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. 1995 May 12;38(10):1826-30.
doi: 10.1021/jm00010a028.

Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations

V Kumar  1 , P M Carabateas, J A Dority Jr, W G Earley, J P Mallamo, C Subramanyam, L D Aimone, B Ault, D L DeHaven Hudkins, M S Miller
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Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations

V Kumar et al. J Med Chem. .

Abstract

Replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with thiazolium (4a and 4b) and N-methylimidazolium (4c and 4d) resulted in equipotent compounds in the [3H]TCP binding assay. The corresponding N-methyl-1,2,4-triazolium analogs were less potent in this assay. The thiazolium derivative 4b, with a Ki = 2.9 nM, is being evaluated as a possible neuroprotective N-methyl-D-aspartic acid (NMDA) antagonist.

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