Anticonvulsants NMDA receptor antagonists

Parsons, C. G., Quack, G., Bresink, I., Baran, L., Przegalinski, E., Kostowski, W., Krzascik, P., Hartmann, S., Danysz, W. 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, Neuropharmacology 1995, 34, 1239-1258. 

Priese A, SeiUer E, Quack G, Lorenz B, Kreuter J (2000) Increase of the duration of the anticonvulsive activity of a novel NMDA receptor antagonist using poly(butylcyanoacrylate) nanoparticles as a parenteral controlled release system. Eur J Pharm Biopharm 49 103-109. 

Gaoni, Y, Chapman, A.G., Parvez, N., Pook, P.C.K., Jane, D.E., and Watkins, J.C., Synthesis, NMDA receptor antagonist activity, and anticonvulsant action of 1-aminocyclobutanecarboxylic acid derivatives, J. Med. Chem., 37, 4288, 1994. 

Lbscher, W., Honack, D., 1993. Effects of the competitive NMDA receptor antagonist, CGP-37849, on anticonvulsant activity and adverse effects of valproate in amygdala-kindled rats. Eur. J. Pharmacol. 234, 237-245. 

APV (2-amino-5-phosphonopentanoic acid) is a competitive (NMDA) GLUTAMATE RECEPTOR ANTAGONIST which has anticonvulsant/antiepileptic actions. It is used as a pharmacological tool. 

RECEPTOR ANTAGONIST (channel-blocking at NMDA receptors). It is an OPIOID ANALGESIC, (dissociate) GENERAL ANAESTHETIC, PSYCHOTROPIC and ANTICONVULSANT. It iS a drug of abuse and has been withdrawn from human clinical use. etidocaine [ban, inn, usan] (Duranest ) is an amide series LOCAL ANAESTHETIC, used by injection for infiltration and regional pain relief. 

The quadracyclic ( )-5-aminocarbonyl-10,ll-dihydro-5H-dibenzo[a,c ]cyclohepten-5,10-imine (ADCI,47), results from the fusion of two active anticonvulsant compounds, MK 801 (dizocilpine,46), a potent noncompetitive NMDA antagonist (224, 225) and carbamazepine (2). The compound acts as a selective, low affinity channel blocker of the NMDA receptor and also possesses Na" channel-blocking activity (226). ADCI is devoid of the tendency to cause behavioral impairment as MK 801. ADCI is a racemate, although the (- -)-enantiomer displays a four- to fivefold greater potency at the NMDA receptor and a greater than twofold potency for seizure models in animals. There was no enantioselectivity in the Na" channel evaluation, however. The (- -)-enantiomer (SGB-017)is currently in Phase II of clinical development. 

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