[3H]R214127: A novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists

Molecular Pharmacology

Volumn 63, Issue 5, 2003, Pages 1082-1093

  Lavreysen, Hilde ^a,b   Janssen, Cor ^a   Bischoff, François ^a   Langlois, Xavier ^a   Leysen, Josée E ^b   Lesage, Anne S J ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b VU UNIVERSITY AMSTERDAM   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

1 (3,4 DIHYDRO 2H PYRANO[2,3 B]QUINOLIN 7 YL) 2 PHENYL 1 ETHANONE; 2 QUINOXALINECARBOXAMIDE N ADAMANTAN 1 YL; 6A NAPHTHALAN 2 YLMETHYL 5 METHYLIDENEHEXAHYDROCYCLOPENTA[C]FURAN 1 ONE; 7 (HYDROXYIMINO)CYCLOPROPA[B]CHROMENE 1A CARBOXYLATE ETHYL ESTER; BAY 367620; CHROMENE DERIVATIVE; DECALIN DERIVATIVE; FURANONE DERIVATIVE; GLUTAMIC ACID; METABOTROPIC RECEPTOR; NPS 2390; OXIME DERIVATIVE; QUINOXALINE DERIVATIVE; QUISQUALIC ACID; R 214127; RADIOLIGAND; RECEPTOR SUBTYPE; TRITIUM; UNCLASSIFIED DRUG; 7 (HYDROXYIMINO)CYCLOPROPAN(B)CHROMEN 1A CARBXOYLIC ACID ETHYL ESTER; 7-(HYDROXYIMINO)CYCLOPROPAN(B)CHROMEN-1A-CARBXOYLIC ACID ETHYL ESTER; BAY36 7620; BAY36-7620; CHROMONE DERIVATIVE; METABOTROPIC GLUTAMATE RECEPTOR TYPE 1; NAPHTHALENE DERIVATIVE; PYRAN DERIVATIVE; QUINOLINE DERIVATIVE;

ALLOSTERISM; AMYGDALOID NUCLEUS; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BINDING KINETICS; BINDING SITE; BRAIN CORTEX; CEREBELLUM; CHO CELL; CONTROLLED STUDY; CORPUS STRIATUM; DENTATE GYRUS; DRUG RECEPTOR BINDING; GLOBUS PALLIDUS; HIPPOCAMPUS; ISOTOPE LABELING; MALE; MOUSE; NONHUMAN; NUCLEUS ACCUMBENS; OLFACTORY BULB; PRIORITY JOURNAL; PUTAMEN; RAT; SUBSTANTIA NIGRA; THALAMUS; TISSUE DISTRIBUTION; ANIMAL; BINDING COMPETITION; BRAIN; CELL LINE; CELL MEMBRANE; COMPARATIVE STUDY; DRUG ANTAGONISM; DRUG EFFECT; GENETIC TRANSFECTION; HAMSTER; HUMAN; METABOLISM; RADIOASSAY;

ALLOSTERIC REGULATION; ANIMALS; BINDING SITES; BINDING, COMPETITIVE; BRAIN; CELL LINE; CELL MEMBRANE; CHO CELLS; CHROMONES; CRICETINAE; HUMANS; NAPHTHALENES; PYRANS; QUINOLINES; QUISQUALIC ACID; RADIOLIGAND ASSAY; RATS; RECEPTORS, METABOTROPIC GLUTAMATE; TRANSFECTION; TRITIUM;

EID: 0037731410     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.63.5.1082     Document Type: Article

References (29)

