Anxiolytic activity of glycine-B antagonists and partial agonists - No relation to intrinsic activity in the patch clamp

Neuropharmacology

Volumn 36, Issue 10, 1997, Pages 1355-1367

  Karcz Kubicha, M ^a   Jessa, M ^b   Nazar, M ^b   Plaznik, A ^b,c   Hartmann, S ^a   Parsons, C G ^a   Danysz, W ^a  

^a MERZ PHARMACEUTICALS GMBH   (Germany)

^b INSTITUTE OF PSYCHIATRY AND NEUROLOGY   (Poland)

^c MEDICAL UNIVERSITY OF WARSAW   (Poland)

Author keywords

Anxiety; Glycine(B) antagonists; Glycine(B) partial agonists; NMDA receptor antagonists; Patch clamp; Plus maze; Vogel test

Indexed keywords

2 AMINO 4 METHYL 5 PHOSPHONO 3 PENTENOIC ACID ETHYL ESTER; 3 AMINO 1 HYDROXY 2 PYRROLIDINONE; 7 CHLORO 4 HYDROXY 3 (3 PHENOXYPHENYL) 2 QUINOLONE; ACPC; AMINO ACID RECEPTOR BLOCKING AGENT; AMINO ACID RECEPTOR STIMULATING AGENT; ANXIOLYTIC AGENT; CYCLOSERINE; DIAZEPAM; MRZ 2 570; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANXIETY; ARTICLE; DRUG EFFECT; DRUG RECEPTOR BINDING; INTRAPERITONEAL DRUG ADMINISTRATION; MALE; NONHUMAN; PATCH CLAMP; PRIORITY JOURNAL; RAT; STATISTICAL ANALYSIS;

ANIMALS; ANXIETY; BEHAVIOR, ANIMAL; DISEASE MODELS, ANIMAL; EXCITATORY AMINO ACID AGENTS; MALE; MAZE LEARNING; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GLYCINE; RECEPTORS, N-METHYL-D-ASPARTATE; TRANQUILIZING AGENTS;

EID: 0030859819     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(97)00130-5     Document Type: Article

References (66)

