Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins

Molecular Pharmacology

Volumn 51, Issue 2, 1997, Pages 312-319

  Burstein, E S ^a   Spalding, T A ^a,b   Brann, M R ^a,b  

^a UNIVERSITY OF VERMONT   (United States)

^b ACADIA PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 DIPHENYLACETOXY 1 METHYLPIPERIDINE; ARECOLINE; ATROPINE; CARBACHOL; GUANINE NUCLEOTIDE BINDING PROTEIN; METHYLSCOPOLAMINE; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; MUSCARINIC M3 RECEPTOR; MUSCARINIC M5 RECEPTOR; MUSCARINIC RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; PARTIAL AGONIST; PILOCARPINE; PIRENZEPINE; QUINUCLIDINYL BENZILATE; RECEPTOR SUBTYPE; TRIHEXYPHENIDYL;

ALLOSTERISM; ANIMAL CELL; ARTICLE; CELL STRAIN 3T3; CELL STRAIN COS1; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; GENE OVEREXPRESSION; MOUSE; NONHUMAN; PRIORITY JOURNAL;

EID: 0031037633     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.51.2.312     Document Type: Article

References (40)

1. Lefkowitz, R. J., S. Cotecchia, P. Samama, and T. Costa. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol. Sci. 14:303-307 (1993).
2. Leff P. The two state model of receptor activation. Trends Pharmacol. Sci. 16:89-97 (1995)
3. Chidiac, P., T. E. Hebert, M. Valiquette, M. Dennis, and M. Bouvier. Inverse agonist activity of beta-adrenergic antagonists. Mol. Pharmacol. 45:490-499 (1994).
4. Hilf, G., and K. H. Jakobs. Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes. Eur. J. Pharmacol. 225:245-252 (1992).
5. Costa, T., and A. Herz. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86:7321-7325 (1989).
6. Tian, W., E. Duzic, S. M. Lanier, and R. C. Deth. Determinants of α2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G-protein state. Mol. Pharmacol. 45:524-531 (1994).
7. Barker, E. L., R. S. Westphal, D. Schmidt, and E. Sanders-Bush. Constitutively active 5-hydroxytryptamine 2C receptors reveal novel inverse agonist activity of receptor ligands. J. Biol. Chem. 269:11687-11690 (1994).
8. Leeb-Lundberg, L. M., S. A. Mathis, and M. C. S. Herzig. Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells. J. Biol. Chem. 269:25970-25973 (1994).
9. Jakubik, J., L. Bacakova, E. E. El-Fakahany, and S. Tucek. Constitutive activity of the M1-M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists. FEBS Lett. 377:275-279 (1995).
10. Samama, P., S. Cotecchia, T. Costa, and R. J. Lefkowitz. A mutation-induced activated state of the beta2-adrenergic receptor. J. Biol. Chem. 268:4625-4636 (1993).
11. Spalding, T. A., E. S. Burstein, H. B. Jørgensen, D. Hill-Eubanks, and M. R. Brann. Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis. J. Pharmacol. Exp. Ther. 275:1274-1279 (1995).
12. Burstein, E. S., T. A. Spalding, H. Bräuner-Osborne, and M. R. Brann. Constitutive activation of muscarinic receptors by the G protein Gq. FEBS Lett. 363:261-263 (1995).
13. M. Soejima, and A. Noma. Mode of regulation of the ACh-sensitive K-channel by the muscarinic receptor in rabbit atrial cells. Pfluegers Arch. Eur. J. Physiol. 400:424-431 (1984).
14. Burgisser, E., A. DeLean, and R. J. Lefkowitz. Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide. Proc. Natl. Acad. Sci. USA 79:1732-1736 (1982).
15. Mitchell, F. M., N. J. Buckley, and G. Milligan. Enhanced degradation of the phosphoinositidase C-linked guanine-nucleotide-binding protein Gαq/ Gall following activation of the human m1 muscarinic acetylcholine receptor expressed in CHO cells. Biochem. J. 293:495-499 (1993).
16. Levis M. J., and H. R. Bourne. Activation of the α subunit of Gs in intact cells alters its abundance, rate of degradation and membrane avidity. J. Cell. Biol. 119:1297-1307 (1992).
17. Liang, B. T., M. R. Hellmich, E. J. Neer, and J. B. Galper. Development of muscarinic cholinergic inhibition of adenylate cyclase in embryonic chick heart. J. Biol. Chem. 261:9011-9021 (1986).
18. Hadcock, J. R., M. Ros, D. C. Watkins, and C. C. Malbon. Cross-regulation between G-protein mediated pathways: stimulation of adenylyl cyclase increases expression of the inhibitory G-protein Gi2. J. Biol. Chem. 265: 14784-14790 (1990).
