메뉴 건너뛰기




Volumn 23, Issue 1, 1998, Pages 61-69

Identification and pharmacological characterization of GV150526, a novel glycine antagonist as a potent neuroprotective agent

Author keywords

[No Author keywords available]

Indexed keywords

DIZOCILPINE; GAVESTINEL; GLYCINE; GLYCINE RECEPTOR AGONIST; N METHYL DEXTRO ASPARTIC ACID; UNCLASSIFIED DRUG;

EID: 0031951717     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1998.023.01.442870     Document Type: Article
Times cited : (29)

References (55)
  • 1
    • 0025063609 scopus 로고
    • Excitatory amino acid neurotoxicity and neurodegenerative diseases
    • Meldrum, B., Garthwaite, J. Excitatory amino acid neurotoxicity and neurodegenerative diseases. Trends Pharmacol Sci 1990, 11:379.
    • (1990) Trends Pharmacol Sci , vol.11 , pp. 379
    • Meldrum, B.1    Garthwaite, J.2
  • 2
    • 0025470262 scopus 로고
    • Cerebral hypoxia: Some new approaches and unanswered questions
    • Choi, D.W. Cerebral hypoxia: Some new approaches and unanswered questions. J Neurosci 1990, 10: 2493.
    • (1990) J Neurosci , vol.10 , pp. 2493
    • Choi, D.W.1
  • 3
    • 0025390880 scopus 로고
    • Protection against ischaemic neuronal damage by drugs acting on excitatory neurotransmission
    • Meldrum, B. Protection against ischaemic neuronal damage by drugs acting on excitatory neurotransmission. Cerebrovasc Brain Metab Rev 1990, 2: 27.
    • (1990) Cerebrovasc Brain Metab Rev , vol.2 , pp. 27
    • Meldrum, B.1
  • 4
    • 0026701712 scopus 로고
    • Excitatory amino acid antagonists and their potential for the treatment of ischemic brain damage in man
    • McCullogh, J. Excitatory amino acid antagonists and their potential for the treatment of ischemic brain damage in man. Br J Clin Pharmacol 1992, 34: 106.
    • (1992) Br J Clin Pharmacol , vol.34 , pp. 106
    • McCullogh, J.1
  • 7
    • 0025265926 scopus 로고
    • The role of glutamate neurotoxicity in hypoxic-ischemic neuronal death
    • Choi D.W., Rothman, S.M. The role of glutamate neurotoxicity in hypoxic-ischemic neuronal death. Ann Rev Pharmacol Toxicol 1991, 31: 171.
    • (1991) Ann Rev Pharmacol Toxicol , vol.31 , pp. 171
    • Choi, D.W.1    Rothman, S.M.2
  • 8
    • 0025762248 scopus 로고
    • Site for antagonism on the N-methyl-D-aspartate receptor channel complex
    • Wong, E.H.F., Kemp, J.A. Site for antagonism on the N-methyl-D-aspartate receptor channel complex. Ann Rev Pharmacol Toxicol 1991, 31: 401.
    • (1991) Ann Rev Pharmacol Toxicol , vol.31 , pp. 401
    • Wong, E.H.F.1    Kemp, J.A.2
  • 11
    • 0023091647 scopus 로고
    • Glycine potentiates the NMDA receptor response in cultured brain mouse neurones
    • Johnson, J.W., Ascher, P. Glycine potentiates the NMDA receptor response in cultured brain mouse neurones. Nature 1987, 325: 529.
    • (1987) Nature , vol.325 , pp. 529
    • Johnson, J.W.1    Ascher, P.2
  • 12
    • 0023754192 scopus 로고
    • Requirements for glycine in activation of NMDA receptors expressed in Xenopus oocytes
    • Kleckner, N.W., Dingledine, R. Requirements for glycine in activation of NMDA receptors expressed in Xenopus oocytes. Science 1988, 241: 835.
    • (1988) Science , vol.241 , pp. 835
    • Kleckner, N.W.1    Dingledine, R.2
  • 13
    • 0025285077 scopus 로고
    • Glycine is a coagonist at the NMDA receptor/ion channel complex
    • Thomson, A.M. Glycine is a coagonist at the NMDA receptor/ion channel complex. Prog Neurobiol 1990, 35: 53.
    • (1990) Prog Neurobiol , vol.35 , pp. 53
    • Thomson, A.M.1
  • 14
    • 0026097969 scopus 로고
    • Competitive antagonism of glycine at the N-methyl-D-aspartate (NMDA) receptor
    • Huettner, J.E. Competitive antagonism of glycine at the N-methyl-D-aspartate (NMDA) receptor. Biochem Pharmacol 1991, 41: 9.