1. Anthony E. W. and Nevins M. E. (1993) Anxiolytic-like effects of N-methyl-D-aspartate-associated glycine receptor ligands in the rat potentiated startle test. European Journal of Pharmacology 250: 317-324.
2. Bennett D. A. and Amrick C. L. (1986) 2-Amino-7-phosphono-heptanoic acid (AP7) produces discriminative stimuli and anticonflict effects similar to diazepam. Life Sciences 39: 2455-2461.
3. Berger P., Farrel D., Sharp F. and Skolnick P. (1994) Drugs acting at the strychnine-insensitive glycine receptor do not induce HSP-70 protein in the cingulate cortex. Neuroscience Letters 168: 147-150.
4. Bresink I., Benke T. A., Collett V. J., Seal A. J., Parsons C. G., Henley J. M. and Collingridge G. L. (1996) Effects of memantine on recombinant rat NMDA receptors expressed in HEK 293 cells. British Journal of Pharmacology 119: 195-204.
5. Bristow L. J., Flatman K. L., Hutson P. H., Kulagowski J. J., Leeson P. D., Young L. and Tricklebank M. D. (1996) The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, 1-701,324, in rodents. Journal of Pharmacology and Experimental Therapeutics 277: 578-585.
6. Bubser M., Keseberg U., Notz P. K. and Schmidt W. J. (1992) Differential behavioural and neurochemical effects of competitive and non-competitive NMDA receptor antagonists in rats. European Journal of Pharmacology 229: 75-82.
7. Carter A. J. (1994) Many agents that antagonize the NMDA receptor-channel complex in vivo also cause disturbances of motor coordination. Journal of Pharmacology and Experimental Therapeutics 269: 573-580.
8. Chen J., Graham S., Moroni F. and Simon R. (1993) A study of the dose dependency of a glycine receptor antagonist in focal ischemia. Journal of Pharmacology and Experimental Therapeutics 267: 937-941.
9. Chiamulera C., Costa S. and Reggiani A. (1990) Effect of NMDA-insensitive and strychnine-insensitive glycine site antagonists on NMDA-mediated convulsions and learning. Psychopharmacology 102: 551-553.
10. Corbett R. and Dunn R. W. (1991) Effects of HA-966 on conflict, social interaction, and plus maze behaviors. Drug Development Research 24: 201-205.
11. Corbett R. and Dunn R. W. (1993) Effects of 5,7dichloroky-nurenic acid on conflict, social interaction and plus maze behaviors. Neuropharmacology 32: 461-466.
12. Danysz W., Essmann U., Bresink I. and Wilke R. (1994) Glutamate antagonists have different effects on spontaneous locomotor activity in rats. Pharmacology Biochemistry and Behavior 48: 111-118.
13. Danysz W., Parsons C. G., Bresink I. and Quack G. (1995) Glutamate in CNS disorders - a revived target for drug development. Drug News and Perspectives 8: 261-277.
14. Danysz W., Wroblewski J. T., Brooker G. and Costa E. (1989b) Modulation of glutamate receptors by phencyclidine and glycine in the rat cerebellum: cGMP increase in vivo. Brain Research 479: 270-276.
15. Dunn R. W., Corbett R. and Fielding S. (1989) Effects of 5-HT1A receptor agonists and NMDA receptor antagonists in the social interaction test and the elevated plus maze. European Journal of Pharmacology 169: 1-10.
16. Emmett M. R., Mick S. J., Cler J. A., Rao T. S., Iyengar S. and Wood P. L. (1991) Actions of D-cycloserine at the N-methyl-D-aspartate-associated glycine receptor site in vivo. Neuropharmacology 30: 1167-1171.
17. Faiman C. P., Viu E., Skolnick P. and Trullas R. (1994) Differential effects of compounds that act at strychnine-insensitive glycine receptors in a punishment procedure. Journal of Pharmacology and Experimental Therapeutics 270: 528-533.
18. Fossom L. H., Basile A. S. and Skolnick P. (1995a) Sustained exposure to 1-aminocyclopropanecarboxylic acid, a glycine partial agonist, alters N-methyl-D-aspartate receptor function and subunit composition. Molecular Pharmacology 48: 981-987.