19. Burstein, E. S., H. Bräuner-Osborne, T. A. Spalding, B. R. Conklin, and M. R. Brann. Interactions of muscarinic receptors with the heterotrimeric G-proteins Gq and G12: transduction of proliferative signals. J. Neurochem., in press.
20. Burstein, E. S., T. A. Spalding, and M. R. Brann. Amino acid side chains that define muscarinic receptor/G-protein coupling. J. Biol. Chem. 271: 2882-2885 (1996).
21. Conklin, B. R., O. Chabre, Y. -H. Wong, A. D. Federman, and H. R. Bourne. Recombinant Gaq. Mutational activation and coupling to receptors and phospholipase C. J. Biol. Chem. 267:31-34 (1992).
22. Bräuner-Osborne, H., B. Ebert, M. R. Brann, E. Falch, and P. Krogsgaard-Larsen. Annulated heterocyclic bioisosteres of norarecoline: synthesis and molecular pharmacology at five human muscarinic acetylcholine receptors. J. Med. Chem 38:2188-2195 (1995).
23. Bräuner-Osborne, H., and M. R. Brann. Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): high throughput assays in mammalian cells. Eur. J. Pharmacol. 295:93-102 (1996).
24. Hulme, E. C., N. J. M. Birdsall, and N. J. Buckley. Muscarinic receptor subtypes. Anna. Rev. Pharmacol. Toxicol. 30:633-673 (1990).
25. Amatruda, T. T., III, S. Dragas-Graonic, R. Holmes, and H. D. Perez. Signal transduction by the formyl peptide receptor. J. Biol. Chem. 270: 28010-28013 (1995).
26. Furchgott, R. F. The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. In Advances in Drug Research (N. J. Harper and A. B. Simmonds, eds.). Vol. 3, Academic Press, New York, 21-55 (1966).
27. Kenakin, T. Agonist-receptor efficacy. I. Mechanisms of efficacy and receptor promiscuity. Trends. Pharmacol. Sci. 16:188-192 (1995).
28. Hulme, E. C., C. P. Berrie, N. J. M. Birdsall, and A. S. V. Burgen. Two populations of binding sites for muscarinic antagonists in the rat heart. Eur. J. Pharmacol. 73:137-142 (1981).
29. Milano, C. A., L. F. Allen, H. A. Rockman, P. C. Dolber, T. R. McMinn, K. R. Chien, T. D. Johnson, R. A. Bond, and R. J. Lefkowitz. Enhanced myocardial function in transgenic mice overexpressing the β2-adrenergic receptor. Science (Washington D. C.) 264:582-585 (1994).
30. Ehlert, F. J. Inverse agonists, cooperativity and drug action at benzodiazepine receptors. Trends Pharmacol. Sci. 7:28-32 (1986).
31. Dorje, F., A. I. Levey, and M. R. Brann. Immunological detection of muscarinic receptor subtype proteins (m1-m5) in rabbit peripheral tissues. Mol. Pharmacol. 40:459-462 (1991).
32. Bräuner-Osborne, H., B. Ebert, M. R. Brann, E. Falch, and P. Krogsgaard-Larson. Functional partial agonism at human muscarinic receptors. Eur. J. Pharmacol. (in press).
33. Parma, J., L. Duprez, J. VanSande, P. Cochaux, C. Gervy, J. Mockel, J. Dumont, and G. Vassart. Somatic mutations in the thyrotropin receptor gene cause hyperfunctioning thyroid adenomas. Nature (Lond.) 365:649-654 (1993).
34. Shenker, A., L. Laue, S. Kosugi, J. J. Merendino, T. Minegishi, and G. B. Cutler. A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature (Lond.) 365:652-654 (1993).
35. Rim, J., and D. Oprian. Constitutive activation of opsin: interaction of mutants with rhodopsin kinase and arrestin. Biochemistry 34:11938-11945 (1995).
36. Julius, D., T. J. Livelli, T. M. Jessell, and R. Axel. Ectopic expression of the serotonin 1c receptor and the triggering of malignant transformation. Science (Washington D. C.) 244:1057-1062 (1989).
37. Gutkind, J. S., E. A. Novotny, M. R. Brann, and K. C. Robbins. Muscarinic acetylcholine receptor subtypes as agonist-dependent oncogenes. Proc. Natl. Acad. Sci. USA 88:A103-4707 (1991).
38. Allen, L. F., R. J. Lefkowitz, M. G. Caron, and S. Cotecchia. G-protein coupled receptors as protooncogenes: constitutively activating mutation of the α1B adrenergic receptor enhances mitogenesis and tumorigenicity. Proc. Natl. Acad. Sci. USA 88:11354-11358 (1991).
39. Brann, M. R., and L. V. Cohen. Diurnal expression of transducin mRNA and translocation of transducin in rods of rat retina. Science (Washington D. C.) 235:585-587 (1987).
40. 50) of an enzymatic reaction. Biochem. Pharmacol. 22:3099-3108 (1973).