1. Aiba A, Kano M, Chen C, Stanton ME, Fox GD, Herrup K, Zwingman TA, and Tonegawa S (1994) Deficient cerebellar long-term depression and impaired motor learning in mGluR1 mutant mice. Cell 79:377-388.
2. Bordi F and Ugolini A (1999) Group I metabotropic glutamate receptors: implications for brain diseases. Prog Neurobiol 59:55-79.
3. Carroll FY, Stolle A, Beart PM, Voerste A, Brabet I, Mauler F, Joly C, Antonicek H, Bockaert J, Muller T, et al. (2001) BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol Pharmacol 59:965-973.
4. i) and the concentration of inhibitor which causes 50 percent inhibition (IC50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
5. Conquet F, Bashir ZI, Davies CH, Daniel H, Ferraguti F, Bordi F, Franz-Bacon K, Reggiani A, Matarese V, and Conde F (1994) Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1. Nature (Lond) 372:237-243.
6. Ferraguti F, Conquet F, Corti C, Grandes P, Kuhn R, and Knopfel T (1998) Immunohistochemical localization of the mGluR1β metabotropic glutamate receptor in the adult rodent forebrain: evidence for a differential distribution of mGluR1 splice variants. J Comp Neur 400:391-407.
7. 3H]M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5. Bioorg Med Chem Lett 12:407-409.
8. Grandes P, Mateos JM, Ruegg D, Kuhn R, and Knopfel T (1994) Differential cellular localization of three splice variants of the mglur1 metabotropic glutamate receptor in rat cerebellum. Neuroreport 5:2249-2252.
9. Hermans E, Nahorski SR, and Chaliss RA (1998) Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor. Neuropharmacology 37:1645-1647.
10. Kingston AE, Lowndes J, Evans N, Clark B, Tomlinson R, Burnett JP, Mayne NG, Cockerham SL, and Lodge D (1998) Sulphur-containing amino acids are agonists for group 1 metabotropic receptors expressed in clonal RGT cell lines. Neuropharmacology 37:277-287.
11. Lavreysen H, Le Poul E, Van Gompel P, Dillen L, Leysen JE, and Lesage ASJ (2002) Supersensitivity of the human metabotropic glutamate la receptor signaling in L929sA cells. Mol Pharmacol 61:1244-1254.
12. Litschig S, Gasparini F, Rueegg D, Stoehr N, Flor PJ, Vranesic I, Prezeau L, Pin JP, Thomsen C, and Kuhn R (1999) CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate Binding. Mol Pharmacol 55:453-461.
13. Lujan R, Nusser Z, Roberts JD, Shigemoto R, and Somogyi P (1996) Perisynaptic location of metabotropic glutamate receptors mGluR1 and mGluR5 on dendrites and dendritic spines in the rat hippocampus. Eur J Neurosci 8:1488-1500.
14. Mabire DJ, Venet MG, Coupa S, Poncelet AP, and Lesage ASJ (2002) inventors; Janssen Pharmaceutica, applicant. Metabotropic glutamate receptor antagonists. Patent application WO 02/28837. 2002 April 11.
15. Martin LJ, Blackstone CD, Huganir RL, and Price DL (1992) Cellular localization of a metabotropic glutamate receptor in rat brain. Neuron 9:259-270.
16. 3H]quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem 75:2590-2601.
17. 3H]quisqualate binding to the baculovirally expressed type 1 metabotropic glutamate receptor. Soc Neurosci Abstr 23:2023.
18. Pin JP, De Colle C, Bessis AS, and Acher F (1999) New perspectives for the development of selective metabotropic glutamate receptor ligands. Eur J Pharmacol 375:277-294.
19. Pin JP and Duvoisin R (1995) The metabotropic glutamate receptors: structure and functions. Neuropharmacology 34:1-26.
20. Schoepp DD, Jane DE, and Monn JA (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38:1431-1476.
21. 3H]glutamate receptor binding in membranes. Neurosci Lett 145:100-104.
22. Shigemoto R, Abe T, Nomura S, Nakanishi S, and Hirano T (1994) Antibodies inactivating mGluR1 metabotropic glutamate receptor block long-term depression in cultured purkinje cells. Neuron 12:1245-1255.
23. Shigemoto R, Kinoshita A, Wada E, Nomura S, Ohishi H, Takada M, Flor PJ, Neki A, Abe T, Nakanishi S, et al. (1997) Differential presynaptic localization ofmetabotropic glutamate receptor subtypes in the rat hippocampus. J Neurosci 17:7503-7522.
24. 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.
25. Shigemoto R, Nomura S, Ohishi H, Sugihara H, Nakanishi S, and Mizuno N (1993) Immunohistochemical localization of a metabotropic glutamate receptor, mGluR5, in the rat brain. Neurosci Lett 163:53-57.
26. Thomsen C, Mulvihill ER, Haldeman B, Pickering DS, Hampson DR, and Suzdak PD (1993) A pharmacological characterization of the mGluR1 alpha subtype of the metabotropic glutamate receptor expressed in a cloned baby hamster kidney cell Line. Brain Res 619:22-28.
27. Van de Waterbeemd H, Carrupt P, and Testa B (1986) Molecular electrostatic potential of orthopramides: implications for their interaction with the D-2 dopamine receptor. J Med Chem 29:600-606.
28. 3H]glutamate binding sites in the rat brain. J Neurochem 63:938-945.
29. Zhu BT (1993) The competitive and noncompetitive antagonism of receptor-mediated drug actions in the presence of spare receptors. J Pharm Tox Meth 29:85-91.