Interaction of full and partial agonists of the A1 adenosine receptor with receptor/G protein complexes in rat brain membranes

Molecular Pharmacology

Volumn 49, Issue 5, 1996, Pages 915-926

  Lorenzen, Anna ^b   Guerra, Laura ^a   Vogt, Heidrun ^b   Schwabe, Ulrich ^b  

^a UNIVERSITY OF FERRARA   (Italy)

^b UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 ANILINOADENOSINE; 2 CHLORO 6 N CYCLOPENTYLADENOSINE; 3 [(3 CHOLAMIDOPROPYL)DIMETHYLAMMONIO] 1 PROPANESULFONIC ACID; 5' METHYLTHIOADENOSINE; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; 8 CYCLOPENTYLTHEOPHYLLINE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A1 RECEPTOR; ADENOSINE A1 RECEPTOR AGONIST; CLADRIBINE; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); GUANOSINE DERIVATIVE; RECEPTOR PROTEIN; THEOPHYLLINE;

ANIMAL CELL; ARTICLE; BRAIN MEMBRANE; CONTROLLED STUDY; DOSE RESPONSE; DRUG RECEPTOR BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; RAT; RECEPTOR OCCUPANCY; SECOND MESSENGER;

ANIMALS; BINDING, COMPETITIVE; BRAIN; CELL MEMBRANE; GTP-BINDING PROTEINS; RATS; RECEPTORS, PURINERGIC P1; SIGNAL TRANSDUCTION; THERMODYNAMICS;

EID: 0029915945     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (50)