    • (1991) Biochem Pharmacol , vol.41 , pp. 9
    • Huettner, J.E.1
  • 15
    • 0022650213 scopus 로고
    • Selective impairment of learning and blockage of long-term potentiation by an N-methyl-D-aspartate antagonist, AP5
    • Morris, R.G.M., Anderson, E., Lynch, G.S., Baudry, M. Selective impairment of learning and blockage of long-term potentiation by an N-methyl-D-aspartate antagonist, AP5. Nature 1986, 319: 774.
    • (1986) Nature , vol.319 , pp. 774
    • Morris, R.G.M.1    Anderson, E.2    Lynch, G.S.3    Baudry, M.4
  • 16
    • 0025057540 scopus 로고
    • Selective blockade of N-methyl-D-aspartate (NMDA)-induced convulsions by NMDA antagonists and putative glycine antagonists: Relationship with phenylcyclidine-like behavioral effects. J
    • Koek, W., Colpaert, F.C. Selective blockade of N-methyl-D-aspartate (NMDA)-induced convulsions by NMDA antagonists and putative glycine antagonists: Relationship with phenylcyclidine-like behavioral effects. J Pharmacol Exp Ther 1990, 252: 349.
    • (1990) Pharmacol Exp Ther , vol.252 , pp. 349
    • Koek, W.1    Colpaert, F.C.2
  • 17
    • 0025185844 scopus 로고
    • Effect of NMDA and strychnine-insensitive glycine site antagonists on NMDA-mediated convulsions and learning
    • Chiamulera, C., Costa, S., Reggiani, A. Effect of NMDA and strychnine-insensitive glycine site antagonists on NMDA-mediated convulsions and learning. Psychopharmacology 1990, 112: 551.
    • (1990) Psychopharmacology , vol.112 , pp. 551
    • Chiamulera, C.1    Costa, S.2    Reggiani, A.3
  • 18
    • 0000988467 scopus 로고
    • Non-competitive NMDA antagonists acting at the glycine site
    • Meldrum, B. (Ed.). Blackwell: Oxford
    • Palfreyman, M.G., Baron, M.B. Non-competitive NMDA antagonists acting at the glycine site. In: Excitatory Amino Acid Antagonists. Meldrum, B. (Ed.). Blackwell: Oxford 1991, 101-29.
    • (1991) Excitatory Amino Acid Antagonists , pp. 101-129
    • Palfreyman, M.G.1    Baron, M.B.2
  • 19
    • 0026630259 scopus 로고
    • Glycine antagonists: Regulation of the NMDA receptor-complex by the strychnine-insensitive glycine site
    • Carter, A.J. Glycine antagonists: Regulation of the NMDA receptor-complex by the strychnine-insensitive glycine site. Drugs Fut 1992, 17: 595.
    • (1992) Drugs Fut , vol.17 , pp. 595
    • Carter, A.J.1
  • 20
    • 0027469106 scopus 로고
    • The glycine site of the NMDA receptor - Five years on
    • Kemp, J.A., Leeson, P.D. The glycine site of the NMDA receptor - Five years on. TIPS 1993, 14: 20.
    • (1993) TIPS , vol.14 , pp. 20
    • Kemp, J.A.1    Leeson, P.D.2
  • 21
    • 0027988561 scopus 로고
    • The glycine site on the NMDA receptor: Structure-activity relationships and therapeutic potential
    • Leeson, P.D., Iversen, L.L. The glycine site on the NMDA receptor: Structure-activity relationships and therapeutic potential. J Med Chem 1994, 37: 4053.
    • (1994) J Med Chem , vol.37 , pp. 4053
    • Leeson, P.D.1    Iversen, L.L.2
  • 22
    • 0002864470 scopus 로고
    • Non competitive NMDA antagonists as drugs
    • Collingridge, G.L., Watkins, J.C. (Eds.). IRL Press: Oxford
    • Iversen, L.L., Kemp, J.A. Non competitive NMDA antagonists as drugs. In: The NMDA Receptor, 2nd Ed.. Collingridge, G.L., Watkins, J.C. (Eds.). IRL Press: Oxford 1994, 469-86.
