Modulation of agonist responses at the A1 adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state

Biochemical Pharmacology

Volumn 64, Issue 8, 2002, Pages 1251-1265

  Lorenzen, Anna ^a   Beukers, Margot W ^b   Van der Graaf, Piet Hein ^c   Lang, Heidrun ^a   Van Muijlwijk Koezen, Jacqueline ^b   De Groote, Miriam ^b   Menge, Wiro ^b   Schwabe, Ulrich ^a   IJzerman, Adriaan P ^b  

^a UNIVERSITY OF HEIDELBERG   (Germany)

^b LEIDEN UNIVERSITY   (Netherlands)

^c PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Adenosine; Efficacy; Intrinsic activity; Potency; Receptor reserve; Two state model

Indexed keywords

1 PROPYL 3 [3 [[4 (FLUOROSULFONYL)BENZOYL]OXY]PROPYL] 8 CYCLOPENTYLXANTHINE; 2 CHLORO 6 N CYCLOPENTYLADENOSINE; 5' METHYLTHIOADENOSINE; ADENOSINE A1 RECEPTOR; ADENOSINE RECEPTOR BLOCKING AGENT; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); GUANOSINE DIPHOSPHATE; N ETHYLMALEIMIDE; UNCLASSIFIED DRUG; XANTHINE DERIVATIVE;

ANIMAL TISSUE; ARTICLE; BRAIN MEMBRANE; CONCENTRATION RESPONSE; CONTROLLED STUDY; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT; STIMULATION;

ANIMALS; BRAIN; ETHYLMALEIMIDE; GTP-BINDING PROTEINS; GUANINE NUCLEOTIDES; LIGANDS; RATS; RECEPTORS, PURINERGIC P1; SULFHYDRYL REAGENTS; XANTHINES;

EID: 0037107511     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(02)01293-5     Document Type: Article

References (42)

