Pharmacological basis for functional selectivity of partial muscarinic receptor agonists

European Journal of Pharmacology

Volumn 297, Issue 3, 1996, Pages 283-291

  Heldman, Eliahu ^a   Barg, Jacob ^b   Fisher, Abraham ^a   Levy, Rivka ^b   Pittel, Zipora ^a   Zimlichman, Reuven ^c   Kushnir, Moshe ^d   Vogel, Zvi ^b  

^a ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCH   (Israel)

^b WEIZMANN INSTITUTE OF SCIENCE   (Israel)

^c WOLFSON MEDICAL CENTER   (Israel)

^d KAPLAN HOSPITAL   (Israel)

Author keywords

Acetylcholine; Adenylate cyclase; Muscarinic receptor; Selectivity; Spare receptor

Indexed keywords

ACETYLETHYLCHOLINE MUSTARD; ADENYLATE CYCLASE; ATROPINE; CARBACHOL; COMPLEMENTARY DNA; METHYLSCOPOLAMINE; MUSCARINIC AGENT; MUSCARINIC M1 RECEPTOR; MUSCARINIC M3 RECEPTOR; MUSCARINIC RECEPTOR; OXOTREMORINE; PARTIAL AGONIST; PHOSPHATIDYLINOSITIDE; RADIOLIGAND; RECEPTOR RESERVE; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG; [4 [(3 CHLOROPHENYL)CARBAMOYLOXY] 2 BUTYNYL]TRIMETHYLAMMONIUM;

ALKYLATION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL LINE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG SELECTIVITY; ENZYME ACTIVITY; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; HYDROLYSIS; NONHUMAN; PHOSPHOINOSITIDE METABOLISM; PRIORITY JOURNAL; RECEPTOR DOWN REGULATION; SIGNAL TRANSDUCTION;

EID: 0030040987     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/0014-2999(95)00745-8     Document Type: Article

References (36)

