A-methyl-D-aspartate antagonists

A -methyl-D-aspartate antagonists Dextromethorphan Limited number of drugs in this class are available for human use. Study findings have been negative. 

Albers G. W., Atkinson R. R, Kelley R. E., and Rosenbaum D. M. (1995). Safety, tolerability, and pharmacokinetics of the A-methyl-D-aspartate antagonist dextrorphan in patients with acute stroke. Dextrorphan Study Group. Stroke 26 254-258. 

Dibenzo[a,c/]cycloalkenimines were synthesized and pharmacologically evaluated as A/-methyl-D-aspartate antagonists by P.S. Anderson et al. A symmetrical 3,7-difluoro derivative was accessed by applying the Balz-Schiemann reaction on the corresponding 3,7-diamino analog. 

Farfel, G.M. Vosmer, G.L. and Seiden, L.S. The A-methyl-D-aspartate antagonist MK-801 protects against serotonin depletions induced by methamphetamine, 3,4-methylenedioxymethamphetamine and / -chloroamphetamine. Brain Res 595 121-127, 1992. 

Kamei J, Ogawa M, Kasuya Y (1987) Monoamine and the mechanisms of action of antitussive drugs in rats. Arch Int Pharmacodyn 290 117-127 Kamei J, Tanihara H, Igarashi H, Kasuya Y (1989) Effects of A-methyl-D-aspartate antagonists on the cough reflex. Eur J Pharmacol 168 153-158... 

Stump, G.L., Lynch, J.J., Macaulay, A., Wafford, K.A., Koblan, K.S. and Liverton, N.J. (2004) NR2B-selective N-methyl-D-aspartate antagonists synthesis and evaluation of 5-substituted benzimidazoles. Journal of Medicinal Chemistry, 47, 2089-2096. 

Malhotra et al. [66] modelled the route of administration-based enhancement of delivery of EAB 515, a hydrophilic N-methyl-D-aspartate antagonist, to the brain. 

In this chapter, we use the term cognitive enhancers to refer to two classes of pharmacological agents used in the treatment of Alzheimer s disease the cholinesterase inhibitors and the A-methyl-D-aspartate (NMDA) receptor antagonists. 

Thieno[2,3-, ]pyridinones, 159, act as inhibitors of [ H]glycine binding to the A -methyl-D-aspartate (NMDA) receptor. The effects of substitution patterns on reactivity have been studied, leading to thienopyridinones with activity comparable to known quinolinone antagonists <2006JME864>. 

Chizh, B. A., Schlutz, H., Scheed, M., Englberger, W. The N-methyl-D-aspartate antagonistic and opioid components of D-methadone antinociception in the rat spinal cord, Neurosci. Lett. 2000, 296, 117-120. 

Ebert, B., Andersen, S Hjeds, H., Dickenson, A. H. Dextropropoxyphene acts as a noncompetitive N-methyl-D-aspartate antagonist, J. Pain Symptom Manage. 1998, 15, 269-274. 

CGP68730A a N-methyl-D-aspartate antagonist acting at the strychnine-insensitive glycine site, Prog. Neuropsychopharmacol. Biol. Psychiatry 2000, 24, 547-670. 

Turski L., Bressler K., Rettig K.-J., Loschmann P.-A., and Wachtel H. (1991). Protection of substantia nigra from MPP+ neurotoxicity by N-methyl-D-aspartate antagonists. Nature 349 414 117. 

Paul C. and Bolton C. (2002). Modulation of blood-brain barrier dysfunction and neurological deficits during acute experimental allergic encephalomyelitis by the A-methyl-D-aspartate receptor antagonist memantine. J. Pharmacol. Exp. Ther. 302 50-57. 

Beister A, Kraus P, Kuhn W, Dose M, Weindl A, Gerlach M (2004) The N-methyl-D-aspartate antagonist memantine retards progression of Huntington s disease. J Neural Transm Suppl 117-122. 

Minematsu K, Fisher M, Li L, Sotak CH (1993b) Diffusion and perfusion magnetic resonance imaging studies to evaluate a noncompetitive N-methyl-D-aspartate antagonist and reperfusion in experimental stroke in rats. Stroke 24 2074-2081... 

Buchan A. and Pulsinelli W. A. (1990) Hypothermia but not the N-methyl-D-aspartate antagonist, MK-801, attenuates neuronal damage in gerbils subjected to transient global ischemia. J. Neurosci. 10, 311-316. 

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