    • (1994) The NMDA Receptor, 2nd Ed. , pp. 469-486
    • Iversen, L.L.1    Kemp, J.A.2
  • 23
    • 0000721597 scopus 로고    scopus 로고
    • Strychnine-insensitive glycine binding site and the NMDA receptor
    • Di Fabio, R., Gaviraghi, G., Reggiani, A. Strychnine-insensitive glycine binding site and the NMDA receptor. Chim Industria 1996, 78: 283.
    • (1996) Chim Industria , vol.78 , pp. 283
    • Di Fabio, R.1    Gaviraghi, G.2    Reggiani, A.3
  • 24
    • 0027439407 scopus 로고
    • Anticonvulsant activity of glycine-site NMDA antagonists. 1. 2-Carboxyl prodrugs of 5,7-dichlorokynurenic acid
    • Moore, K.W., Leeson, P.D., Carling, R.W. et al. Anticonvulsant activity of glycine-site NMDA antagonists. 1. 2-Carboxyl prodrugs of 5,7-dichlorokynurenic acid. Bioorg Med Chem Lett 1993, 3: 61.
    • (1993) Bioorg Med Chem Lett , vol.3 , pp. 61
    • Moore, K.W.1    Leeson, P.D.2    Carling, R.W.3
  • 25
    • 0027396632 scopus 로고
    • Anticonvulsant activity of glycine-site NMDA antagonists. 2. Trans 2-carboxy-4-substituted tetrahydroquinolines
    • Carling, R.W., Leeson, P.D., Moseley, A.M. et al. Anticonvulsant activity of glycine-site NMDA antagonists. 2. Trans 2-carboxy-4-substituted tetrahydroquinolines. Bioorg Med Chem Lett 1993, 3: 65.
    • (1993) Bioorg Med Chem Lett , vol.3 , pp. 65
    • Carling, R.W.1    Leeson, P.D.2    Moseley, A.M.3
  • 26
    • 0002453543 scopus 로고
    • Neuroprotective activity of GV150526A, a novel potent and selective glycine antagonist
    • Reggiani, A., Costa, S., Pietra, C. et al. Neuroprotective activity of GV150526A, a novel potent and selective glycine antagonist. Eur J Neurol 1995, 2: 6.
    • (1995) Eur J Neurol , vol.2 , pp. 6
    • Reggiani, A.1    Costa, S.2    Pietra, C.3
  • 27
    • 0002704022 scopus 로고    scopus 로고
    • Neuroprotection of GV150526A. Comparison with reference compounds
    • Pietra, C., Ziviani, L., Valerio, E., Tarter, G., Reggiani, A. Neuroprotection of GV150526A. Comparison with reference compounds. Stroke 1996, 27: 26.
    • (1996) Stroke , vol.27 , pp. 26
    • Pietra, C.1    Ziviani, L.2    Valerio, E.3    Tarter, G.4    Reggiani, A.5
  • 28
    • 0344892748 scopus 로고    scopus 로고
    • Novel substituted indole-2-carboxylates as potent glycine antagonists
    • (March 24-28, New Orleans) Abst 107
    • Di Fabio, R., Cugola, A., Donati, D. et al. Novel substituted indole-2-carboxylates as potent glycine antagonists. 211th ACS Natl Meet (March 24-28, New Orleans) 1996, Abst 107.
    • (1996) 211th ACS Natl Meet
    • Di Fabio, R.1    Cugola, A.2    Donati, D.3
  • 29
    • 0030739272 scopus 로고    scopus 로고
    • The glycine antagonist GV150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal ischemia in the rat
    • Bordi, F., Pietra, C., Ziviani, L., Reggiani, A. The glycine antagonist GV150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal ischemia in the rat. Exp Neurol 1997, 145: 425.
    • (1997) Exp Neurol , vol.145 , pp. 425
    • Bordi, F.1    Pietra, C.2    Ziviani, L.3    Reggiani, A.4
  • 30
    • 0009482135 scopus 로고    scopus 로고
    • Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site
    • Di Fabio, R., Capelli, A.M., Conti, N. et al. Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J Med Chem 1997, 40: 841.
    • (1997) J Med Chem , vol.40 , pp. 841
    • Di Fabio, R.1    Capelli, A.M.2    Conti, N.3
  • 31
    • 0019781152 scopus 로고
    • Determination of the equilibrium dissociation constants at a number of glycine binding sites in several areas of the rat central nervous system, using a Na-independent system
    • Kishimoto, H., Simon, J.R., Aprison, M.H. Determination of the equilibrium dissociation constants at a number of glycine binding sites in several areas of the rat central nervous system, using a Na-independent system. J Neurochem 1981, 37: 1015.
