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Updated: Apr 18, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Published on: August 16, 2018

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GABAA receptor partial agonists and antagonists: structure, binding mode, and pharmacology

Jacob Krall1, Thomas Balle2, Niels Krogsgaard-Larsen3

  • 1Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.

Advances in Pharmacology (San Diego, Calif.)
|January 21, 2015
PubMed
Summary

Developing selective GABA-A receptor (GABAAR) antagonists is crucial for understanding brain inhibition. This review explores structural classes of GABAAR antagonists and their potential for subtype selectivity.

Keywords:
4-PIOLGABA(A) receptor antagonistsGABA(A) receptor partial agonistsGABA(A) receptorsReceptor homology modelsStructure–activity relationship studiesTonic inhibition

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