期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 19, 页码 6872-6878出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.08.029
关键词
[(3)H]Strychnine binding; (Nor)tropeines; Binding heterogeneity; 5-HT(3) receptors
资金
- Hungarian Science Research Fund OTKA [K 62203]
Heteroaromatic carboxylic esters of (nor) tropine were synthesized. Tropine esters displaced [(3)H]strychnine binding to glycine receptors of rat spinal cord with low Hill slopes. Two-site displacement resulted in nanomolar IC(50,1) and micromolar IC(50,2) values, and IC(50,2)/IC(50,1) ratios up to 615 depending on the heteroaromatic rings and N-methyl substitution. Nortropeines displayed high affinity and low heterogeneity. IC(50,1) and IC(50,2) values of tropeines did not correlate suggesting different binding modes/sites. Glycine potentiated only the nanomolar displacement reflecting positive allosteric interactions and potentiation of ionophore function. Affinities of three (nor) tropeines were different for glycine receptors but identical for 5-HT(3) receptors. (C) 2009 Elsevier Ltd. All rights reserved.
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