    • (1981) J Neurochem , vol.37 , pp. 1015
    • Kishimoto, H.1    Simon, J.R.2    Aprison, M.H.3
  • 32
    • 0023857628 scopus 로고
    • Kinetic characterization of the phenylcyclidine-N-methyl-D-aspartate receptor interaction: Evidence for steric blockade of the channel
    • Kloog, Y., Haring, R., Sokolovsky, M. Kinetic characterization of the phenylcyclidine-N-methyl-D-aspartate receptor interaction: Evidence for steric blockade of the channel. Biochemistry 1988, 27: 843.
    • (1988) Biochemistry , vol.27 , pp. 843
    • Kloog, Y.1    Haring, R.2    Sokolovsky, M.3
  • 33
    • 0025145549 scopus 로고
    • Requirement of glycine for the glutamate activity at the NMDA receptor site
    • Ratti, E., Tacconi, S., Graziani, F., Gaviraghi, G. Requirement of glycine for the glutamate activity at the NMDA receptor site. Eur J Pharmacol 1990, 183: 1665.
    • (1990) Eur J Pharmacol , vol.183 , pp. 1665
    • Ratti, E.1    Tacconi, S.2    Graziani, F.3    Gaviraghi, G.4
  • 34
    • 0026612860 scopus 로고
    • 3-[(+)-2-Carboxypiperazin-4-yl]propyl-1-phosphonic acid recognizes two N-methyl-D-aspartate binding sites in rat cerebral cortex membranes
    • Van Amsterdam, F.Th.M., Giberti, A., Mugnaini, M., Ratti, E. 3-[(+)-2-Carboxypiperazin-4-yl]propyl-1-phosphonic acid recognizes two N-methyl-D-aspartate binding sites in rat cerebral cortex membranes. J Neurochem 1992, 59: 1850.
    • (1992) J Neurochem , vol.59 , pp. 1850
    • Van Amsterdam, F.Th.M.1    Giberti, A.2    Mugnaini, M.3    Ratti, E.4
  • 35
    • 0025923790 scopus 로고
    • 3H]-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) to rat cortex membranes reveals two sites or affinity states
    • 3H]-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) to rat cortex membranes reveals two sites or affinity states. J Recept Res 1991, 11: 727.
    • (1991) J Recept Res , vol.11 , pp. 727
    • Giberti, A.1    Ratti, E.2    Gaviraghi, G.3    Van Amsterdam, F.Th.M.4
  • 36
    • 0022559513 scopus 로고
    • 3H]-kainate binding sites with different molecular target sizes in rat cortex
    • 3H]-kainate binding sites with different molecular target sizes in rat cortex. Neurosci Lett 1986, 65: 47.
    • (1986) Neurosci Lett , vol.65 , pp. 47
    • Honoré, T.1    Drejer, J.2    Nielsen, M.3
  • 37
    • 0019868418 scopus 로고
    • Focal cerebral ischemia in rat: 1. Description of technique and early neuropathological consequences
    • Tamura, A., Graham, D.I., McCullogh, J., Teasdale, G.M. Focal cerebral ischemia in rat: 1. Description of technique and early neuropathological consequences. J Cereb Blood Flow Metab 1981, 1: 53.
    • (1981) J Cereb Blood Flow Metab , vol.1 , pp. 53
    • Tamura, A.1    Graham, D.I.2    McCullogh, J.3    Teasdale, G.M.4
  • 38
    • 0024518502 scopus 로고
    • Indole-2-carboxylic acid: A competitive antagonist of potentiation by glycine at the NMDA receptor
    • Huettner, J.E. Indole-2-carboxylic acid: A competitive antagonist of potentiation by glycine at the NMDA receptor. Science 1989, 243: 1611.
    • (1989) Science , vol.243 , pp. 1611
    • Huettner, J.E.1
  • 39
    • 0025027922 scopus 로고
    • Indole derivatives: Antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex
    • Salituro, F.G., Harrison, B.L., Baron, B.M. et al. Indole derivatives: Antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex. J Med Chem 1990, 33: 2944.
    • (1990) J Med Chem , vol.33 , pp. 2944
    • Salituro, F.G.1    Harrison, B.L.2    Baron, B.M.3
  • 40
    • 0025766904 scopus 로고
    • Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor
    • Gray, N.M., Dappen, M.S., Cheng, B.K. et al. Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor. J Med Chem 1991, 34: 1283.
