Effects of positive allosteric modulators on single-cell oscillatory Ca2+ signaling initiated by the type 5 metabotropic glutamate receptor

Molecular Pharmacology

Volumn 76, Issue 6, 2009, Pages 1302-1313

  Bradley, Sophie J ^a   Watson, Jeannette M ^b   Challiss, R A John ^a  

^a UNIVERSITY OF LEICESTER   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

(4 FLUOROPHENYL)[3 [3 (4 FLUOROPHENYL) [1,2,4]OXADIAZOL 5 YL]PIPERIDINL 1 YL]METHANONE; 3 CYANO N (1,3 DIPHENYL 1H PRAZOL 5 YL)BENZAMIDE; 3,3' DIFLUOROBENZALDAZINE; ADX 47273; CALCIUM ION; GLUTAMIC ACID; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR AGONIST; N [4 CHLORO 2 [(1,3 DIOXO 1,3 DIHYDRO 2H ISOINDOL 2 YL)METHYL]PHENYL]2 HYDROXYBENZAMIDE; PROTEIN KINASE C; QUISQUALIC ACID; RECOMBINANT PROTEIN; UNCLASSIFIED DRUG;

ALLOSTERISM; AMPLITUDE MODULATION; ANIMAL CELL; ARTICLE; ASTROCYTE; CALCIUM SIGNALING; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOSOL; ENZYME ACTIVITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEPHOSPHORYLATION; PROTEIN PHOSPHORYLATION; RAT;

ALLOSTERIC REGULATION; ANIMALS; BENZAMIDES; CALCIUM COMPOUNDS; CALCIUM SIGNALING; CEREBRAL CORTEX; CHO CELLS; CRICETINAE; CRICETULUS; GLUTAMIC ACID; HYDRAZINES; OXADIAZOLES; OXIDES; PHTHALIMIDES; PIPERIDINES; PYRAZOLES; RATS; RATS, WISTAR; RECEPTORS, METABOTROPIC GLUTAMATE;

EID: 73149087939     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.109.059170     Document Type: Article

References (40)

