1, 1988)
Published	36 years, 10 months ago (Nov. 1, 1988)
Published Online	18 years, 11 months ago (Oct. 5, 2006)
Published Print	36 years, 10 months ago (Nov. 1, 1988)

Funders 0

None

BibTeX

@article{Stiles_1988, title={A1 Adenosine Receptor‐G Protein Coupling in Bovine Brain Membranes: Effects of Guanine Nucleotides, Salt, and Solubilization}, volume={51}, ISSN={1471-4159}, url={http://dx.doi.org/10.1111/j.1471-4159.1988.tb01129.x}, DOI={10.1111/j.1471-4159.1988.tb01129.x}, number={5}, journal={Journal of Neurochemistry}, publisher={Wiley}, author={Stiles, Gary L.}, year={1988}, month=nov, pages={1592–1598} }

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