SIB-1757 and SIB-1893: Selective, noncompetitive antagonists of metabotropic glutamate receptor type 5

Journal of Pharmacology and Experimental Therapeutics

Volumn 290, Issue 1, 1999, Pages 170-181

  Varney, Mark A ^a   Cosford, Nicholas D P ^a   Jachec, Christine ^a   Rao, Sara P ^a   Sacaan, Aida ^a   Lin, Fen Fen ^a   Bleicher, Leo ^a   Santori, Emily M ^a   Flor, Peter J ^b   Allgeier, Hans ^b   Gasparini, Fabrizio ^b   Kuhn, Rainer ^b   Hess, Stephen D ^a   Veliçelebi, GÖNÜL ^a   Johnson, Edwin C ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL 6 (2 PHENYLVINYL)PYRIDINE; 3,5 DIHYDROXYPHENYLGLYCINE; 6 METHYL 2 PHENYLAZO 3 PYRIDINOL; CALCIUM; GLUTAMATE RECEPTOR; GLUTAMATE RECEPTOR ANTAGONIST; GLUTAMIC ACID; METABOTROPIC RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CALCIUM CELL LEVEL; CELL LINE; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; GENETIC RECOMBINATION; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANIMALS, NEWBORN; BINDING, COMPETITIVE; BRAIN; CALCIUM; CELLS, CULTURED; CHO CELLS; CRICETINAE; EXCITATORY AMINO ACID ANTAGONISTS; HUMANS; INOSITOL PHOSPHATES; METHOXYHYDROXYPHENYLGLYCOL; NEURONS; PHENAZOPYRIDINE; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, METABOTROPIC GLUTAMATE; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0033004276     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Aiba A, Chen C, Herrup K, Rosenmund C, Stevens CF and Tonegawa S (1994) Reduced hippocampal long-term potentiation and context-specific deficit in associative learning in mGluR1 mutant mice. Cell 79:365-375.
2. Arias HR (1998) Noncompetitive inhibition of nicotinic acetylcholine receptors by endogenous molecules. J Neurosci Res 52:369-379.
3. Baude A, Nusser Z, Roberts JD, Mulvihill E, McIlhinney RA and Somogyi P (1993) The metabotropic glutamate receptor (mGluR1 alpha) is concentrated at perisynaptic membrane of neuronal subpopulations as detected by immunogold reaction. Neuron 11:771-787.
4. Blumcke I, Behle K, Malitschek B, Kuhn R, Knöpfel T, Wolf HK and Wiestler OD (1996) Immunohistochemical distribution of metabotropic glutamate receptor subtypes mGluR1b, mGluR2/3, mGluR4a and inGluR5 in human hippocampus. Brain Res 736:217-226.
5. Bruno V, Copani A, Knöpfel T, Kuhn R, Casabona G, Dell'Albani P, Condorelli DF and Nicoletti F (1995) Activation of metabotropic glutamate receptors coupled to inositol phospholipid hydrolysis amplifies NMDA-induced neuronal degeneration in cultured cortical cells. Neuropharmacology 34:1089-1098.
6. Conn PJ and Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Anna Rev Pharmacol Toxicol 37:205-237.
7. Contractor A, Gereau RW, Green T and Heinemann SF (1998) Direct effects of metabotropic glutamate receptor compounds on native and recombinant N-methyl-D-aspartate receptors. Proc Natl Acad Sci USA 95:8969-8974.
8. Daggett LP, Johnson EC, Varney MA, Lin FF, Hess SD, Deal CR, Jachec C, Lu CC, Kerner JA, Landwehrmeyer GB, Standaert DG, Young AB, Harpold MM and Velicelebi G (1998) The human N-methyl-D-aspartate receptor 2C subunit: Genomic analysis, distribution in human brain, and functional expression. J Neurochem 71:1953-1968.
9. Daggett LP, Sacaan AI, Akong M, Rao SP, Hess SD, Liaw C, Urrutia A, Jachec C, Ellis SB, Dreessen J, Knöpfel T, Landwehrmeyer GB, Testa CM, Young AB, Varney M, Johnson EC and Velicelebi G (1995) Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5. Neuropharmacalogy 34:871-886.
10. Flor PJ, Lindauer K, Puttner I, Ruegg D, Lukic S, Knöpfel T and Kuhn R (1995a) Molecular cloning, functional expression and pharmacological characterization of the human metabotropic glutamate receptor type 2. Eur J Neurosci 7:622-629.
11. Flor PJ, Lukic S, Ruegg D, Leonhardt T, Knöpfel T and Kuhn R (1995b) Molecular cloning, functional expression and pharmacological characterization of the human metabotropic glutamate receptor type 4. Neuropharmacology 34:149-155.
12. Flor PJ, Van Der Putten H, Ruegg D, Lukic S, Leonhardt T, Bence M, Sansig G, Knöpfel T and Kuhn R (1997) A novel splice variant of a metabotropic glutamate receptor, human mGluR7b. Neuropharmacology 36:153-915.
13. Fong TM, Yu H and Strader CD (1992) Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580. J Biol Chem 267:25668-25671.
14. Hall JM, Caulfield MP, Watson SP and Guard S (1993) Receptor subtypes or species homologues: Relevance to drug discovery. Trends Pharmacol Sci 14:376-383.
15. Ikeda SR, Lovinger DM, McCool BA and Lewis DL (1995) Heterologous expression of metabotropic glutamate receptors in adult rat sympathetic neurons: Subtype-specific coupling to ion channels. Neuron 14:1029-1038.
16. + current in neurones of the rat cerebellum. J Physiol (London) 509:347-354.
