Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.

doi:10.1016/S0960-894X(99)00542-9

Paper

Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.

Published Nov 1, 1999 · M. Chebib, G. Johnston, J. Mattsson

Bioorganic & medicinal chemistry letters

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3

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Abstract

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In Vitro Study

Study Snapshot

4-(Aminomethyl)-2,6-difluorophenol is a competitive and selective antagonist at 1 GABA C receptors, a novel class of increased lipophilicity GABA C receptor antagonists with little activity at 122 GABA A and B receptors.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.

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References

GABAC receptor antagonists differentiate between human ρ1 and ρ2 receptors expressed in Xenopus oocytes

The antagonist profiles of human recombinant 1 and 2 GABA C receptors show significant differences, highlighting the need for further research on their roles in neurotransmitter regulation.

Unsaturated phosphinic analogues of γ-aminobutyric acid as GABAC receptor antagonists

Unsaturated phosphinic analogues of -aminobutyric acid (GABA) are potent GABA C receptor antagonists, but even more potent as GABA B receptor agonists.

Design and in vitro pharmacology of a selective gamma-aminobutyric acidC receptor antagonist.

TPMPA is a selective gamma-aminobutyric acidC receptor antagonist that can be used to investigate their function in the outer retina and other nervous system areas.

THE FIRST SELECTIVE ANTAGONIST FOR A GABAC RECEPTOR

TMPPA is the first selective antagonist for mammalian GABA C receptors, offering potential therapeutic applications in treating neurodegenerative diseases.

Structure-reactivity correlations for reactions of substituted phenolate anions with acetate and formate esters

Substituted phenolate anions with acetate and formate esters show nonlinear BrOnsted-type correlations, supporting a concerted mechanism for both acetyl- and formyl-transfer reactions.

Citations

(3-Aminocyclopentyl)methylphosphinic acids: Novel GABAC receptor antagonists

()-cis -3- and ()-trans -3-ACPMPA show potential as potent and selective GABA C receptor antagonists with increased lipophilicity for in vivo studies.

A quantitative structure–activity relationship investigation into agonist binding at GABAC receptors

The QSAR model effectively predicts GABA C agonist binding, providing a reliable alternative to gain insight into its three-dimensional structure.