Pharmacological evaluation of the long-term effects of xanomeline on the M1 muscarinic acetylcholine receptor

PLoS ONE

Volumn 5, Issue 12, 2010, Pages

  Grant, Marianne K O ^a   Noetzel, Meredith J ^a   De Lorme, Kayla C ^a   Jakubík, Jan ^b   Doležal, Vladimír ^b   El Fakahany, Esam E ^a  

^a UNIVERSITY OF MINNESOTA MEDICAL SCHOOL   (United States)

^b INSTITUTE OF PHYSIOLOGY   (Czech Republic)

Author keywords

[No Author keywords available]

Indexed keywords

CARBACHOL; MUSCARINIC M1 RECEPTOR; XANOMELINE; ATROPINE; MUSCARINIC AGENT; PYRIDINE DERIVATIVE; THIADIAZOLE DERIVATIVE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BINDING SITE; DRUG HYDROLYSIS; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SCREENING; INCUBATION TIME; LIGAND BINDING; LONG TERM CARE; NONHUMAN; PROTEIN EXPRESSION; ANIMAL; BINDING SITE; CHEMISTRY; CHO CELL; CRICETULUS; DOSE RESPONSE; DOWN REGULATION; HAMSTER; HUMAN; HYDROLYSIS; METABOLISM; PROTEIN BINDING;

ANIMALS; ATROPINE; BINDING SITES; CARBACHOL; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOWN-REGULATION; HUMANS; HYDROLYSIS; MUSCARINIC AGONISTS; PROTEIN BINDING; PYRIDINES; RECEPTOR, MUSCARINIC M1; THIADIAZOLES;

EID: 78650842922     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0015722     Document Type: Article

References (31)

1. Hulme EC, Birdsall NJ, Buckley NJ (1990) Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 30: 633-673.
2. Caulfield MP (1993) Muscarinic receptors - Characterization, coupling and function. Pharmacol Ther 58: 319-379.
3. Wess J (1993) Mutational analysis of muscarinic acetylcholine receptors: structural basis of ligand/receptor/G protein interactions. Life Sci 53: 1447-1463.
4. Lu ZL, Saldanha JW, Hulme EC (2002) Seven-transmembrane receptors: crystals clarify. Trends Pharmacol Sci 23: 140-146.
5. Shannon HE, Bymaster FP, Calligaro DO, Greenwood B, Mitch CH, et al. (1994) Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors. J Pharmacol Exp Ther 269: 271-281.
6. Bymaster FP, Carter PA, Peters SC, Zhang W, Ward JS, et al. (1998) Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects. Brain Res 795: 179-190.
7. Bymaster FP, Whitesitt CA, Shannon HE, DeLapp N, Ward JS, et al. (1997) Xanomeline: A selective muscarinic agonist for the treatment of Alzheimer's disease. Drug Dev Res 40: 158-170.
8. Shekhar A, Potter WZ, Lightfoot J, Lienemann J, Dubé S, et al. (2008) Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry 165: 1033-1039.
9. Christopoulos A, El-Fakahany EE (1997) Novel persistent activation of muscarinic M1 receptors by xanomeline. Eur J Pharmacol 334: R3-R4.
10. Christopoulos A, Pierce TL, Sorman JL, El-Fakahany EE (1998) On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor. Mol Pharmacol 53: 1120-1130.
11. Christopoulos A, Parsons AM, El-Fakahany EE (1999) Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor. J Pharmacol Exp Ther 289: 1220-1228.
12. Jakubik J, Tucek S, El-Fakahany EE (2002) Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor. J Pharmacol Exp Ther 301: 1033-1041.
13. De Lorme KC, Sikorski KL, Grant MK, El-Fakahany EE (2006) Long-term wash-resistant effects of brief interaction of xanomeline at the M1 muscarinic receptor. Neurosci Lett 410: 11-14.
14. De Lorme KC, Grant MK, Noetzel MJ, Polson SB, El-Fakahany EE (2007) Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex. J Pharmacol Exp Ther 323: 868-876.
15. El-Fakahany EE, Cioffi CL (1990) Molecular mechanisms of regulation of neuronal muscarinic receptor sensitivity. Membr Biochem 9: 9-27.
16. Kelly E, Bailey CP, Henderson G (2008) Agonist-selective mechanisms of GPCR desensitization. Br J Pharmacol 153: S379-S388.
17. Jakubik J, Tucek S, El-Fakahany EE (2004) Role of receptor protein and membrane lipids in xanomeline wash-resistant binding to muscarinic M1 receptors. J Pharmacol Exp Ther 308: 105-110.
18. Bradford MM (1976) 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.
19. Feigenbaum P, El-Fakahany EE (1985) Regulation of muscarinic cholinergic receptor density in neuroblastoma cells by brief exposure to agonist: possible involvement in desensitization of receptor function. Journal of Pharmacology and Experimental Therapeutics 233: 134-140.
20. Jakubik J, El-Fakahany EE, Dolezal V (2006) Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) muscarinic acetylcholine receptors. Mol Pharmacol 70: 656-666.
21. Zhu SZ, Wang SZ, Hu J, el-Fakahany EE (1994) An arginine residue conserved in most G protein-coupled receptors is essential for the function of the m1 muscarinic receptor. Mol Pharmacol 45: 517-523.
22. Hu J, Wang SZ, el-Fakahany EE (1991) Effects of agonist efficacy on desensitization of phosphoinositide hydrolysis mediated by m1 and m3 muscarinic receptors expressed in Chinese hamster ovary cells. J Pharmacol Exp Ther 257: 938-945.
23. Lefkowitz RJ (1993) G protein-coupled receptor kinases. Cell 74: 409-412.
24. Ferguson SS (2001) Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling. Pharmacol Rev 53: 1-24.
25. Wang SZ, el-Fakahany EE (1993) Application of transfected cell lines in studies of functional receptor subtype selectivity of muscarinic agonists. J Pharmacol Exp Ther 266: 237-243.
26. Wood MD, Murkitt KL, Ho M, Watson JM, Brown F, et al. (1999) Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry. Br J Pharmacol 126: 1620-1624.
27. Ehlert FJ (1985) The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium. Mol Pharmacol 28: 410-421.
28. Furchgott R (1966) The use of beta-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Advances in Drug Research, In: Harper N, Simmonds A, eds. New York: Academic Press. pp 21-55.
29. Davis CN, Bradley SR, Schiffer HH, Friberg M, Koch K, et al. (2009) Differential regulation of muscarinic M1 receptors by orthosteric and allosteric ligands. BMC Pharmacol 9: 14.
30. Spalding TA, Burstein ES, Brauner-Osborne H, Hill-Eubanks D, Brann MR (1995) Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis. J Pharmacol Exp Ther 275: 1274-1279.
31. Ford DJ, Essex A, Spalding TA, Burstein ES, Ellis J (2002) Homologous Mutations Near the Junction of the Sixth Transmembrane Domain and the Third Extracellular Loop Lead to Constitutive Activity and Enhanced Agonist Affinity at all Muscarinic Receptor Subtypes. J Pharmacol Exp Ther 300: 810-817.