Dizocilpine anticonvulsant

Determine the absolute configuration of the chirality centres in the anticonvulsant dizocilpine. 

NMDA-Glu-R antagonist [1] (antagonist Dizocilpine displacement) [1] (AD-R, mACh-R, D-R, 5HT-R, 5HT-TR, NE-TR, kO-R, V-D-TR, V-MA-TR) [anticonvulsant, CNS activity, hallucinogen, inhibits morphine dependence]... 

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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