A PK/PD study on antihyperalgesia by an α2/3‐GABA <sub>A</sub> receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABA <sub>A</sub> receptors

Antihyperalgesic effects of TPA023B do not undergo tolerance development. Besides γ2-GABA<sub>A</sub>Rs, γ1-GABA<sub>A</sub>Rs appear to contribute to the antihyperalgesic effects of TPA023B. γ1-GABA<sub>A</sub>R selective PAMs may hence have a therapeutic potential in chronic pain conditions.

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Publication Details

Journal
British Journal of Pharmacology
Published
2026-01-06
DOI
https://doi.org/10.1111/bph.70301
Primary Topic
Neuroscience and Neuropharmacology Research
Type
article
Field-Weighted Citation Impact
0.00

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article

A PK/PD study on antihyperalgesia by an α2/3‐GABA A receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABA A receptors

Thomas Grampp, Dietmar Benke, Hanns Ulrich Zeilhofer, M. Oana Popa et al.
British Journal of Pharmacology
Neuroscience and Neuropharmacology Research
article

A PK/PD study on antihyperalgesia by an α2/3‐GABA A receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABA A receptors

Thomas Grampp, Dietmar Benke, Hanns Ulrich Zeilhofer, M. Oana Popa, Thomas Hathaway, Marcus Hanley, Daniel Ulrich, Karen T Elvers, Gui Jie Feng, Elena Neumann, John R. Atack, Misa Oyama, William T. Ralvenius
article en

Abstract

Antihyperalgesic effects of TPA023B do not undergo tolerance development. Besides γ2-GABA<sub>A</sub>Rs, γ1-GABA<sub>A</sub>Rs appear to contribute to the antihyperalgesic effects of TPA023B. γ1-GABA<sub>A</sub>R selective PAMs may hence have a therapeutic potential in chronic pain conditions.

British Journal of Pharmacology
University of Zurich (CH), ETH Zurich (CH), University Hospital of Zurich (CH), University of Wales Institute Cardiff (SG), École Polytechnique Fédérale de Lausanne (CH), Cardiff University (GB)
Deutsche Forschungsgemeinschaft, Universität Zürich, Medical Research Council
Openalex Percentile: Top 95%
Neuroscience and Neuropharmacology Research
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A PK/PD study on antihyperalgesia by an α2/3‐GABA <sub>A</sub> receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABA <sub>A</sub> receptors — Thomas Grampp, Dietmar Benke, et al. · British Journal of Pharmacology (2026) | TGRS Research Map | TGRS