19. Fossom L. H., Vonlubitz D. K. J. E., Lin R. C. S. and Skolnick P. (1995b) Neuroprotective actions of 1-aminocyclopropanecarboxylic acid (ACPC): a partial agonist at strychnine-insensitive glycine sites. Neurological Research 17: 265-269.
20. Globus M. Y. T., Busto R., Martinez E., Valdes I., Dietrich W. D. and Ginsberg M. D. (1991) Comparative effect of transient global ischemia on extracellular levels of glutamate, glycine, and gamma-aminobutyric acid in vulnerable and nonvulnerable brain regions in the rat. Journal of Neurochemistry 57: 470-478.
21. Grimwood S., Kulagowski J. J., Mawer I. M., Rowley M., Leeson P. D. and Foster A. C. (1995) Allosteric modulation of the glutamate site on the NMDA receptor by four novel glycine site antagonists. European Journal of Pharmacology - Molecular Pharmacology Section 290: 221-226.
22. Haggerty G. C., Charles V. and Lanthorn T. H. (1993) Acute vacuolization study of subcutaneously administered d-cycloserine (DCS) in Sprague Dawley rats. Society of Neuroscience Abstracts 19: 1888.
23. Hargreaves R. J., Rigby M., Smith D. and Hill R. G. (1993) Lack of effect of 1-687,414 ((+)-cis-4-methyl-HA-966), an NMDA receptor antagonist acting at the glycine site, on cerebral glucose metabolism and cortical neuronal morphology. British Journal of Pharmacology 110: 36-42.
24. Hollmann M. and Heinemann S. (1994) Cloned glutamate receptors. Annual Review of Neuroscience 17: 31-108.
25. Hood W. F., Compton R. P. and Monahan J. B. (1989) D-Cycloserine: a ligand for the N-methyl-D-aspartate coupled glycine receptors has partial agonist characteristics. Neuroscience Letters 98: 91-95.
26. Jessa M., Nazar M., Bidzinski A. and Plaznik A. (1996a) The effects of repeated administration of diazeparn, MK-801 and CGP 37849 on rat behavior in two models of anxiety. European Neuropsychopharmacology 6: 55-61.
27. Jessa M., Nazar M. and Plaznik A. (1996b) Effects of intraaccumbens blockade of NMDA receptors in two models of anxiety, in rats. Neuroscience Research Communications 19: 19-25.
28. Kehne J. H., Baron B. M., Harrison B. L., McCloskey T. C., Palfreyman M. G., Poirot M., Salituro F. G., Siegel B. W., Slone A. L., Vangiersbergen P. L. M. and White H. S. (1995) MDL 100,458 and MDL 102,288: two potent and selective glycine receptor antagonists with different functional profiles. European Journal of Pharmacology 284: 109-118.
29. Kehne J. H., McCloskey T. C., Baron B. M., Chi E. M., Harrison B. L., Whitten J. P. and Palfreyman M. G. (1991) NMDA receptor complex antagonists have potential anxiolytic effects as measured with separation-induced ultrasonic vocalizations. European Journal of Pharmacology 193: 283-292.
30. Kemp J. A. and Priestley T. (1991) Effects of (+)-HA-966 and 7-chlorokynurenic acid on the kinetics of N-methyl-D-aspartate receptor agonist responses in rat cultured cortical neurons. Molecular Pharmacology 39: 666-670.
31. Koek W. and Colpaert F. C. (1990) Selective blockade of N-methyl-D-aspartate (NMDA)-induced convulsions by NMDA antagonists and putative glycine antagonists -relationship with phencyclidine-like behavioral effects. Journal of Pharmacology and Experimental Therapeutics 252: 349-357.
32. Koek W. and Colpaert F. C. (1991) Use of a conflict procedure in pigeons to characterize anxiolytic drug activity - evaluation of N-methyl-D-aspartate antagonists. Life Sciences 49: PL37-PL42.
33. Lanthorn T. H. (1994) D-Cycloserine: agonist turned antagonist. Amino Acids 6: 247-260.
34. Marvizon J. C. G., Lewin A. H. and Skolnick P. (1989) 1-Aminocyclopropane carboxylic acid: a potent and selective ligand for the glycine modulatory site of the N-methyl-D-aspartate receptor complex. Journal of Neurochemistry 52: 992-994.
