The muscarinic M5 receptor: A silent or emerging subtype?

British Journal of Pharmacology

Volumn 130, Issue 1, 2000, Pages 13-21

  Eglen, R M ^a,c   Nahorski, S R ^b  

^a ROCHE BIOSCIENCE   (United States)

^b UNIVERSITY OF LEICESTER   (United Kingdom)

^c LJL BioSystems   (United States)

Author keywords

Ciliary iris muscle; Dopaminergic transmission; Phosphoinositide hydrolysis; Receptor channelling; Salivary gland

Indexed keywords

11 [[4 [4 (DIETHYLAMINO)BUTYL] 1 PIPERIDYL]ACETYL] 5,11 DIHYDRO 6H PYRIDO[2,3 B][1,4]BENZODIAZEPIN 6 ONE; 3,6A,11,14 TETRAHYDRO 9 METHOXY 2 METHYL 12H ISOQUINO[1,2 B]PYRROLO[3,2 F][1,3]BENZOXAZINE 1 CARBOXYLIC ACID ETHYL ESTER; ATROPINE; DARIFENACIN; HIMBACINE; METHOCTRAMINE; MUSCARINIC AGENT; MUSCARINIC M5 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; OXYBUTYNIN; PIRENZEPINE; SECOVERINE; TOLTERODINE; TRIPITRAMINE; UNCLASSIFIED DRUG; ZAMIFENACIN;

ANIMAL CELL; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; RECEPTOR GENE; REVIEW; SIGNAL TRANSDUCTION;

EID: 0034017317     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703276     Document Type: Review

References (86)

