Low affinity channel blocking (uncompetitive) NMDA receptor antagonists as therapeutic agents - Toward an understanding of their favorable tolerability

Amino Acids

Volumn 19, Issue 1, 2000, Pages 133-149

  Rogawski, M A ^a  

^a NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE   (United States)

Author keywords

Amino acids; NMDA Receptors antagonists

Indexed keywords

DIZOCILPINE; KETAMINE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; PHENCYCLIDINE;

BINDING AFFINITY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SYNTHESIS; DRUG TOLERABILITY; HUMAN; MENTAL DISEASE; NEUROLOGIC DISEASE; NONHUMAN; PRIORITY JOURNAL; REVIEW; TREATMENT INDICATION;

ANIMAL; BINDING SITES; EXCITATORY AMINO ACID ANTAGONISTS; KINETICS; NERVOUS SYSTEM DISEASES; PROTEIN BINDING; RECEPTORS, N-METHYL-D-ASPARTATE;

ANIMALIA;

EID: 0033800566     PISSN: 09394451     EISSN: None     Source Type: Journal    
DOI: 10.1007/s007260070042     Document Type: Review

References (71)

1. The NMDA antagonist model for schizophrenia: Promise and pitfalls
2. The dissociative anaesthetics, ketamine and phencyclidine, selectively reduce excitation of central mammalian neurones by N-methyl-aspartate
3. Efficacy of felbamate in childhood epileptic encephalopathy (Lennox-Gastaut syndrome). The felbamate study group in Lennox-Gastaut syndrome
4. Novel adamantane derivatives act as blockers of open ligand-gated channels and as anticonvulsants
5. WIN 63480, a hydrophilic TCP-site ligand, has reduced agonist-independent NMDA ion channel access compared to MK-801 and phencyclidine
6. AntagOnist properties of eliprodil and other NMDA receptor antagonists at rat NR1A/NR2A and NR1A/NR2B receptors expressed in Xenopus oocytes
7. Progress report on new antiepileptic drugs: A summary of the fourth Eilat conference (EILAT IV)
8. Anticonvulsant 1-phenylcycloalkylamines: Two analogs with low motor toxicity when orally administered
9. Trapping channel block of NMDA-activated responses by amantadine and memantine
10. Effects of memantine on recombinant rat NMDA receptors expressed in HEK 293 cells
11. Behavioural pharmacology of the non-competitive NMDA antagonists dextrorphan and ADCI: Relations between locomotor stimulation, anticataleptic potential and forebrain dopamine metabolism
12. Antagonists selective for NMDA receptors containing the NR2B subunit
13. Low-frequency activation of the NMDA receptor system can prevent the induction of LTP
14. Multiple actions of arylalkylamine arthropod toxins on the N-methyl-D-aspartate receptor
15. Novel benzo [b]quinolizinium cations as uncompetitive N-methyl-D-aspartic acid (NMDA) antagonists: The relationship between log D and agonist independent (closed) NMD A channel block
16. Clinical experience with oral ketamine
17. Structural determinants of the blocker binding site in glutamate and NMDA receptor channels
18. Neuronal vacuolization and necrosis induced by the noncompetitive N-methyl-D-aspartate (NMDA) antagonist MK(+)801 (dizocilpine maleate): A light and electron microscopic evaluation of the rat retrosplenial cortex
19. 2+ in hippocampal slices
20. Comparison of the effects of the uncompetitive N-methyl-D-aspartate antagonist (±)-5-aminocarbonyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (ADCI) with its structural analogs dizocilpine (MK-801) and carbamazepine on ethanol withdrawal seizures
21. Dizocilpine-like discriminitive stimulus effects of low affinity uncompetitive NMDA antagonists
22. NMDA Receptor channel block by the enantiomeric 6,7-benzomorphans BIII 277 CL and BIII 281 CL
23. NMDA-receptor channel blocker heterogeneity
24. Channel block of NMDA receptors by the anticonvulsant ADCI: Studies with cloned NR1a/NR2A and NR1a/NR2B subunits
25. Felbamate block of recombinant N-methyl-D-aspartate receptors in a human cell expression system
26. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: Selective binding to open channels
27. Brain uptake and biotransformation of remacemide hydrochloride, a novel anticonvulsant
28. Effects of anticonvulsants in a novel operant learning paradigm in rats: Comparison of remacemide hydrochloride and FPL 15896AR to other anticonvulsant agents
29. 3H]MK-801 binding: Evidence for access to closed and open N-methyl-D-aspartate receptor channels