    • (1991) J Med Chem , vol.34 , pp. 1283
    • Gray, N.M.1    Dappen, M.S.2    Cheng, B.K.3
  • 41
    • 0025993114 scopus 로고
    • Design, synthesis and molecular modeling of 3-acylamino-2-carboxyindole NMDA receptor glycine site antagonists
    • Salituro, F.G., Tomlinson, R.C., Baron, B.M. et al. Design, synthesis and molecular modeling of 3-acylamino-2-carboxyindole NMDA receptor glycine site antagonists. Bioorg Med Chem Lett 1991, 1: 455.
    • (1991) Bioorg Med Chem Lett , vol.1 , pp. 455
    • Salituro, F.G.1    Tomlinson, R.C.2    Baron, B.M.3
  • 42
    • 0026652403 scopus 로고
    • 3-(2-Carboxylindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site
    • Salituro, F.G., Harrison, B.L., Baron, B.M. et al. 3-(2-Carboxylindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. J Med Chem 1992, 35: 1791.
    • (1992) J Med Chem , vol.35 , pp. 1791
    • Salituro, F.G.1    Harrison, B.L.2    Baron, B.M.3
  • 43
    • 0027397787 scopus 로고
    • Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: In vivo characterization
    • Rao, T.S., Gray, N.M., Dappen, M.S. et al. Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: In vivo characterization. Neuropharmacology 1993, 32: 139.
    • (1993) Neuropharmacology , vol.32 , pp. 139
    • Rao, T.S.1    Gray, N.M.2    Dappen, M.S.3
  • 44
    • 0027531485 scopus 로고
    • Structure-activity relationship of a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid
    • Smith, E.C.R., McQuaid, L.A., Calligaro, D.O., O'Malley, P.J. Structure-activity relationship of a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid. Bioorg Med Chem Lett 1993, 3: 81.
    • (1993) Bioorg Med Chem Lett , vol.3 , pp. 81
    • Smith, E.C.R.1    McQuaid, L.A.2    Calligaro, D.O.3    O'Malley, P.J.4
  • 45
    • 0025740632 scopus 로고
    • Kynurenic acid derivatives: Structure-activity relationship for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor
    • Leeson, P.D., Baker, R., Carling, R.W. et al. Kynurenic acid derivatives: Structure-activity relationship for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor. J Med Chem 1991, 34: 1243.
    • (1991) J Med Chem , vol.34 , pp. 1243
    • Leeson, P.D.1    Baker, R.2    Carling, R.W.3
  • 46
    • 0026766273 scopus 로고
    • 4-Amino-2-carboxytetrahydroquinolines. Structure-activity relationship for antagonism at the glycine site of the NMDA receptor
    • Leeson, P.D., Carling, R.W., Moore, K.W. et al. 4-Amino-2-carboxytetrahydroquinolines. Structure-activity relationship for antagonism at the glycine site of the NMDA receptor. J Med Chem 1992, 35: 1954.
    • (1992) J Med Chem , vol.35 , pp. 1954
    • Leeson, P.D.1    Carling, R.W.2    Moore, K.W.3
  • 48
    • 0000602289 scopus 로고
    • Determination of positional weighting factors for the Swain and Lupton substituent constants F and R
    • Williams, S.G., Norrington, F.E. Determination of positional weighting factors for the Swain and Lupton substituent constants F and R. J Am Chem Soc 1976, 98: 508.
    • (1976) J Am Chem Soc , vol.98 , pp. 508
    • Williams, S.G.1    Norrington, F.E.2
  • 51
    • 2642610894 scopus 로고
    • Bolt Beranek and Newman, Inc.
    • RS/1 v 4.4.1. Bolt Beranek and Newman, Inc. 1992.
    • (1992) RS/1 V 4.4.1
  • 52
    • 2642702368 scopus 로고
    • Oxford Molecular, Ltd.
    • TSAR v.2.2. Oxford Molecular, Ltd. 1993.
    • (1993) TSAR V.2.2
  • 53
    • 2642644382 scopus 로고
    • Daylight Chemical Information Systems
    • Daylight v4.41. Daylight Chemical Information Systems 1995.
    • (1995) Daylight V4.41
  • 55
    • 0027398676 scopus 로고
    • Synthesis of amides: An efficient and chemoselective method for the preparation of p-lactam derivatives related to HLE inhibitors
    • and references therein
    • Di Fabio, R., Summa, V., Rossi, T. Synthesis of amides: An efficient and chemoselective method for the preparation of p-lactam derivatives related to HLE inhibitors. Tetrahedron 1993, 49: 2239 and references therein.
    • (1993) Tetrahedron , vol.49 , pp. 2239
    • Di Fabio, R.1    Summa, V.2    Rossi, T.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.