35. Matheus M. G., Nogueira R. L., Carobrez A. P., Graeff F. G. and Guimaraes F. S. (1994) Anxiolytic effect of glycine antagonists microinjected into the dorsal periaqueductal grey. Psychopharmacology 113: 565-569.
36. McAllister K. H. (1990) Ethological analysis of the effects of MK-801 upon aggressive male mice: similarity to chlordiazepoxide. Pharmacology Biochemistry and Behavior 37: 101-106.
37. Moroni F., Alesiani M., Facci L., Fadda E., Skaper S. D., Galli A., Lombardi G., Mori F., Ciuffi M., Natalini B. and Pellicciari R. (1992) Thiokynurenates prevent excitotoxic neuronal death in vitro and in vivo by acting as glycine antagonists and as inhibitors of lipid peroxidation. European Journal of Pharmacology 218: 145-151.
38. Murata S. and Kawasaki K. (1993) Common and uncommon behavioural effects of antagonists for different modulatory sites in the NMDA receptor/channel complex. European Journal of Pharmacology 239: 9-15.
39. Newell D. W., Barth A. and Malouf A. T. (1995) Glycine site NMDA receptor antagonists provide protection against ischemia-induced neuronal damage in hippocampal slice cultures. Brain Research 675: 38-44.
40. Obrenovitch T. P. and Zilkha E. (1996) Inhibition of cortical spreading depression by L-701,324, a novel antagonist at the glycine site of the N-methyl-D-aspartate receptor complex. British Journal of Pharmacology 117: 931-937.
41. Palfreyman, M. G. and Baron, B. M. (1991) Non-competitive NMDA antagonists, acting on the glycine site. In Excitatory Amino Acid Antagonists, ed. B. S. Meldrum, pp. 101-129. Blackwell Scientific, Oxford.
42. Parsons, C. G., Danysz, W., Quack, G., Hartmann, S., Lorenz, B., Baran, L., Przegalinski, E., Kostowski, W., Krzascik, P., Headley, P. M. and Chizh, B. A. (1997) Novel systemically-active antagonists of the glycine site of the NMDA receptor - electrophysiological, biochemical and behavioural characterisation. Journal of Pharmacology and Experimental Therapeutics (in press).
43. Parsons C. G., Gruner R., Rozental J., Millar J. and Lodge D. (1993a) Patch clamp studies on the kinetics and selectivity of N-methyl-D-aspartate receptor antagonism by memantine (1-amino-3,5-dimethyladamantan). Neuropharmacology 32: 1337-1350.
44. Parsons C. G., Zong X. G. and Lux H. D. (1993b) Whole cell and single channel analysis of the kinetics of glycine-sensitive N-methyl-D-aspartate receptor desensitization. British Journal of Pharmacology 109: 213-221.
45. Pellegrini-Giampietro D. E., Cozzi A. and Moroni F. (1994) The glycine antagonist and free radical scavenger 7-cl-thiokynurenate reduces CA1 ischemic damage in the gerbil. Neuroscience 63: 701-709.
46. Pellow S. and File S. (1986) Anxiolytic and anxiogenic effects of drug effects on exploratory activity in an elevated plus-maze: novel test of anxiety in rats. Pharmacology Biochemistry and Behavior 24: 525-529.
47. Peterson S. L. and Schwade N. D. (1993) The anticonvulsant activity of d-cycloserine is specific for tonic convulsions. Epilepsy Research 15: 141-148.
48. Plaznik A., Palejko W., Nazar M. and Jessa M. (1994) Effects of antagonists at the NMDA receptor complex in two models of anxiety. European Neuropsychopharmacology 4: 503-512.
49. Priestley T. and Kemp J. A. (1994) Kinetic study of the interactions between the glutamate and glycine recognition sites on the n-methyl-D-aspartic acid receptor complex. Molecular Pharmacology 46: 1191-1196.
50. Przegalinski E., Tatarczynska E., Derenwesolek A. and Chojnackawojcik E. (1996) Anticonflict effects of a competitive NMDA receptor antagonist and a partial agonist at strychnine-insensitive glycine receptors. Pharmacology Biochemistry and Behavior 54: 73-77.
51. Rao T. S., Cler J. A., Compton R. P., Emmett M. R., Mick S., Sun E. T., Iyengar S. and Wood P. L. (1990) Neuropharmacological characterization of 1-aminocyclopropane-1-carboxylate and 1-aminocyclobutane-1-carboxylate, ligands of the N-methyl-D-aspartate-associated glycine receptor. Neuropharmacology 29: 305-309.