1. Agulhon C, Petravicz J, McMullen AB, Sweger EJ, Minton SK, Taves SR, Casper KB, Fiacco TA, and McCarthy KD (2008) What is the role of astrocyte calcium in neurophysiology? Neuron 59:932-946.
2. 2+ signaling. Mol Pharmacol 69: 174-184.
3. Berridge MJ, Lipp P, and Bootman MD (2000) The versatility and universality of calcium signalling. Nat Rev Mol Cell Biol 1:11-21.
4. Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, and Conn PJ (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol Pharmacol 71:1389-1398.
5. Chen Y, Goudet C, Pin JP, and Conn PJ (2008) N-{4-Chloro-2-[(1,3- dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol 73:909-918.
6. Conn PJ and Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol 37:205-237.
7. Conn PJ, Lindsley CW, and Jones CK (2009) Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol Sci 30:25-31.
8. D'Ascenzo M, Fellin T, Terunuma M, Revilla-Sanchez R, Meaney DF, Auberson YP, Moss SJ, and Haydon PG (2007) mGluR5 stimulates gliotransmission in the nucleus accumbens. Proc Natl Acad Sci U S A 104:1995-2000.
9. 2+ oscillations. Science 279:227-230.
10. Dolmetsch RE, Xu K, and Lewis RS (1998) Calcium oscillations increase the efficiency and specificity of gene expression. Nature 392:933-936.
11. Ferraguti F and Shigemoto R (2006) Metabotropic glutamate receptors. Cell Tissue Res 326:483-504.
12. Flint AC, Dammerman RS, and Kriegstein AR (1999) Endogenous activation of metabotropic glutamate receptors in neocortical development causes neuronal calcium oscillations. Proc Natl Acad Sci U S A 96:12144-12199.
13. Gasparini F, Kuhn R, and Pin JP (2002) Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol 2:43-49.
14. Herman MA and Jahr CE (2007) Extracellular glutamate concentration in hippocampal slice. J Neurosci 27:9736-9741.
15. Hermans E and Challiss RA (2001) Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-proteincoupled receptors. Biochem J 359:465-484.
16. 2+ signalling in an inducible cell expression system. J Neurochem 70:1772-1775.
17. Jean YY, Lercher LD, and Dreyfus CF (2008) Glutamate elicits release of BDNF from basal forebrain astrocytes in a process dependent on metabotropic receptors and the PLC pathway. Neuron Glia Biol 4:35-42.
18. Kawabata S, Tsutsumi R, Kohara A, Yamaguchi T, Nakanishi S, and Okada M (1996) Control of calcium oscillations by phosphorylation of metabotropic glutamate receptors. Nature 383:89-92.
19. Kew JN (2004) Positive and negative allosteric modulation of metabotropic glutamate receptors: emerging therapeutic potential. Pharmacol Ther 104:233-244.
20. 2+ oscillations. J Biol Chem 280:25409- 25415.
21. Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, et al. (2005) A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther 313:199-206.
22. 2+ release. J Biol Chem 283:14072-14083.
23. Le Poul E, Bessis AS, Lutjens R, Bonnet B, Rocher JP, Epping-Jordan M, and Mutel V (2005) In vitro pharmacological characterisation of selective mGluR5 allosteric modulators (Abstract). Neuropharmacology 49:252.
24. Lindsley CW, Shipe WD, Wolkenberg SE, Theberge CR, Williams DL Jr., Sur C, and Kinney GG (2006) Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia. Curr Top Med Chem 6:771-785.
25. Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, et al. (2008) ADX47273 [S-(4-fluoro- phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl} -methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities. J Pharmacol Exp Ther 327:827-839.
26. Malherbe P, Kratochwil N, Zenner MT, Piussi J, Diener C, Kratzeisen C, Fischer C, and Porter RH (2003) Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Mol Pharmacol 64:823-832.
27. Mannaioni G, Marino MJ, Valenti O, Traynelis SF, and Conn PJ (2001) Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function. J Neurosci 21:5925-5934.
28. Mühlemann A, Ward NA, Kratochwil N, Diener C, Fischer C, Stucki A, Jaeschke G, Malherbe P, and Porter RH (2006) Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′- difluorobenzaldazine on rat mGlu5 receptors. Eur J Pharmacol 529:95-104.
29. Nakahara K, Okada M, and Nakanishi S (1997) The metabotropic glutamate receptor mGluR5 induces calcium oscillations in cultured astrocytes via protein kinase C phosphorylation. J Neurochem 69:1467-1475.
30. Nash MS, Young KW, Challiss RA, and Nahorski SR (2001) Intracellular signaling. Receptor-specific messenger oscillations. Nature 413:381-382.
31. 2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration. J Biol Chem 277:35947-35960.
32. O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, et al. (2003) A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol 64:731-740.
33. O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, et al. (2004) A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther 309:568-577.
34. Pagano A, Ruegg D, Litschig S, Stoehr N, Stierlin C, Heinrich M, Floersheim P, Prezèau L, Carroll F, Pin JP, et al. (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxy-iminocyclopropan[b]chromen-1acarboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors. J Biol Chem 275:33750-33758.
35. Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, and Conn PJ (2005) A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol Pharmacol 68:1793-1802.
36. 2+ oscillation. EMBO J 22:3825-3832.
37. 2+-dependent PKC. J Biol Chem 279:2254-2261.
38. 2+-sensing receptor require negative feedback by protein kinase C. J Biol Chem 277:46871-46876.
39. Zhang Y, Rodriguez AL, and Conn PJ (2005) Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J Pharmacol Exp Ther 315:1212-1219.
40. Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, et al. (2007) Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg Med Chem Lett 17:1386-1391.