G protein coupling and signaling pathway activation by M1 muscarinic acetylcholine receptor orthosteric and allosteric agonists

Journal of Pharmacology and Experimental Therapeutics

Volumn 327, Issue 2, 2008, Pages 365-374

  Thomas, Rachel L ^a   Mistry, Rajendra ^a   Langmead, Christopher J ^b   Wood, Martyn D ^b   Challiss, R A John ^a  

^a UNIVERSITY OF LEICESTER   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 (4 BUTYL 1 PIPERIDINYL)PROPYL] 3,4 DIHYDRO 2(1H) QUINOLINONE; 4 N BUTYL 1 [4 (2 METHYLPHENYL) 4 OXO 1 BUTYL]PIPERIDINE; 77 LH 28 1; AC 42; ARECOLINE; CYCLIC AMP; FORSKOLIN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); INOSITOL PHOSPHATE; MUSCARINIC M1 RECEPTOR; MUSCARINIC M1 RECEPTOR AGONIST; OXOTREMORINE; PILOCARPINE; SULFUR 35; TRITIUM; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHO CELL; CONCENTRATION RESPONSE; CONFOCAL MICROSCOPY; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; IMMUNOPRECIPITATION; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; GTP-BINDING PROTEIN ALPHA SUBUNITS, GI-GO; GTP-BINDING PROTEIN ALPHA SUBUNITS, GQ-G11; GTP-BINDING PROTEIN ALPHA SUBUNITS, GS; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; INOSITOL 1,4,5-TRISPHOSPHATE; MUSCARINIC AGONISTS; N-METHYLSCOPOLAMINE; PIPERIDINES; QUINOLONES; RECEPTOR, MUSCARINIC M1; SIGNAL TRANSDUCTION;

EID: 54349106685     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.108.141788     Document Type: Article

References (38)

1. i/o activation profiles in CHO cells expressing human muscarinic acetylcholine receptors: dependence on agonist as well as receptor-subtype. Br J Pharmacol 132:950-958.
2. 2+, diacylglycerol, and protein kinase C signaling using fluorescent biosensors. J Biol Chem 280:21837- 21846.
3. Berg KA, Maayani S, Goldfarb J, Scaramellini C, Leff P, and Clarke WP (1998) Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus. Mol Pharmacol 54:94-104.
4. Birdsall NJ and Lazareno S (2005) Allosterism at muscarinic receptors: ligands and mechanisms. Mini Rev Med Chem 5:523-543.
5. Bonhaus DW, Chang LK, Kwan J, and Martin GR (1998) Dual activation and inhibition of adenylyl cyclase by cannabinoid receptor agonists: evidence for agonist-specific trafficking of intracellular responses. J Pharmacol Exp Ther 287:884-888.
6. Bonner TI, Buckley NJM, Young AC, and Brann MR (1987) Identification of a family of muscarinic acetylcholine receptor genes. Science 237:527-532.
7. sα and is not a consequence of phosphoinositidase C activation. Biochem J 315:883-888.
8. sα proteins. Br J Pharmacol 126:1221-1229.
9. Caulfield MP and Birdsall NJ (1998) International Union of Pharmacology: XVII. Classification of muscarinic acetylcholine receptors. Pharmacol Rev 50:279-290.
10. Challiss RA, Batty IH, and Nahorski SR (1988) Mass measurements of inositol 1,4,5-trisphosphate in rat cerebral cortex slices using a radioreceptor assay: effects of neurotransmitters and depolarization. Biochem Biophys Res Commun 157:684-691.
11. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
12. Cooper DM, Mons N, and Karpen JW (1995) Adenylyl cyclases and the interaction between calcium and cAMP signalling. Nature 374:421-424.
13. Delmas P and Brown DA (2005) Pathways modulating neural KCNQ/M (Kv7) potassium channels. Nat Rev Neurosci 6:850-862.
14. Felder CC, Kanterman RY, Ma AL, and Axelrod J (1989) A transfected m1 muscarinic acetylcholine receptor stimulates adenylate cyclase via phosphatidylinositol hydrolysis. J Biol Chem 264:20356-20362.
15. Friedman E, Butkerait P, and Wang HY (1993) Analysis of receptor-stimulated and basal guanine nucleotide binding to membrane G proteins by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Anal Biochem 214:171-178.
16. Gregory KJ, Sexton PM, and Christopoulos A (2007) Allosteric modulation of muscarinic acetylcholine receptors. Curr Neuropharmacol 5:157-167.
17. q-deficient mice. J Neurosci 20:3973-3979.
18. Hilf G, Gierschik P, and Jakobs KH (1989) Muscarinic acetylcholine receptorstimulated binding of guanosine 5′-O-(3-thiotriphosphate) to guanine-nucleotide-binding proteins in cardiac membranes. Eur J Biochem 186:725-731.
19. s in the transfected Chinese hamster ovary cells. Mol Pharmacol 48:392-400.
20. Hulme EC, Lu ZL, and Bee MS (2003) Scanning mutagenesis studies of the M1 muscarinic acetylcholine receptor. Receptors Channels 9:215-228.
21. Kenakin T (2003) Ligand-selective receptor conformations revisited: the promise and the problem. Trends Pharmacol Sci 24:346-354.
22. 1 muscarinic receptor agonist, 77-LH-28-1. Br J Pharmacol 154:1104-1115.
23. 1 receptor: direct pharmacological evidence that AC-42 is an allosteric agonist. Mol Pharmacol 69:236-246.
24. 35S]-GTPγS binding mediated by human muscarinic m1-m4 receptors: antagonist studies. Br J Pharmacol 109:1120-1127.
25. + channels. J Physiol 553:789-802.
26. 2 muscarinic acetylcholine receptors. Mol Pharmacol 72:463-476.
27. Migeon JC and Nathanson NM (1994) Differential regulation of cAMP-mediated gene transcription by m1 and m4 muscarinic acetylcholine receptors: preferential coupling of m4 receptors to Gi alpha-2. J Biol Chem 269:9767-9773.
28. s proteins. Br J Pharmacol 144: 566-575.
29. 2+ and inositol 1,4,5-trisphosphate oscillation frequency: receptor density versus agonist concentration. J Biol Chem 277:35947-35960.
30. q/11. Mol Pharmacol 45:890-898.
31. q/11 protein coupling in membranes prepared from post mortem human brain tissue. J Pharmacol Exp Ther 325:869-874.
32. 1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation. Mol Pharmacol 70:1974-1983.
33. 1 muscarinic receptor. Mol Pharmacol 61:1297-1302.
34. Spengler D, Waeber C, Pantaloni C, Holsboer F, Bockaert J, Seeburg PH, and Journot L (1993) Differential signal transduction by five splice variants of the PACAP receptor. Nature 365:170-175.
35. 2 concentration monitored in living cells. Curr Biol 8:343-346.
36. Urban JD, Clarke WP, von Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA, Roth BL, Christopoulos A, Sexton PM, et al. (2007) Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther 320:1-13.
37. Violin JD and Lefkowitz RJ (2007) β-Arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci 28:416-422.
38. 2+ signalling in human neuroblastoma cells. Br J Pharmacol 114:1133-1142.