52. Rowley M., Leeson P. D., Stevenson G. I., Moseley A. M., Stansfield I., Sanderson I., Robinson L., Baker R., Kemp J. A., Marshall G. R., Foster A. C., Grimwood S., Tricklebank M. D. and Saywell K. L. (1993) 3-Acyl-4-hydroxyquinolin-2(1h)-ones - systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex. Journal of Medical Chemistry 36: 3386-3396.
53. Schmitt M. L., Coelho W., Lopesdesouza A. S., Guimaraes F. S. and Carobrez A. P. (1995) Anxiogenic-like effect of glycine and d-serine microinjected into dorsal periaqueductal gray matter of rats. Neuroscience Letters 189: 93-96.
54. Singh L., Donald A. E., Foster A. C., Hutson P. H., Iversen L. L., Iversen S. D., Kemp J. A., Leeson P. D., Marshall G. R., Oles R. J., Priestley T., Thorn L., Tricklebank M. D., Vass C. A. and Williams B. J. (1990) Enantiomers of HA-966 (3-amino-1-hydroxypyrrolid-2-one) exhibit distinct central nervous system effects: (+)-HA-966 is a selective glycine/ N-methyl-D-aspartate receptor antagonist, but (-)-HA-966 is a potent γ-butyrolactone-like sedative. Proceedings of the National Academy of Sciences U.S.A. 87: 347-351.
55. Skolnick P., Marvizon J. C. G., Jackson B. W., Monn J. A., Pice K. C. and Lewin A. P. (1989) Blockade of N-methyl-D-aspartate induced convulsions by 1-aminocyclopropanecarboxylates. Life Sciences 45: 1647-1656.
56. Smith R. D., Grzelak M. E. and Coffin V. L. (1994) Felbamate, a novel antiepileptic agent, does not affect cognition in rodents. Behavioural Pharmacology 5: 365-368.
57. Stephens D. N., Meldrum B. S., Weidmann R., Schneider C. and Grutzner M. (1986) Does the excitatory amino acid receptor antagonist 2-APH exhibit anxiolytic activity? Psychopharmacology 90: 166-169.
58. Trullas R., Folio T., Young A., Miller R., Boje K. and Skolnick P. (1991) 1-Aminocyclopropanecarboxylates exhibit anti-depressant and anxiolytic actions in animal models. European Journal of Pharmacology 203: 379-385.
59. Trullas R., Jackson B. and Skolnick P. (1989) Anxiolytic properties of 1-aminocyclopropanecarboxylic acid, a ligand at strychnine-insensitive glycine receptors. Pharmacology Biochemistry and Behavior 34: 313-316.
60. Turski L., Diedrichs S., Klockgether T., Schwarz M., Turski W. A., Sontag K. H., Bortolotto Z. A., Calderazzofiho L. S. and Cavalheiro E. A. (1991) Paradoxical anticonvulsant activity of the gamma-aminobutyrate antagonist bicuculline methiodide in the rats striatum. Synapse 7: 14-20.
61. Watson G. B., Bolanowski M. A., Baganoff M. P., Deppeler C. J. and Lanthorn T. H. (1989) Glycine antagonist action of 1-aminocyclobutane-1-carboxylate (ACBC) in Xenopus oocytes injected with rat brain mRNA. European Journal of Pharmacology 167: 291-294.
62. Watson G. B., Bolanowski M. A., Baganoff M. P., Deppeler C. L. and Lanthorn T. H. (1990) D-cycloserine acts as a partial agonist at the glycine modulatory site of the NMDA receptor expressed in Xenopus oocytes. Brain Research 510: 158-160.
63. Wiley J. L., Cristello A. F. and Balster R. L. (1995) Effects of site-selective NMDA receptor antagonists in an elevated plus-maze model of anxiety in mice. European Journal of Pharmacology 294: 101-107.
64. Willetts J., Balster R. L. and Leander J. D. (1990) The behavioral pharmacology of NMDA receptor antagonists. Trends in Pharmacological Sciences 11: 423-428.
65. Winslow J. T., Insel T. R., Trullas R. and Skolnick P. (1990) Rat pup isolation calls are reduced by functional antagonists of the NMDA receptor complex. European Journal of Pharmacology 190: 11-22.
66. Woodward R. M., Huettner J. E., Guastella J., Keana J. F. W. and Weber E. (1995) In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites. Molecular Pharmacology 47: 568-581.