17. Knöpfel T, Kuhn R and Allgeier H (1995) Metabotropic glutamate receptors: Novel targets for drug development. J Med Chem 38:1417-1426.
18. Laurie DJ, Schoeffter P, Wiederhold KH and Sommer B (1997) Cloning, distribution and functional expression of the human mGlu6 metabotropic glutamate receptor. Neuropharmacology 36:145-152.
19. Lazareno S, Farries T and Birdsall NJ (1993) Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4. Life Sci 52:449-456.
20. Leff P and Dougall IG (1993) Further concerns over Cheng-Prusoff analysis. Trends Pharmacol Sci 14:110-112.
21. Lin FF, Varney M, Sacaan AI, Jachec C, Daggett LP, Rao S, Flor P, Kuhn R, Kerner JA, Standaert D, Young AB and Velicelebi G (1997) Cloning and stable expression of the mGluR1b subtype of human metabotropic receptors and pharmacological comparison with the mGluR5a subtype. Neuropharmacology 38:917-931.
22. Litschig S, Gasparini F, Ruegg D, Stoehr N, Flor PJ, Vranesic I, Prezeau L, Pin JP, Thomsen C, Kuhn R (1999) CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol Pharmacol 55:453-461.
23. Lu YM, Jia Z, Janus C, Henderson JT, Gerlai R, Wojtowicz JM and Roder JC (1997) Mice lacking metabotropic glutamate receptor 5 show impaired learning and reduced CA1 long-term potentiation (LTP) but normal CA3 LTP. J Neurosci 17:5196-5205.
24. Martin LJ, Blackstone CD, Huganir RL and Price DL (1992) Cellular localization of a metabotropic glutamate receptor in rat brain. Neuron 9:259-270.
25. Massot O, Rousselle JC, Fillion MP, Grimaldi B, Cloez-Tayarani I, Fugelli A, Prudhomme N, Seguin L, Rousseau B, Plantefol M, Hen R and Fillion G (1996) 5-Hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5-hydroxytryptamine 1B/1D receptors. Mol Pharmacol 60:752-762.
26. Masu M, Iwakabe H, Tagawa Y, Miyoshi T, Yamashita M, Fukuda Y, Sasaki H, Hiroi K, Nakamura Y and Shigemoto R (1995) Specific deficit of the ON response in visual transmission by targeted disruption of the mGluR6 gene. Cell 80:757-765.
27. 2+ channels via multiple signal transduction pathways in HEK 293 cells. J Neurophysiol 79:379-391.
28. Petralia RS, Wang YX, Niedzielski AS and Wenthold RJ (1996) The metabotropic glutamate receptors, mGluR2 and mGluR3, show unique postsynaptic, presynaptic and glial localizations. Neuroscience 71:949-976.
29. Petralia RS, Wang YX, Singh S, Wu C, Shi L, Wei J and Wenthold RJ (1997) A monoclonal antibody shows discrete cellular and subcellular localizations of mGluR1 alpha metabotropic glutamate receptors. J Chem Neuroanat 13:77-93.
30. Pin JP and Duvoisin R (1995) The metabotropic glutamate receptors: Structure and functions. Neuropharmacology 34:1-26.
31. Romano C, Sesma MA, McDonald CT, O'Malley K, Van den Pol AN and Olney JW (1995) Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain. J Comp Neurol 355:455-469.
32. Sacaan AI, Santori EM and Rao TS (1998) (S)-4-Carboxy-3-hydroxyphenylglycine activates phosphatidyl inositol linked metabotropic glutamate receptors in different brain regions of the neonatal rat. Neurochem Int 32:77-85.
33. Saugstad JA, Segerson TP and Westbrook GL (1996) Metabotropic glutamate receptors activate G-protein-coupled inwardly rectifying potassium channels in Xenopus oocytes. J Neurosci 16:5979-5985.
34. Shigemoto R, Kinoshita A, Wada E, Nomura S, Ohishi H, Takada M, Flor PJ, Neki A, Abe T, Nakanishi S and Mizuno N (1997) Differential presynaptic localization of metabotropic glutamate receptor subtypes in the rat hippocampus. J Neurosci 17:7503-7522.
35. Shigemoto R, Nakanishi S and Mizuno N (1992) Distribution of the mRNA for a metabotropic glutamate receptor (mGluR1) in the central nervous system: An in situ hybridization study in adult and developing rat. J Comp Neurol 322: 121-135.
36. Varney MA, Lin F-F, Jachec C, Rao SP, Hess SD, Johnson EC and Veliçelebi G (1999) Stable expression of human NMDA receptors in cultures mammalian cells. Methods Mol Biol 128:42-60.
37. Varney MA, Rao SP, Jachec C, Deal C, Hess SD, Daggett LP, Lin F, Johnson EC and Velicelebi G (1998) Pharmacological characterization of the human ionotropic glutamate receptor subtype GluR3 stably expressed in mammalian cells. J Pharmacol Exp Ther 285:358-370.
38. Veliçelebi G, Stauderman KA, Varney MA, Akong M, Hess SD and Johnson EC (1998) Fluorescent techniques for measuring ion channel activity. Methods Enzymol 294:20-47.
39. Watkins J and Collingridge G (1994) Phenylglycine derivatives as antagonists of metabotropic glutamate receptors. Trends Pharmacol Sci 15:333-342.
40. Zhou FM and Hablitz JJ (1997) Metabotropic glutamate receptor enhancement of spontaneous IPSCs in neocortical interneurons. J Neurophysiol 78:2287-2295.