The pharmacology of SDZ EAA 494, a competitive NMDA antagonist
作者： D.A. Lowe , M. Emre , P. Frey , P.H. Kelly , J. Malanowski
DOI: 10.1016/0197-0186(94)90157-0
关键词:
摘要: Abstract SDZ EAA 494 ( d -CPPene) was characterized as a competitive NMDA antagonist, having pA2 value against depolarizations in frog spinal cord and rat neocortex of 6.7–6.8 pKi 7.5 [3H]CGP39653 binding assay, with no action on other receptors or amine reuptake. The compound orally active rodent maximal electroshock models an ED50 around 16 mg/kg, protective rats even 24 hours after oral application had therapeutic index 8. Muscle relaxation, ataxia, flattened body posture reduced acquisition passive avoidance task, suggesting potential effects memory formation, occurred at supra-anticonvulsant doses rodents, PCP-like stimulatory produced only by high i.p. constant i.v. infusions. This favourable profile is discussed relation to the negative outcome recent trial patients intractable epilepsy. conclusion drawn that standard for screening new anticonvulsants are inappropriate seeking drugs protracted convulsive history. anti-ischaemic encourages further testing brain trauma, which anticonvulsant may be added benefit.
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