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Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.

Abstract：

: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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Maksay G,Vincze Z,Nemes P

doi

10.1016/j.bmc.2009.08.029

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

6872-8

issue

19

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00791-3

journal_volume

17

pub_type

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