Bioorganic & medicinal chemistry

Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors

G Maksay, Z Vincze, P Nemes

文献索引：Maksay, Gabor; Vincze, Zoltan; Nemes, Peter Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 19 p. 6872 - 6878

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被引用次数: 2

摘要

Heteroaromatic carboxylic esters of (nor) tropine were synthesized. Tropine esters displaced [3H] strychnine binding to glycine receptors of rat spinal cord with low Hill slopes. Two-site displacement resulted in nanomolar IC50, 1 and micromolar IC50, 2 values, and IC50, 2/IC50, 1 ratios up to 615 depending on the heteroaromatic rings and N-methyl substitution. Nortropeines displayed high affinity and low heterogeneity. IC50, 1 and IC50, 2 values of ...