L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor. L-701,324 produced a marked increase in the seizure threshold, which was significantly reversed by the administration of glycine[3]. In contrast to N-methyl-D-aspartate receptor ion channel blockers such as MK-801 (dizocilpine), L-701,324 is a potent, p.o. active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents[4]. L-701324 (2.5-40 mg/kg, i.p.) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg, i.p.). L-701324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia[5]. Pretreatment with L-701,324 dose-dependently antagonized amphetamine-induced hyperactivity in the mouse (ED50 = 1.12 +/- 0.45 mg/kg p.o.), an effect which was similar to that of the classical neuroleptic, haloperidol, and the atypical neuroleptic, clozapine. In addition, p.o. administration of L-701,324 (2.5 or 5 mg/kg) attenuated the hyperactivity response induced by amphetamine infusion into the rat nucleus accumbens. L-701,324 failed to impair spontaneous locomotor activity or induce catalepsy in the mouse at doses > or = 100 mg/kg[6]. Moreover, anticonvulsant and neuroprotective actions of L-701,324 may not be associated with marked anaesthesia-like side-effects[7].
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