30. Noncompetitive antagonists of excitatory amino acid receptors
31. Subtype-selective antagonism of N-methyl-D-aspartate receptors by felbamate: Insights into the mechanism of action
32. Kinetic characterization of the phencyclidine-N-methyl-D-aspartate receptor interaction: Evidence for a steric blockade of the channel
33. 3H]dibenzocycloal-kenimine (MK-801) to the N-methyl-D-aspartate (NMDA) receptor and its therapeutic implication
34. Differences in degree of trapping between AR-R15986 and other uncompetitive NMDA receptor antagonists
35. Cerestat and other NMDA antagonists in ischemic stroke
36. GABA and neuroprotection
37. Differences in degree of trapping of low-affinity uncompetitive N-methyl-D-aspartic acid receptor antagonists with similar kinetics of block
38. Antagonism of N-methyl-D-aspartate-evoked currents in rat cortical cultures by ARL 15896AR
39. NR1 and NR2 subunit contributions to N-methyl-D-aspartate receptor channel blocker pharmacology
40. Molecular determinants of NMDA receptor pharmacological diversity
41. Structure and function of the NMDA receptor channel
42. Clinical experience with excitatory amino acid antagonist drugs
43. [S]-AR-R 15896AR - A novel anticonvulsant: Acute safety, pharmacokinetic and pharmacodynamic properties
44. Glutamate in CNS disorders as a target for drug development: An update
45. Amino-alkyl-cyclohexanes are novel uncompetitive NMDA receptor antagonists with strong voltage-dependency and fast blocking kinetics: In vitro and in vivo characterization
46. Memantine is a clinically well tolerated NMDA receptor antagonist - A review of preclinical data
47. Memantine and the amino-alkyl-cyclohexane MRZ 2/579 are moderate affinity uncompetitive NMDA receptor antagonists - In vitro characterization
48. Comparison of the potency, kinetics and voltage-dependency of a series of uncompetitive NMDA receptor antagonists in vitro with anticonvulsive and motor impairment activity in vivo
49. Electrophysiological actions of felbamate on rat striatal neurones
50. ADCI, a novel anticonvulsant, does not impair avoidance or spatial learning in the rat
51. Mechanism of action of the anticonvulsant felbamate: Opposing effects on N-methyl-D-aspartate and γ-aminobutyric acid(A) receptors
52. Therapeutical potential of excitatory amino acid antagonists: Channel blockers and 2,3-benzodiazepines
53. Epilepsy
54. Mechanism-specific pathways for new antiepileptic drug discovery
55. Piperidine ring modified phencyclidine analogs retain PCP's anticonvulsant activity with a reduction in motor side effects
56. Anticonvulsant activity of the low affinity uncompetitive N-methyl-D-aspartate antagonist (±)-5-aminocarbonyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5,10-imine (ADCI): Comparison with the structural analogs dizocilpine (MK-801) and carbamazepine
57. Anticonvulsant efficacy of ADCI (5-aminocarbonyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine) after acute and chronic dosing in mice
58. Evaluation of ADCI against convulsant and locomotor stimulant effects of cocaine: Comparison with the structural analogs dizocilpine and carbamazepine
59. Two blocking sites of amino-adamantane derivatives in open N-methyl-D-aspartate channels
60. Felbamate block of the N-methyl-D-aspartate receptor
61. Block of the N-methyl-D-aspartate receptor by remacemide and its des-glycine metabolite
62. Discovery of 6,11-ethano-12,12-diaryl-6,11-dihydrobenzo[b]quinoliznium cations, a novel class of N-methyl-D-aspartate antagonists
63. Synthesis and anticonvulsant activities of 1-phenylcyclohexylamine analogs
64. Felbamate neuroprotection against CA1 traumatic neuronal injury
65. Remacemide HCl and its metabolite, FPL 12495AA, limit action potential firing frequency and block NMDA responses of mouse spinal cord neurons in cell culture
66. Posthypoxic treatment with felbamate is neuroprotective in a rat model of hypoxia-ischemia
67. The broad spectrum anticonvulsant ADCI blocks TTX sensitive voltage-activated Na channel currents in NE1-115 mouse neuroblastoma cells
68. Pharmacological properties of ketamine
69. The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist
70. Different sensitivities of NMDA receptor channel subtypes to non-competitive antagonists