Persistent activation by and receptor reserve for an irreversible A1- adenosine receptor agonist in DDT1 MF-2 cells and in guinea pig heart

Molecular Pharmacology

Volumn 52, Issue 3, 1997, Pages 491-498

  Zhang, Jiahui ^a   Belardinelli, Luiz ^a,b   Jacobson, Kenneth A ^c   Otero, Deborah H ^a   Baker, Stephen P ^a,b  

^a UNIVERSITY OF FLORIDA   (United States)

^b UNIVERSITY OF FLORIDA COLLEGE OF MEDICINE   (United States)

^c NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 N CYCLOPENTYLADENOSINE; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; 8 CYCLOPENTYLTHEOPHYLLINE; ADENOSINE A1 RECEPTOR AGONIST; ADENOSINE DERIVATIVE; ADENOSINE RECEPTOR BLOCKING AGENT; CYCLIC AMP; RADIOLIGAND; RECEPTOR RESERVE;

ACYLATION; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING KINETICS; CONTROLLED STUDY; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG RESPONSE; GUINEA PIG; HEART ATRIOVENTRICULAR NODE; HEART CONDUCTION; ISOLATED HEART; NONHUMAN; PRIORITY JOURNAL; RECEPTOR OCCUPANCY;

EID: 0030845719     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.52.3.491     Document Type: Article

References (38)

1. 2 receptors: structure-function relationships. Med. Res. Rev. 12:423-471 (1992).
2. Collis, M. G., and S. M. O. Hourani. Adenosine receptor subtypes. Trends Pharmacol. Sci. 14:360-366 (1993).
3. 3 receptors: pharmacological properties, species differences and receptor functions. Trends Pharmacol. Sci. 15:298-306 (1994).
4. Belardinelli, L., J. C. Shryock, S. D. Wang, and M. Srinivas. Ionic basis of the electrophysiological actions of adenosine on cardiomyocytes. FASEB J. 9:369-365 (1995).
5. 3 adenosine receptor. Proc. Natl. Acad. Sci. USA 89:7432-7436 (1992).
6. 3 receptors in rat brain. Mol. Pharmacol. 48:1038-1045 (1995).
7. Jacobson, K. A., P. J. M. van Galen, and M. Williams. Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential. J. Med. Chem. 35:407-422 (1992).
8. 3 adenosine receptor. Mol. Pharmacol. 45:1101-1111 (1994).
9. Baker, S. P., and M. D. Deyrup. Development of novel irreversible ligands. Neuroprotocols 4:66-75 (1994).
10. Jasper, J. R., H. J. Motulsky, and P. A. Insel. Characterization of a bromoacetylated derivative of pindolol as a high affinity, irreversible beta adrenergic antagonist in cultured cells. J. Pharmacol. Exp. Ther. 244:820-824 (1988).
11. 1-adenosine receptors in guinea pig atrioventricular node. Am. J. Physiol. 262:H661-H671 (1992).
12. 1-adrenergic receptors revealed by chlorethylclonidine. Mol. Pharmacol. 32:505-510 (1987).
13. Salles, J., M. A. Wallace, and J. N. Fain. Differential effects of alkylating agents on the multiple muscarinic receptor subtypes linked to activation of phospholipase C by carbachol in rat brain cortical membranes. J. Pharmacol. Exp. Ther. 264:521-529 (1993).
14. Hunter, D. D., and N. M. Nathanson. Biochemical and physical analyses of newly synthesized muscarinic acetylcholine receptors in cultured embryonic chicken cardiac cells. J. Neurosci. 6:3739-3748 (1986).
15. Mahan, L. C., R. M. McKernan, and P. A. Insel. Metabolism of alpha-and beta-adrenergic receptors in vitro and in vivo. Annu. Rev. Pharmacol. Toxicol. 27:215-235 (1987).
16. 2-adrenergic receptor. Biochemistry 27:1813-1817 (1988).
17. Curtis, C. A. M., M. Wheatley, S. Bansal, N. J. M. Birdsall, P. Eveleigh, E. K. Pedder, D. Poyner, and E. C. Hulme. Propylbenzilycholine mustard labels an acidic residue in transmembrane helix 3 of the muscarinic receptor. J. Biol. Chem. 264:489-495 (1989).
18. 1 adenosine receptors. J. Med. Chem. 32:1043-1051 (1989).
19. Standifer, K. A., J. Pitha, and S. P. Baker. Carbostyril-based beta-adrenergic agonists: evidence for long lasting or apparent irreversible receptor binding and activation of adenylate cyclase in vitro. Naunyn-Schmiedebergs Arch. Pharmacol. 339:129-137 (1989).
20. 1MF-2 cells. J. Pharmacol. Exp. Ther. 275:1167-1176 (1995).
21. Bradford, M. M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein dye binding. Anal. Biochem. 72:248-254 (1976)
22. 1 adenosine receptors. J. Med. Chem. 37:2704-2712 (1994)
23. Jenkins, J. R., and L. Belardinelli. Atrioventricular nodal accommodation in isolated guinea pig hearts: physiological significance and role of adenosine. Circ. Res. 63:97-116 (1988).
24. Rosenthal, H. E. A graphic method for the determination and presentation of binding parameters in a complex system. Anal. Biochem. 20:525-532 (1967).
25. 1 MF-2 cells. Mol. Pharmacol. 40:639-647 (1991).
26. Williams, M., M. Abreu, M. F. Jarvis, and L. Noronha-Blob. Characterization of adenosine receptors in the PC12 pheochromocytoma cell line using radioligand binding: evidence for A-2 selectivity. J. Neurochem. 48:498-502 (1987).
27. 2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol. Pharmacol. 41:352-359 (1992).
28. 1-selective adenosine agonist preconditions rabbit heart. Can. J. Cardiol. 12:517-521 (1996).
29. 1 adenosine receptors: persistent activation reveals spare receptors. Mol. Pharmacol. 30:403-409 (1986).
30. 2 adenosine receptors by photoaffinity labeling. Mol. Pharmacol. 39:517-523 (1991).
31. 2 adenosine receptors. Naunyn-Schmiedebergs Arch. Pharmacol. 347:521-526 (1993)
32. Stephenson, R. P. A modification of receptor theory. Br. J. Pharmacol. 11:379-393 (1956).
33. Kenakin, T. P. The classification of drugs and drug receptors in isolated tissues. Pharmacol. Rev. 36:165-222 (1984).
34. Kenakin, T. P. Receptor reserve as a tissue misnomer. Trends Pharmacol. Sci. 7:93-95 (1986).
35. 1 MF-2 cells. Br. J. Pharmacol. 106:215-221 (1992).
36. Brown, J. H., and D. Goldstein. Differences in muscarinic receptor reserve for inhibition of adenylate cyclase and stimulation of phosphoinositide hydrolysis in chick heart cells. Mol. Pharmacol. 30:566-570 (1986).
37. KAdo in guinea pig atria. Circulation 94 (Suppl. I):I-47-I-48 (1996).
38. Furchgott, R. F. The use of haloalkylamines in the differentiation of receptors and the determination of dissociation constants of receptor-agonist complexes. Adv. Drug Res. 3:21-55 (1966).