(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a potent and selective antagonist of type 2 metabotropic glutamate receptors

Molecular Pharmacology

Volumn 50, Issue 1, 1996, Pages 6-9

  Thomsen, Christian ^a   Bruno, Valeria ^b,c   Nicoletti, Ferdinando ^b,c   Marinozzi, Maura ^d   Pellicciari, Roberto ^d  

^a NOVO NORDISK A S   (Denmark)

^b IRCCS NEUROMED   (Italy)

^c UNIVERSITY OF CATANIA   (Italy)

^d UNIVERSITY OF PERUGIA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2' CARBOXY 3' PHENYLCYCLOPROPYL)GLYCINE; 2 (2,3 DICARBOXYCYCLOPROPYL)GLYCINE; 2 AMINO 4 PHOSPHONOBUTYRIC ACID; ALPHA METHYL 4 CARBOXYPHENYLGLYCINE; CYCLIC AMP; FORSKOLIN; GLUTAMATE RECEPTOR AGONIST; GLUTAMATE RECEPTOR ANTAGONIST; METABOTROPIC RECEPTOR; N METHYL DEXTRO ASPARTIC ACID; PHOSPHATIDYLINOSITIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BRAIN CELL; CELL VIABILITY; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; FETUS; GLIA CELL; HAMSTER; HYDROLYSIS; KIDNEY CELL; MOUSE; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; CELL LINE; CELL SURVIVAL; CELLS, CULTURED; CEREBRAL CORTEX; CRICETINAE; CYCLIC AMP; CYCLOLEUCINE; CYCLOPROPANES; EXCITATORY AMINO ACID ANTAGONISTS; FETUS; GLUTAMIC ACID; GLYCINE; KIDNEY; KINETICS; MICE; N-METHYLASPARTATE; NEUROGLIA; NEURONS; NEUROTOXINS; PHOSPHATIDYLINOSITOLS; RECEPTORS, METABOTROPIC GLUTAMATE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0029891195     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (22)