1. Jasper, J. R., and P. A. Insel. Evolving concepts of partial agonism: the β-adrenoceptor as a paradigm. Biochem. Pharmacol. 43:119-130 (1992).
2. Hoyer, D., and H, W. G. M. Boddeke. Partial agonists, full agonists, antagonists: dilemmas of definition Trends Pharmacol. Sci. 14:270-275 (1993).
3. Feuerstein, T. J., W. Sauermann, C. Allgaier, and E. A. Singer. New insights into receptor theory, as provided by an artificial partial agonist made-to-measure. Naunyn-Schmiedeberg's Arch. Pharmacol. 350:1-9 (1994).
4. Keen, M. Testing models of agonism for G protein-coupled receptors. Trends Pharmacol. Sci. 12:371-374 (1991).
5. 1A receptor. Biochemistry 33:4283-4290 (1994).
6. 2-adrenoceptor. Mol. Pharmacol. 48:316-325 (1995).
7. Weiland, G. A., K. A. Minneman, and P. B. Molinoff. Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. Nature (Lond.) 281:114-117 (1979)
8. Contreras, M. L., B. B. Wolfe, and P. A. Molinoff. Thermodynamic properties of agonist interactions with the beta adrenergic receptor-coupled adenylate cyclase system. I. High- and low-affinity states of agonist binding to membrane-bound beta adrenergic receptors. J. Pharmacol. Exp. Ther. 237:154-164 (1986).
9. Raffa, R. B., and F. Porreca. Thermodynamic analysis of drug-receptor interaction. Life Sci. 44:245-258 (1989).
10. Miklavc, A., D. Kocjan, J. Mavri, J. Koller, and D. Hadzi. On the fundamental difference in the thermodynamics of agonist and antagonist interactions with β-adrenergic receptors and the mechanism of entropy-driven binding. Biochem. Pharmacol. 40:663-669 (1990).
11. 1 adenosine receptor. J. Biol. Chem. 264:13157-13164 (1989).
12. 2-adrenoceptor. Nature (Lond.) 374:272-276 (1995).
13. Van Calker, D., M. Müller, and B. Hamprecht. Adenosine inhibits the accumulation of cyclic AMP in cultured brain cells Nature (Lond.) 276: 839-841 (1978).
14. Cooper, D. M. F., C. Londos, and M. Rodbell. Adenosine receptor-mediated inhibition of rat cerebral cortical adenylate cyclase by a GTP-dependent process. Mol. Pharmacol. 18:598-601 (1980).
15. Trussell, L. O., and M. B. Jackson. Dependence of an adenosine-activated potassium current on a GTP-binding protein in mammalian central neurons. J. Neurosci. 7:3306-3316 (1987).
16. Dolphin, A. C., S. R. Forda, and R. H. Scott. Calcium-dependent currents in cultured rat dorsal root ganglion neurones are inhibited by an adenosine analogue. J. Physiol. 373:47-61 (1986).
17. 1 receptors. Biochem. J. 255:69-77 (1988).
18. 1 receptor ligands. Eur. J. Pharmacol. 267:55-61 (1994).
19. 1 receptor binding in brain tissue. Mol. Pharmacol. 22:250-257 (1982).
20. i adenosine receptors in brain membranes: analysis of guanine nucleotide and temperature effects on radioligand binding. Mol. Pharmacol. 26:1-9 (1984).
21. 1 adenosine receptor ligands. Mol. Neuropharmacol. 2:273-281 (1992).
22. 35S]thio)-triphosphate binding. Mol. Pharmacol. 44:115-123 (1993).
23. Dunwiddie, T. V., and B. B. Fredholm. Adenosine modulation of synaptic responses in rat hippocampus: possible role of inhibition or activation of adenylate cyclase. Adv. Cyclic Nucleotide Protein Phosphorylation Res. 19:259-272 (1985).
24. o. J. Biol. Chem. 266:22285-22289 (1991).
25. Peterson, G. L. A simplification of the protein assay method of Lowry et al. which is more generally applicable. Anal. Biochem. 83:346-356 (1977).
26. De Lean, A., A. A. Hancock, and R. J. Lefkowitz. Validation and statistical analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. Mol. Pharmacol. 21:5-16 (1982).
27. 3H]adenosine from bovine cerebral cortex. J. Neurochem. 60:745-751 (1993).
28. 2a receptors. J. Pharmacol. Exp. Ther. 272:511-518 (1995).
29. 6-(ω-aminoalkyl)adenosines on adenosine receptor affinity and intrinsic activity. Eur. J. Pharmacol. 172: 185-193 (1989).
30. Fraser, C. M. Site-directed mutagenesis of β-adrenergic receptors. J. Biol. Chem. 264:9266-9270 (1989).
31. 2-adrenergic receptor impairs agonist activation of adenylyl cyclase without affecting high affinity agonist binding. J. Biol. Chem. 265:1388-1393 (1990).
32. 2-adenosine receptors coupled to adenylate cyclase. Biochem. Pharmacol. 43:1089-1093 (1992).
33. Munshi, R., A. S. Clanachan, and H. P. Baer. 5′-Deoxy-5′-methylthioadenosine: a nucleoside which differentiates between adenosine receptor types. Biochem. Pharmacol. 37:2085-2089 (1988).
34. 2b adenosine receptor in NIH 3T3 fibroblasts. Biochem. Pharmacol. 47:801-814 (1994).
35. 3H]NECA binding sites by gel nitration. Naunyn-Schmiedeberg's Arch. Pharmacol. 337:64-68 (1988).
36. 3 adenosine receptor. Mol. Pharmacol. 45:1101-1111 (1994).
37. Siddiqi, S. M., K. A. Jacobson, J. L. Esker, M. E. Olah, X.-D. Ji, N. Melman, K. N. Tiwari, J. A. Secrist III, S. W. Schneller, G. Cristalli, G. L. Stiles, C. R. Johnson, and A. P. Ijzerman. Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors. J. Med. Chem. 38:1174-1188 (1995).
38. Maksay, G. Thermodynamics of γ-aminobutyric acid type A receptor binding differentiate agonists from antagonists. Mol. Pharmacol. 46:386-390 (1994).
39. 2 receptors: antimuscarinics of the pridinol, sila-pridinol, dipbenidol and siladiphenidol type. Br. J. Pharmacol. 109:360-370 (1993).
40. 1 receptors. Biochim. Biophys. Acta 1267:145-151 (1995).
41. Kilpatrick, G. J., N. el Tayar, H. van de Waterbeemd, P. Jenner, B. Testa, and C. D. Marsden. The thermodynamics of agonist and antagonist binding to dopamine D-2 receptors. Mol. Pharmacol. 30:226-234 (1986).
42. Testa, B., P. Jenner, G. J. Kilpatrick, N. el Tayar, H. van de Waterbeemd, and C. D Marsden. Do thermodynamic studies provide information on both the binding to and the activation of dopaminergic and other receptors? Biochem. Pharmacol. 36:4041-4046 (1987).
43. Hitzemann, B. Thermodynamic aspects of drug-receptor interactions. Trends Pharmacol. Sci. 9:408-411 (1988).
44. Gilli, P., V. Ferretti, G. Gilli, and P. A. Borea. Enthalpy-entropy-compensation in drug-receptor binding. J. Phys. Chem. 98:1515-1518 (1994).
45. Gies, J.-P., B. Ilien, and Y. Landry. Muscarinic acetylcholine receptor: thermodynamic analysis of the interaction of agonists and antagonists. Biochim. Biophys. Acta 889:103-115 (1986).
46. Tota, M. R., and M. I. Schimerlik. Partial agonist effects on the interaction between the atrial muscarinic receptor and the inhibitory guanine nucleotide-binding protein in a reconstituted system. Mol. Pharmacol. 37:996-1004 (1986).
47. Prather, P. L., H. H. Loh, and P. Y. Law. Interaction of δ-opioid receptors with multiple G proteins: a nonrelationship between agonist potency to inhibit adenylyl cyclase and to activate G proteins. Mol. Pharmacol. 45: 997-1003 (1994).
48. Ferguson, K. M., T. Higashijima, M. D. Smigel, and A. G. Gilman. The influence of bound GDP on the kinetics of guanine nucleotide binding to G proteins. J. Biol. Chem. 261:7393-7399 (1986).
49. 3H]GDP release from rat and hamster adipocyte membranes independently linked to receptors involved in activation or inhibition of adenylate cyclase. J. Biol. Chem. 259:761-769 (1984).
50. Kühl, P. W. Excess-substrate inhibition in enzymology and high-dose inhibition in pharmacology, a re-interpretation. Biochem. J. 298:171-180 (1994).