1. 35S]GTPγS and Gα specific immunoprecipitation. Br. J. Pharmacol., 125, 24P.
2. 3 antagonists for clinical use. Life Sci., 60, 1053-1060.
3. ALLAOUA, H., CHAUDIEU, I., ALONSO, R. & QUIRION, R.P. & BOKSA, P. (1993). Muscarinic potentiation of excitatory amino-acid evoked dopamine release in mesencephalic cells: specificity for the NMDA response and role of intracellular messengers. Synapse, 15, 39-47.
4. 2+ signalling. J. Physiol., 499, 291-306.
5. 11 and phospholipase C-β1. J. Biol. Chem., 267, 8081-8088.
6. 4 subtype mediates the contraction of the rabbit iris sphincter. Naunyn Schmeideberg's Arch. Pharmacol., 345, 611-618.
7. 2 muscarinic receptors on the iris sphincter muscle differ from those on iris noradrenergic nerves. Eur. J. Pharmacol., 163, 263-274.
8. 5 muscarinic acetylcholine receptor genes. Neuron, 1, 403-410.
9. 5): high throughput assays in mammalian cells. Eur. J. Pharmacol., 295, 93-102.
10. BUCKLEY, N.J., BONNER, T.I., BUCKLEY, C.M. & BRANN, M.R. (1989). Antagonist binding properties of five cloned muscarinic receptors expressed in Chinese hamster ovary cells. Mol. Pharmacol., 35, 469-476.
11. 1 receptor-stimulated adenylate cyclase activity in Chinese hamster ovary cells is mediated by Gsalpha and is not a consequence of phosphoinositidase C activation. Biochem. J., 315, 883-888.
12. 3 muscarinic receptor subtypes to inositol 1,4,5 trisphosphate and adenosine 3′, 5′-cyclic monophosphate accumulation in Chinese hamster ovary cells. J. Pharm. Exp. Ther., 274, 134-142.
13. BURSTEIN, E.S., SPALDING, T.A. & BRANN, M.R. (1997). Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol. Pharmacol., 51, 312-319.
14. 5 muscarinic receptor. Biochemestry, 37, 4052-4058.
15. 5 muscarinic receptor is the switch which enables G-protein coupling. J. Biol. Chem., 273, 24322-24327.
16. BURSTEIN, E.S., SPALDING, T.A., HILL-EUBANKS, D. & BRANN, M.R. (1995). Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins. J. Biol. Chem., 270, 3141-3146.
17. CAULFIELD, M.P. (1993). Muscarinic receptors - characterisation, coupling and function. Pharmac. Ther., 58, 319-379.
18. CAULFIELD, M.P. & BIRDSALL, N.J.M. (1998). International Union of Pharmacology XVII. Classification of muscarinic acetylcholine receptors. Pharmacol. Rev., 50, 279-290.
19. CHOPPIN, A. & EGLEN, R.M. (2000). Pharmacological characterisation of muscarinic receptors in feline and human isolated ciliary smooth muscle. Br. J. Pharmacol (in press).
20. CHOPPIN, A., EGLEN, R.M. & HEGDE, S.S. (1998). Pharmacological characterisation of muscarinic receptors in rabbit isolated iris sphincter and urinary bladder smooth muscle. Br. J. Pharmacol., 124, 883-888.
21. CHOPPIN, A., STEPPAN, G.J., LOURY, D.N., WATSON, N. & EGLEN, R.M. (1999a). Characterisation of the muscarinic receptor in isolated uterus of sham operated and ovariectomized rats. Br. J. Pharmacol., 127, 1551-1558.
22. 5 receptor characterization. Br. J. Pharmacol. 128, 33P.
23. CHOPPIN, A., HEGDE, S.S. & EGLEN, R.M. (1999c). Pharmacological characterization of muscarinic receptors in dog ciliary smooth muscle. Br. J. Pharmacol., 126, 93P.
24. 35S] guanosine-5′-o-(3-thio)triphosphate binding mediated by cholinergic muscarinic receptors in membranes from Chinese hamster ovary cells and rat striatum using an anti-G protein scintillation proximity assay. J. Pharmacol. Exp. Ther., 289, 946-955.
25. DORJE, F., WESS, J., LAMBRECHT, G., TACKE, R., MUTSCHLER, E. & BRANN, M.R. (1991). Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J. Pharmacol. Exp. Ther., 256, 727-733.
26. EGLEN, R.M. & HEGDE, S.S. (1998). Selective modulation of muscarinic receptor subtypes: therapeutic potential. Emerging Drugs. 3, 67-79.
27. EGLEN, R.M., HEGDE, S.S. & WATSON, N. (1996). Muscarinic receptor subtypes and smooth muscle function. Pharmacol. Revs., 48, 531-565.
28. EGLEN, R.M. & WHITING, R.L. (1990). Heterogeneity of vascular muscarinic receptors. J. Auton. Pharmacol., 19, 187-200.