1. o. J. Biol. Chem. 266:1991;22285-22289.
2. 1 adenosine receptor with recombinant G protein α-subunits. J. Biol. Chem. 266:1991;17778-17783.
3. iα2 suppressed by inducible antisense RNA. Dev. Genet. 14:1993;266-273.
4. Pelleg A., Belardinelli L. Cardiac electrophysiology and pharmacology of adenosine: basic and clinical aspects. Cardiovasc. Res. 27:1993;54-61.
5. 2+ channel agonist Bay K 8644 produce a synergistic stimulation of the GTPase activity in rat frontal cortical membranes. J. Neurochem. 64:1995;2034-2042.
6. Kenakin T. The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol. Rev. 48:1996;413-463.
7. o protein stoichiometry Mol. Pharmacol. 54:1998;899-906.
8. Leff P., Scaramellini C., Law C., McKechnie K. A three-state receptor model of agonist action. Trends Pharmacol. Sci. 18:1997;355-362.
9. Leff P. The two-state model of receptor activation. Trends Pharmacol. Sci. 16:1995;89-97.
10. Spengler D., Waeber C., Pantaloni C., Holsboer F., Bockaert J., Seeburg P.H., Journot L. Differential signal transduction by five splice variants of the PACAP receptor. Nature. 365:1993;170-175.
11. Robb S., Cheek T.R., Hannan F.L., Hall L.M., Midgley J.M., Evans P.D. Agonist-specific coupling of a clonal Drosophila octopamine/tyramine receptor to multiple second messenger systems. EMBO J. 13:1994;1325-1330.
12. 1 receptor. Biochem. Pharmacol. 56:1998;1287-1293.
13. i/oα fusion proteins. Biochemistry. 38:1999;2272-2278.
14. 6-cyclopentyladenosine in vivo: haemodynamic vs. antilipolytic responses in rats. Br. J. Pharmacol. 124:1998;607-618.
15. Furchgott RF. The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. In: Harper NJ, Simmonds AB, editors. Advances in drug research, vol. 3. New York: Academic Press, 1966. p. 21-55.
16. Furchgott R.F., Bursztyn P. Comparison of dissociation constants and of relative efficacies of selected agonists acting on parasympathetic receptors. Ann. N. Y. Acad. Sci. 144:1967;882-899.
17. 1 adenosine receptor reserve in guinea-pig atrium. Br. J. Pharmacol. 123:1998;1425-1433.
18. 1 adenosine receptors. J. Med. Chem. 37:1994;2704-2712.
19. 1 antagonist as a 'receptor knock-down' tool. Bioorg. Med. Chem. Lett. 11:2001;815-818.
20. 35S ]thio)triphosphate binding Mol. Pharmacol. 44:1993;115-123.
21. Peterson G.L. A simplification of the protein assay method of Lowry et al. which is more generally applicable. Anal. Biochem. 83:1977;346-356.
22. 1 adenosine receptor with receptor/G protein complexes in rat brain membranes. Mol. Pharmacol. 49:1996;915-926.
23. De Lean A., Hancock A.A., Lefkowitz R.J. Validation and statistical analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. Mol. Pharmacol. 21:1982;5-16.
24. 1 adenosine receptors in rat brain membranes. J. Biol. Chem. 263:1988;17522-17526.
25. Böhm M., Gräbel C., Kirchmayr R., Lensche H., Erdmann E., Gierschik P. C-terminal modifications of pertussis toxin-sensitive G protein α-subunits differentially affect immunoreactivity. Biochem. Pharmacol. 46:1993;2145-2154.
26. 1 adenosine receptors stably expressed in Chinese hamster ovary cells. Mol. Pharmacol. 53:1998;886-893.
27. 2D-adrenergic receptor regulated G protein activation in PC 12 cell membranes. Pharmacology. 52:1996;252-262.
28. 35S ]GTPγS binding Eur. J. Pharmacol. 320:1997;267-275.
29. 1A receptors as a function of receptor: G protein stoichiometry. Neuropharmacology. 36:1997;451-459.
30. 1 adenosine receptor. Mol. Pharmacol. 50:1996;196-205.
31. 1 MF-2 cells. Br. J. Pharmacol. 130:2000;1156-1164.
32. 35S ]GTPγS and cAMP functional assays Eur. J. Pharmacol. 411:2001;211-221.
33. 35S ]thio)-triphosphate binding and antibody study Mol. Pharmacol. 55:1999;564-574.
34. 1 adenosine receptor/G protein coupling: identification of a membrane protein that stabilizes the association of the receptor/G protein complex. Mol. Pharmacol. 48:1995;806-817.
35. 1 adenosine receptor - partial purification of a protein which stabilizes the receptor-G protein association. Neuropharmacology. 36:1997;1211-1219.
36. 1A receptor agonists in recombinant cell lines. Modulation of apparent efficacy by G protein activation state Naunyn-Schmiedeberg's Arch. Pharmacol. 356:1997;551-561.
37. 1A receptors: intrinsic activity and modulation by G protein activation state. Naunyn-Schmiedeberg's Arch. Pharmacol. 357:1998;490-499.
38. Selley D.E., Sim L.J., Xiao R., Liu Q., Childers S.R. μ-Opioid receptor-stimulated guanosine-5′-O-(γ-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist efficacy. Mol. Pharmacol. 51:1997;87-96.
39. 35S ]GTPγS binding to rat cerebellar membranes correlates with agonist-induced decreases in GDP affinity J. Biol. Chem. 273:1998;16865-16873.
40. Yeung S.-M.H., Green R.D. Agonist and antagonist affinities for inhibitory adenosine receptors are reciprocally affected by 5′-guanylylimidodiphosphate or N-ethylmaleimide. J. Biol. Chem. 258:1984;2334-2339.
41. Green R.D. Reciprocal modulation of agonist and antagonist binding to inhibitory adenosine receptors by 5′-guanylylimidodiphosphate and monovalent cations. J. Neurosci. 4:1984;2472-2476.
42. 1 adenosine receptors. Mol. Pharmacol. 38:1990;72-83.