Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor

SJ Hays, PM Novak, DF Ortwine, CF Bigge…

文献索引：Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670

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被引用次数: 13

摘要

PCP, is a potent antagonist at this site (IC60= 30 nM for displacement of [3HlTCP). On the basis of this finding, a number of derivatives encompassing variations in stereochemistry, amine substitution and position, aromatic and aliphatic ring substitution, and heteroatom ring substitution have been prepared to explore the structure-activity relationships around this ring system. All compounds were evaluated for their PCP receptor affinity; potent ...