LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors

Neuropharmacology

Volumn 37, Issue 1, 1998, Pages 1-12

  Kingston, A E ^a   Ornstein, P L ^a   Wright, R A ^a   Johnson, B G ^a   Mayne, N G ^a   Burnett, J P ^a   Belagaje, R ^a   Wu, S ^a   Schoepp, D D ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

cAMP; LY341495; Metabotropic glutamate receptor antagonist; Metabotropic glutamate receptors; Phosphoinositide hydrolysis

Indexed keywords

2 (2 CARBOXYCYCLOPROP 1 YL) 3 (XANTH 9 YL)PROPANOIC ACID; 2 AMINO 2 (2 CARBOXYPROPAN 1 YL) 3 (DIBENZOPYRAN 4 YL)PROPANOIC ACID; 2 AMINO 4 PHOSPHONOBUTYRIC ACID; ALPHA AMINO 3 HYDROXY 5 METHYL 4 ISOXAZOLEPROPIONIC ACID; CYCLOLEUCINE; GLUTAMATE RECEPTOR; GLUTAMATE RECEPTOR ANTAGONIST; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; NEUROTRANSMISSION; NONHUMAN; PHOSPHATE METABOLISM; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

AMINO ACIDS; ANIMALS; CELL LINE; CYCLIC AMP; EXCITATORY AMINO ACID ANTAGONISTS; FORSKOLIN; HUMANS; PROSENCEPHALON; RATS; RECEPTORS, METABOTROPIC GLUTAMATE; XANTHENES;

EID: 0031808420     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(97)00191-3     Document Type: Article

References (33)