29. FELDER, C.C. (1995). Muscarinic acetylcholine receptors: signal transduction through multiple effectors. FASEB J., 9, 619-625.
30. FERRARO-DILEO, G. & FLYNN, D.D. (1995). Characterization of muscarinic receptors on cultured microglia cells. Life Sci., 56, 1037 (abstract).
31. FLYNN, D.D., FERARI-DILEO, G., MASH, D.C. & LEVEY, A.I. (1995). Differential regulation of molecular subtypes of muscarinic receptors in Alzheimer's disease. J. Neurochem., 64, 1888-1891.
32. FLYNN, D.D., REEVER, C.M., & FERRARI-DILEO, G. (1997). Pharmacological strategies to selectively label and localize receptor subtypes. Drug Devel. Res., 40, 104-116.
33. GIL, D.W., KRAUSS, H.A., BOGARDUS, A.M. & WOLDEMUSSIE, E. (1997). Muscarinic receptor subtypes in human iris-ciliary body measurement by immunoprecipitation. Inv. Opthalmol. Vis. Sci., 38, 1434-1442.
34. GUDERMAN, T., KALKBRENNER, F. & CHULTZ, G. (1996). Diversity and selectivity of receptor G-protein interaction. Am. Rev. Pharmacol. Toxicol., 36, 429-459.
35. 1 receptor by several muscarinic ligands. Eur. J. Pharmacol., 267, 21-31.
36. GUSOVSKY, F., LEUDERS, J., KOHN, E.C. & FELDER, C.C. (1993). Muscarinic receptor-mediated tyrosine phosphorylation of phospholipase C-γ. An alternative mechanism for cholinergic-induced phosphomositide breakdown. J. Biol. Chem., 268, 7768-7772.
37. HAMMER, R., BERRIE, C.P., BIRDSALL, N.J.M., BURGEN, A.S.V. & HULME, E.C. (1980). Pirenzepine distinguishes between subclasses of muscarinic receptor. Nature, 283, 90-92.
38. 3 muscarinic receptors in the urinary bladder of rats in vitro and in viro. Br. J. Pharmacol., 120, 1409-1418.
39. HELDMAN, E., BARG, J., FISCHER, A., LEVY, R., PATEL, Z., ZIMLICHMAN, R., KUSHNERE, M. & VOGEL, Z. (1996). Pharmacological basis for functional selectivity of partial muscarinic receptor agonists. Eur. J. Pharmacol., 297, 283-291.
40. JONES, S.V.P., HEILMAN, C.J. & BRANN, M.R. (1991). Functional responses of cloned muscarinic receptors expressed in CHO-KI cells. Mol. Pharmacol., 40, 242-247.
41. KENAKIN, T.P. (1996). The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol. Rev., 48, 413-463.
42. KENAKIN, T.P. (1997). Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry. Trends Pharm Sci., 18, 456-464.
43. 2. J. Biol. Chem., 271, 17476-17484.
44. 5, expressed in SF9 cells using the baculovirus expression system. J. Pharm. Exp. Ther., 279, 593-601.
45. 2 receptor selective antagonist. Life Sci., 64, 535-539.
46. LEFKOWTTZ, R.J. (1998). G-protein coupled receptors III, new roles for receptor kinases and β-arrestins in receptor signalling and desensitisation. J. Biol. Chem., 273, 18677-18680.
47. LEVEY, A.J., KITT, C.A., SIMONS, W.F., PRICE, D.L. & BRANN, M. (1991). Identification and localisation of muscarinic acetylcholine receptor proteins in brain with subtype-specific antibodies. J. Neurosci., 11, 3218-3226.
48. 5 muscarinic acetylcholine receptor as seen in murine L-cells. J. Biol. Chem., 265, 11273-11284.
49. LIAO, C.F., THEMMEN, A.P., BARBERIS, J.R., BIRNBAUMER, M. & BIRNBAUMER, L. (1989). Molecular cloning and expression of a fifth muscarinic acetylcholine receptor. J. Biol. Chem., 264, 7328-7337.
50. 5 cholinoceptors. Life Sci., 64, 6 (abstract).
51. MCINTYRE, R. & QUINN, P. (1995). Characterisation and comparison of muscarinic receptors in the dog ciliary muscle with ileum. Br. J. Pharmacol., 115, 139P.
52. MCRITCHIE, B., MERNER, P.A. & DODD, M.G. (1993). In vivo selectivity of the novel muscarinic antagonist, zamifenacin in the conscious dog. Br. J. Pharmacol., 109, 38P.
53. MELOY, T.D., DANIELS, D.V., HEGDE, S.S., EGLEN, R.M. & FORD, A.P.D.W. (1998). Functional characterization of muscarinic cholinoceptors in rat submaxilliary gland (RSG) using microphysiometry. FASEB J., 12, Proc. Exp. Biol., San Francisco, May.
54. MITA, Y., DOBASHI, K., SUZUKI, K., MORI, M. & NAKAZAWA, T. (1996). Induction of muscarinic receptor subtypes in monocytic: macrophagic cells differentiated from EoL-1 cells. Eur. J. Pharmacol., 297, 121-127.
