Novel NMDA antagonists: replacement of the pyridinium ring of 6, 11-ethanobenzo [b] quinolizinium cations with heteroisoquinolinium cations
…, JA Dority Jr, WG Earley, JP Mallamo…
文献索引:Kumar, Virendra; Carbateas, Phil M.; Dority, John A.; Earley, William G.; Mallamo, John P.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1826 - 1830
Replacement of the pyridinium ring of 6, 11-ethanobenzo [blquinolizinium cations with thiazolium (4a and 4b) and N-methylimidazolium (4c and 4d) resulted in equipotent compounds in the I3H1TCP 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) ...