1. Annoura H., Fukunaga A., Uesugi M., Tatsuoka T., Horikawa Y. A novel class of antagonist for matabotropic glutamate receptors, 7-(hydroxy-imino) cyclopropan (b) chromen-1a carboxylates. Biorg. Med. Chem. Letts. 6:1996;763-766.
2. Bennett, J.P. Jr., 1978. Methods in binding studies. In: Neurotransmitter Receptor Binding. Raven Press, New York, pp. 57-90.
3. Desai M.A., Burnett J.P., Mayne N.G., Schoepp D.D. Cloning and expression of a human mGluR1a: Enhanced coupling upon co-transfection with a glutamate transporter. Mol. Pharmacol. 48:1995;648-657.
4. Hayashi Y., Sekiyama N., Nakanishi S. et al. Analysis of agonist and antagonist activities of phenylglycine derivatives for different cloned metabotropic glutamate receptor subtypes. J. Neurosci. 14:1994;3370-3377.
5. Hollman M., Heinemann S. Cloned glutamate receptors. Ann Rev. Neurosci. 17:1994;31-103.
6. Jane D.E., Jones St. J. P.L., Pook P.C.-K., Tse H.-W., Watkins J.C. Actions of two new antagonists showing selectivity for different subtypes of metabotropic glutamate receptor in the neonatal rat spinal cord. Br. J. Pharmacol. 112:1994;809-816.
7. Kingston A.E., Burnett J.P., Mayne N.G., Lodge D. Pharmacological analysis of 4-carboxyphenylglycine derivatives: Comparison of effects on mGluR1a and mGluR5a subtypes. Neuropharmacology. 34:1995;887-894.
8. Knopfel T., Kuhn R., Allgeier H. Metabotropic glutamate receptors: Novel targets for drug development. J. Med. Chem. 38:1995a;1417-1426.
9. Knopfel T., Lukic S., Leonardt T., Flor P.J., Kuhn R., Gasparini F. Pharmacological characterization of MCCG and MAP4 at the mGluR1b, mGluR2 and mGluR4a human metabotropic glutamate receptor subtypes. Neuropharmacology. 34:1995b;1099-1102.
10. Maslanski, J.A., Busa, W.B., 1990. A sensitive and specific mass assay for myo-inositol and inositol phosphates. In: Irvine, R.F. (Ed.), Methods in Inositide Research. Raven Press, New York, pp. 113-126.
11. Moroni F., Lombardi G., Thomsen C. et al. Pharmacological characterisation of 1-amino-indan-1,5-dicarboxylic acid: a potent mGluR antagonist. J. Pharm. Exp. Ther. 281:1997;721-729.
12. Ornstein, P.L., Bleisch, T.J., Arnold, M.B., Wright, R.A., Johnson, B.G., Schoepp, D.D., 1998a. 2-Substituted 2SR-2-amino-2-(1SR,2SR-2-carboxycyclopropan-1-yl)glycines as potent and selective antagonists of group 2 metabotropic glutamate receptors: Part 1; Effects of alkyl, arylalkyl and diarylalkyl substitution. J. Med. Chem. 41, 346-357.
13. Ornstein, P.L., Bleisch, T.J., Arnold, M.B., Wright, R.A., Johnson, B.G., Tizzano, J.P., Helton, D.R., Kallman, M.J., Schoepp, D.D., 1998b. 2-Substituted 2SR-2-amino-2-(1SR,2SR-2-carboxycyclopropan-1-yl)glyc ines as potent and selective antagonists of group 2 metabotropic glutamate receptors: Part 2; Effects of aromatic substitution: pharmacological characterization and bioavailability. J. Med. Chem. 41, 358-378.
14. Pellicciari R., Luneia R., Costantino G. et al. 1-Aminoindan-1,5,dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors. J. Med. Chem. 38:1995;3717-3719.
15. Pellicciari R., Raimondo M., Marinozzi M., Natalini B., Costantino G., Thomsen C. (S)-(+)-2-(3′-Carboxybicyclo [1.1.1] pentyl)glycine, a structurally new group -1 metabotropic glutamate receptor antagonist. J. Med. Chem. 39:1996a;2874-2876.
16. Pellicciari R., Marinozzi M., Natalini B. et al. Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2′-carboxy-3′-phenylcyclopropyl)glycine. Focus on (2S,1′S,2′S, 3′R)-2-(2′-carboxy-3′-phenylcyclopropyl) glycine, a novel and selective group II metabotropic glutamate receptor antagonist. J. Med. Chem. 39:1996b;2259-2269.
17. Pin J.-P., Duvoisin R.M. The metabotropic glutamate receptors: structure and function. Neuropharmacol. 34:1995;1-26.
18. Saugstad J.A., Kinzie J.M., Shinohara M.M., Segerson T.P., Westbrook G.L. Cloning and expression of rat metabotropic glutamate receptor 8 reveals a distinct pharmacological profile. Mol. Pharmacol. 51:1997;119-125.
19. Schoepp D.D., Conn P.J. Metabotropic glutamate receptors in brain function and pathology. Trends Pharm. Sci. 14:1993;13-25.
20. Schoepp D.D., Sacaan A.I. Metabotropic glutamate receptors and neuronal degenerative disorders. Neurobiol. Aging. 15:1994;261-263.
21. Schoepp D.D., Johnson B.G., Salhoff C.R., Wright R.A., Goldsworthy J.S., Baker S.R. Second messenger responses in brain slices to elucidate novel glutamate receptors. J. Neurosci. Methods. 59:1995a;105-110.
22. Schoepp D.D., Lodge D., Bleakman D. et al. In vitro and in vivo antagonism of AMPA receptor activation by (3S, 4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl) ethyl] decahydroisoquinaline-3-carboxylic acid. Neuropharmacology. 34:1995b;1159-1168.
23. Schoepp D.D., Salhoff C.R., Wright R.A. et al. The novel metabotropic glutamate receptor agonist 2R,4R-APDC potentiates stimulation of phosphoinositide hydrolysis in the rat hippocampus by 3,5-dihydroxyphenylglycine: Evidence for a synergistic interaction between group 1 and group 2 receptors. Neuropharmacology. 35:1996;1661-1672.
24. Schoepp D.D., Johnson B.G., Wright R.A. et al. LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors. Neuropharmacology. 36:1997;1-11.
25. Sekiyama N., Hayashi Y., Nakanishi S., Jane D.E., Tse H.-W., Birse E.F., Watkins J.C. Structure activity relationships of new agonists and antagonists of different metabotropic glutamate receptor subtypes. Brit. J. Pharmacol. 117:1996;1493-1503.
26. +-dependent glutamate/aspartate transporter from rat brain. Proc. Natl. Acad. Sci. USA. 89:1992;10955-10959.
27. Thomas N.K., Jane D.E., Pittaway K., Sunter D.C., Watkins J.C. Antagonism of L-AP4 and (1S,3S)-ACPD induced depression of dorsal root evoked monsynaptic excitation of neonatal motoneurones by the novel antagonists MSPG and MPPG. Brit. J. Pharmacol. 114:1995;9P.
28. Thomsen C., Boel E., Suzdak P.D. Actions of phenylglycine analogs at subtypes of the metabotropic glutamate family. Eur. J. Pharmacol. (Mol. Pharmacol. Section). 267:1994a;77-84.
29. Thomsen C., Hansen L., Suzdak P.D. L-Glutamate uptake inhibitors may stimulate phosphoinositide hydrolysis in baby hamster kidney cells expressing mGluR1α via heteroexchange with L-glutamate without direct activation of mGluR1α J. Neurochem. 59:1994b;383-386.
30. Thomsen C., Bruno V., Nicoletti F., Marinozzi M., Pellicciari R. 2S,1′S,2′S,3′R)-2-(2′-carboxy-3′-phenylcyclopropyl )glycine, a potent and selective antagonist of type 2 metabotropic glutamate receptors. Mol. Pharmacol. 50:1996;6-9.
31. Wermuth C.G., Mann A., Schoenfelder A. et al. 2S,4S)-2-Amino-4-(4,4-diphenylbut-1-yl)-pentane-1,5-dioic acid: a potent and selective antagonist for metabotropic glutamate receptors negatively linked to adenylate cyclase. J. Med. Chem. 39:1996;814-816.
32. 3H]glutamate binding sites in the rat brain. J. Neurochem. 63:1994;938-945.
33. Wu, S., Wright, R.A., Rockey, P.K., Burgett, S.G., Arnold, J.S., Rosteck, P.R., Johnson, B.G., Schoepp, D.D., Belagaje, R.M., 1998. Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression and comparison of pharmacological properties in RGT cells. Mol. Brain Res. 53, 88-97.