55. NEUBIG, R.R. (1994). Membrane organisation in G-protein mechanisms. FASEB. J., 8, 939-946.
56. NEUBIG, R.R. (1998). Specificity of receptor-G-protein coupling: protein structure and cellular determinants. Seminars in Neuroscience, 9, 189-197.
57. NILVEBRANDT, L. & SPARF, B. (1988). Receptor binding profiles of some selective muscarinic antagonists. Eur. J. Pharmacol., 151, 83-96.
58. 11. Mol. Pharmacol., 45, 890-898.
59. 2+ entry and dissociated from tyrosine phosphorylation of phospholipase C-γ I is involved in inositol phosphate production by activated G-protein coupled receptors in myometrium. J. Pharmacol. Exp. Ther., 289, 1022-1030.
60. PARNAS, D., HELDMAN, E., BRANCFE, L., EINESTEIN, N. & LINEAL, M. (1998). Expression and localisation of muscarinic receptors in P19-derived neurones. J. Mol. Neurosci., 10, 17-29.
61. PHILLIPS, J.K., VIDOVIC, M. & HILL, C.E. (1997). Variation in mRNA expression of α adrenergic, neurokinin and muscarinic receptors amongst four arteries of the rat. J. Auton. Nerv. Syst., 62, 85-93.
62. 5 receptors. Mol. Pharmacol., 45, 61-64.
63. 5 receptor subtype: fact or fiction? Life Sci., 60, 1105-1112.
64. RICHARDS, M.H. & VAN GIERSBERGAN, P.L.M. (1995). Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists. Br. J. Pharmacol., 114, 1241-1249.
65. SCHWARZ, R.D., DAVIS, R.E., JAEN, J.C., SPENCER. C.J., TEELE, H. & THOMAS, A.J. (1993). Characterization of muscarinic agonists in recombinant cell lines. Life Sci., 52, 465-472.
66. SPALDING, T.A., BURSTEIN, E.S., HENDERSON, S.C., DUCOTE, K.R., BRANN, M.R. (1998). Identification of a ligand dependent switch within a muscarinic receptor. J. Biol. Chem., 273, 21563-21568.
67. TOBIN, A.B. (1997). Phosphorylation of phospholipase C-coupled receptors. Pharmacol. Ther., 75, 135-151.
68. 5 subtypes: effect of G-protein-coupled receptor kinases GRK2, GRK4, GRK5, GRK6, J. Pharmacol. Exp. Ther., 284, 1218-1226.
69. UMEMORI, H., INOUE, T., KUME, S., SEKIYAMA, N., NAGAO, M., ITOH, H., NAKANISHI, S., MIKOSHIBA, K. & YAMAMOTO, T. (1997). Activation of the G protein Gq/11 through tyrosine phosphorylation of the alpha subunit. Science, 276, 1878-1881.
70. 5) of muscarinic receptors. J. Neurochem., 62, 1345-1351.
71. 5 muscarinic receptor subtypes in rat forebrain. Dev. Brain Res., 66, 181-185.
72. WALLIS, R.M. & NAPIER, C.M. (1999). Muscarinic antagonists in development for disorders of smooth muscle function. Life Sci., 64, 387-394.
73. WANG, S.Z. & EL FAKAHANY, E.E. (1993). Application of tansfected cell lines in studies of functional receptor subtype selectivity of muscarinic agonist. J. Pharmacol. Exp. Ther., 266, 237-243.
74. 5 muscarinic receptors to activation of neuronal nitric oxide synthase. Pharmacology, 53, 271-280.
75. 5 muscarinic acetylcholine receptors to activation of nitric oxide synthase. J. Pharmacol. Exp. Ther., 268, 552-557.
76. WATSON, G.E. & CULP, D.J. (1994). Muscarinic cholinergic receptor subtypes in rat sublingual glands. Am. J. Physiol., 266, C335-C342.
77. 5 muscarinic receptors expressed in CHO-KI cells. Br. J. Pharmacol., 127, 590-596.
78. 5 muscarinic receptor distribution in rat CNS by RT-PCR and HPLC. J. Neurachem., 63, 815-821.
79. WESS, J. (1997). G protein coupled receptors: molecular mechanisms involved in receptor activation and selectivity of G protein recognition. FASEB, J., 11, 346-354.
80. 5 receptors. Mol. Pharmacol., 41, 369-374.
81. WOLDEMUSSIE, E., FELDMANN, B.J. & CHEN, J. (1993). Characterization of muscarinic receptors in cultured human iris sphincter. Exp. Eye Res., 56, 385-392.
82. 5 muscarinic receptors stimulate mitogen activated protein kinase. Pharmacology, 56, 175-186.
83. YARKER, Y.E., GOA, K.L. & FITTON, A. (1995). Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in detrusor instability. Drugs Aging, 6, 243-262.
84. 5 receptors in rat brain. Mol. Pharmacol., 43, 149-157.
85. 5 receptors: genotypes and behaviour. Life Sci., 64, 68 (abstract).
86. 3 mRNA expression in cultured human ciliary muscle cells. J. Ocul. Pharmacol. Ther. 15, 153-163.