1. Berridge, M.J., 1983, Rapid accumulation of inositol triphosphate reveals that agonists hydrolyze polyphosphoinositides instead of phosphatidylinositol, Biochem J. 258, 849.
2. Bond, R.A., P. Leff, T.D. Johnson, C.A. Milano, H.A. Rockman, T.R. McMinn and R.J. Lefkowitz, 1995, Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor, Nature 374, 272.
3. Bonner, T.I., N.J. Buckley, A.C. Young and M.R. Brann, 1987, Identification of a family of muscarinic acetylcholine receptor genes, Science 237, 527.
4. Buckley, N.J., T.I. Bonner, C.M. Buckley and M.R. Brann, 1989, Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells, Mol. Pharmacol. 35, 469.
5. Dorje, F., J. Wess, G. Lambrecht, R. Tacke, E. Mutschler and M.R. Brann, 1991, Antagonist binding profile of five cloned human muscarinic receptor subtypes, J. Pharmacol. Exp. Ther. 256, 727.
6. Eglen, R.M. and R.L. Whiting, 1990, Heterogeneity of vascular muscarinic receptors, J. Auton. Pharmacol. 10, 233.
7. 1 muscarinic acetylcholine receptor stimulates adenylate cyclase via phosphatidylinositol hydrolysis, J. Biol. Chem. 264, 20356.
8. 1 agonist attenuates cognitive dysfunctions in AF64A-treated rats, Neurosci. Lett. 102, 325.
9. 1 selective cholinergic agonist, attenuates cognitive dysfunctions in an animal model of Alzheimer's disease, J. Pharmacol. Exp. Ther. 257, 392.
10. 1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease, Bioorganic Med. Chem. Lett. 2, 839.
11. Fisher, A., Y. Karton, E. Heldman, D. Gurwitz, R. Haring, H. Medhulam, R. Brandeis, Z. Pittel, Y. Segall, D. Marciano, I. Markovitch, Z. Samocha, E. Shirin, M. Sapir, B. Green, G. Shoham and D. Barak, 1993a, Progress in medicinal chemistry of novel selective muscarinic agonists, Drug Design Discovery 9, 221.
12. 1 muscarinic agonists, Ann. NY Acad. Sci. 695, 300.
13. Freedman, S.B., G.R. Dawson, L.L. Iversen, R. Baker and R.J. Hargreaves, 1993, The design of novel muscarinic partial agonists that have functional profile in vivo, Life Sci. 52, 489.
14. Furchgott, R.F., 1966, 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, ed. N.J. Harper and A.B. Simmonds (Academic Press, London and New York) Vol. 3, p. 21.
15. Gray, J.A., A. Enz and R. Spiegel, 1989, Muscarinic agonists for senile dementia: past experience and future trends, Trends Pharmacol. Sci. Suppl., 85.
16. 1 receptor by several muscarinic ligands, Eur. J. Pharmacol. 267, 21.
17. 3 muscarinic receptors, Br. J. Pharmacol. 107, 494.
18. Heldman, E., J. Barg, R. Levy, A. Fisher, I. Ginzburg and Z. Vogel, 1993, Both receptor reserve and conformational adaptability determine signal selectivity in subtypes of muscarinic acetylcholine receptors. Am. Soc. Neurosci. 19, 10.
19. Hoyer, D. and H.W. Boddeke, 1993, Partial agonists, full agonists, antagonists: dilemmas of definition, Trends Pharmcol. Sci. 14, 270.
20. 1 muscarinic receptors, Mol. Pharmacol. 38, 895.
21. 3 muscarinic receptors expressed in chinese hamster ovary cells, J. Pharmacol. Exp. Ther. 257, 938.
22. James, S.R., C. Vaziri, T.R. Walker, G. Milligan and C.P. Downes, 1994, The turkey erythrocyte beta-adrenergic receptor couples to both adenylate cyclase and phospholipase C via distinct G-protein alpha subunits, Biochem J. 304, 359.
23. Johnson, R.A. and Y. Salomon, 1991, Assay of adenylyl cyclase catalytic activity, in: Methods in Enzymology, ed. R. A. Johnson and J.D. Corbin (Academic Press, New York) Vol. 195, p. 3.
24. Kubo, T., K. Fukuda, A. Mikami, A. Maeda, H. Takahashi, M. Mishina, T. Haga, K. Haga, A. Ichiyama, K. Kanawaga, M. Kojima, H. Matsuo, T. Hirose and S. Numa, 1986, Cloning, sequencing and expression of complementary DNA encoding themuscarinic acetylcholine receptor, Nature 323, 411.
25. Leff, P., I.G. Dougall and D. Harper, 1993, Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model-fitting approach, Br. J. Pharmacol. 110, 239.
26. Maloteaux, J.M. and E. Hermans, 1994, Agonist induced muscarinic cholinergic receptor internalization, recycling and degradation in cultured neuronal cells. Cellular mechanisms and role in desensitization, Biochem. Pharmacol. 47, 77.
27. McKinney, M. and J.T. Coyle, 1991, The potential for muscarinic receptor subtype-specific pharmacotherapy for Alzheimer's disease, Mayo Clin. Proc. 66, 1225.
28. Nah, S.-Y., B. Attali and Z. Vogel, 1993, Heterologous desensitization and reduced G protein ADP-ribosylation following exposure to α2-adrenoceptor and muscarinic receptor agonists, Eur. J. Pharmacol. 244, 67.
29. Olianas, M.C. and P. Onali, 1991, Muscarinic stimulation of adenylate cyclase activity of rat olfactory bulb. II. Characterization of the antagonist sensitivity and comparison with muscarinic inhibitors of the enzyme in striatum and heart, J. Pharmacol. Exp. Ther. 259, 680.
30. Pittel, Z., E. Heldman, R. Rubinstein and S. Cohen, 1990, Distinct muscarinic receptor subtypes differentially modulate acetylcholine release from corticocerebral synaptosomes, J. Neurochem. 55, 665.
31. Schwarz, R.D., R.E. Davis, J.C. Jean, C.J. Spencer, H. Tecle and A.J. Thoma, 1993, Characterization of muscarinic agonists in recombinant cell lines, Life Sci. 52, 465.
32. 1 receptor, J. Med. Chem. 35, 15.
33. Spalding, T.A., N.J.M. Birdsall, C.A.M. Curtis and E.C. Hulme, 1994, Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors, J. Biol. Chem. 269, 4092.
34. Vogel, Z., J. Barg, R. Levy, D. Saya, E. Heldman and R. Mechoulam, 1993, Anandamide, a brain endogenous compound, interact specifically with cannabinoid receptors and inhibits adenylate cyclase, J. Neurochem. 61, 352.
35. Wang, S.Z. and E.E. El Fakahany, 1993, Application of transfected cell lines in studies of functional receptor subtype selectivity of muscarinic agonists, J. Pharmacol. Exp. Ther. 266, 237.
36. Whitehouse, P.J., 1993, Cholinergic therapy in dementia, Acta Neurol. Scand. Suppl. 149, 42.