1. Pin, J.-P., and R. Duvoisin. The metabotropic glutamate receptors: structure and functions. Neuropharmacology 34:1-26 (1995).
2. Glaum, S. R., and R. J. Miller. Acute regulation of synaptic transmission by metabotropic glutamate receptors, in The Metabotropic Glutamate Receptors (P. J. Conn and J. Patel, eds.). Humana Press, Totowa, 147-172 (1994).
3. Tanabe, Y., A. Nomura, M. Masu, R. Shigemoto, and S. Nakanishi. Signal transduction, pharmacological properties, and expression patterns of two rat metabotropic glutamate receptors, mGluR3 and mGluR4. J. Neurosci. 13:1372-1378 (1993).
4. Thomsen, C., P. Kristensen, E. Mulvihill, B. Haldeman, and P. D. Suzdak. L-2-Amino-4-phosphonobutyrate (L-AP4) is an agonist at the type IV metabotropic glutamate receptor which is negatively coupled to adenylate cyclase. Eur. J. Pharmacol. 227:361-363 (1992).
5. Hayashi, Y., A. Momiyama, T. Takahashi, H. Ohish, R. Ogawa-Meguro, R. Shigemoto, N. Mizuno, and S. Nakanishi. Role of a metabotropic glutamate receptor in synaptic modulation in the accessory olfactory bulb. Nature (Lond.) 366:687-690 (1993).
6. Schoepp, D. D., J. Goldsworthy, B. G. Johnson, C. R. Salhoff, and S. R. Baker. 3:5-Dihydroxyphenylglycine is a highly selective agonist for phosphoinositide-linked metabotropic glutamate receptors in the rat hippocampus. J. Neurochem. 63:769-772 (1994).
7. Hayashi, Y., N. Sekiyama, S. Nakanishi, D. E. Jane, D. C. Sunter, E. F. Birse, P. M. Udvarhelyi, and J. C. Watkins. Analysis of agonist and antagonist activities of phenylglycine derivatives for different cloned metabotropic glutamate-receptor subtypes. J. Neurosci. 14:3370-3377 (1994).
8. Thomsen C., E. Boel, and P. D. Suzdak. Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family. Eur. J. Pharmacol. 267:77-84 (1994).
9. Koh, J.-Y., E. Palmer, and C. W. Cotman. Activation of the metabotropic glutamate receptor attenuates N-methyl-D-aspartate neurotoxicity in cortical cultures. Proc. Natl. Acad. Sci. USA 88:9431-9435 (1991).
10. Sacaan, A. I., and D. D. Schoepp. Activation of hippocampal metabotropic excitatory amino acid receptors leads to seizures and neuronal damage. Neurosci. Lett. 139:77-82 (1992).
11. Bruno, V., A. Copani, T. Knopfel, R. Kuhn, G. Casabona, P. Dellalbani, D. F. Condorelli, and F. Nicoletti, Activation of metabotropic glutamate receptors coupled to inositol phospholipid hydrolysis amplifies NMDA-induced neuronal degeneration in cultured cortical cells. Neuropharmacology 34:1089-1098 (1995).
12. Buisson, A., and D. W. Choi. The inhibitory mGluR agonist, S-4-carboxy-3-hydroxy-phenylglycine selectively attenuates NMDA neurotoxicity and oxygen-glucose deprivation-induced neuronal death. Neuropharmacology 34:1081-1087 (1995).
13. Graham, M. E., and R. D. Burgoyne. Activation of metabotropic glutamate receptors by L-AP4 stimulates survival of rat cerebellar granule cells in culture. Eur. J. Pharmacol. 288:115-123 (1994).
14. Shinozaki, H. Neuron damage induced by some potent kainoids and neuroprotective action of new agonists of metabotropic glutamate receptors. Eur. Neurol. 34(suppl.):2-9 (1994).
15. Ambrosini, A., L. Bresciani, S. Fracchia, N. Brunello, and G. Racagni. Metabotropic glutamate receptors negatively coupled to adenylate cyclase inhibit N-methyl-D-aspartate receptor activity and prevent neurotoxicity in mesenphalic neurons in vitro. Mol. Pharmacol. 47:1057-1064 (1995).
16. Bruno, V., G. Battaglia, A. Copani, R. G. Giffard, G. Raciti, R. Raffaele, H. Shinozaki, and F. Nicoletti. Activation of class-II or class-III metabotropic glutamate receptors protects cultured cortical neurons against excitotoxic degeneration. Eur. J. Neurosci. 7:1906-1913 (1995).
17. Jane, D. E., K. Pittaway, D. C. Sunter, N. K. Thomas, and J. C. Watkins. New phenylglycine derivatives with potent and selective antagonist activity at presynaptic glutamate receptors in neonatal rat spinal-cord. Neuropharmacology 34:851-856 (1995).
18. Ikeda, S. R., D. M. Lovinger, B. A. McCool, and D. L. Lewis. Heterologous expression of metabotropic glutamate receptors in adult sympathetic neurons: subtype specific coupling to ion channels. Neuron 14:1029-1038 (1995).
19. Testa, C. M., D. G. Standaert, A. B. Young, and J. B. Penney. Metabotropic glutamate receptor mRNA expression in the basal ganglia of the rat. J. Neurosci. 14:3005-3018 (1994).
20. DeLong, M. Primate models of movement disorders of basal ganglia origin. Trends Neurosci. 13:281-285 (1990).
21. Sacaan A. I., F. P, Bymaster, and D. D. Schoepp. Metabotropic glutamate receptor activation produces extrapyramidal motor system activation that is mediated by striatal dopamine. J. Neurochem. 59:245-251 (1992).
22. Kaatz, K. W., and R. L. Albin. Intrastriatal and intrasubthalamic stimulation of metabotropic glutamate receptors: a behavioral and fos immunohistochemical study. Neuroscience 66:55-65 (1995).