Faculty Opinions recommendation of Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain.

2009 ◽  
Author(s):  
Hanns Ulrich Zeilhofer ◽  
Ilja Broll
Keyword(s):  
Neuropathic Pain ◽  
Gabaa Receptor ◽  
Allosteric Modulator ◽  
The Novel ◽  
Methyl Ethyl ◽  
Positive Allosteric Modulator ◽  
Rat Models ◽  
Subtype Selective

scholarly journals Effects of the α2/α3-subtype-selective GABAA receptor positive allosteric modulator KRM-II-81 on pain-depressed behavior in rats

2019 ◽  
Vol 30 (5) ◽  
pp. 452-461 ◽  
Author(s):  
Megan J. Moerke ◽  
Guanguan Li ◽  
Lalit K. Golani ◽  
James Cook ◽  
S. Stevens Negus
Keyword(s):  
Gabaa Receptor ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Subtype Selective

scholarly journals Pharmacology in translation: the preclinical and early clinical profile of the novel α2/3 functionally selective GABAA receptor positive allosteric modulator PF-06372865

2018 ◽  
Vol 175 (4) ◽  
pp. 708-725 ◽  
Author(s):  
Sarah A Nickolls ◽  
Rachel Gurrell ◽  
Guido van Amerongen ◽  
Juha Kammonen ◽  
Lishuang Cao ◽  
...  
Keyword(s):  
Gabaa Receptor ◽  
Clinical Profile ◽  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator

scholarly journals A Comparison of the 2/3/5 Selective Positive Allosteric Modulators L-838,417 and TPA023 in Preclinical Models of Inflammatory and Neuropathic Pain

2011 ◽  
Vol 2011 ◽  
pp. 1-12 ◽  
Author(s):  
Sarah Nickolls ◽  
Hannah Mace ◽  
Rebecca Fish ◽  
Michelle Edye ◽  
Rachel Gurrell ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Side Effect ◽  
Allosteric Modulator ◽  
Allosteric Modulators ◽  
Side Effect Profile ◽  
Preclinical Models ◽  
Positive Allosteric Modulator ◽  
Pain Medications ◽  
Pain Models ◽  
Subtype Selective

receptors containingα2/3 subunits are current targets in the battle to develop new pain medications, as they are expressed in the spinal cord where increasing inhibitory drive should result in analgesia. However, this approach is prone to a range of side effects including sedation, cognitive impairment, and abuse as a consequence of the widespread influence of GABA. The ability to make subtype selective low-efficacy benzodiazepine compounds, which potentiate the action of GABA at specificαsubunits, has the potential to reduce this side effect profile. In this study, we have investigated the effects of the medium-efficacy positive allosteric modulator (PAM) L-838,417 and the low-efficacy PAM TPA023 in a number of preclinical inflammatory and neuropathic pain models. We conclude that either the higher level of efficacy atα2/3 or efficacy atα5 is required for compounds to have a significant analgesic effect in a range of models, and, therefore, although the side-effect profile of compounds can be reduced compared to typical benzodiazepines, it is unlikely that it can be completely eliminated.

scholarly journals Antinociceptive Effects of a Novel α2/α3-Subtype Selective GABAAReceptor Positive Allosteric Modulator

2017 ◽  
Vol 8 (6) ◽  
pp. 1305-1312 ◽  
Author(s):  
Lakeisha A. Lewter ◽  
Janet L. Fisher ◽  
Justin N. Siemian ◽  
Kashi Reddy Methuku ◽  
Michael M. Poe ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Antinociceptive Effects ◽  
Subtype Selective

Efficacy and side effects of baclofen and the novel GABAB receptor positive allosteric modulator CMPPE in animal models for alcohol and cocaine addiction

2018 ◽  
Vol 235 (7) ◽  
pp. 1955-1965 ◽  
Author(s):  
Valentina Vengeliene ◽  
Tatiane T. Takahashi ◽  
Olga A. Dravolina ◽  
Irina Belozertseva ◽  
Edwin Zvartau ◽  
...  
Keyword(s):  
Side Effects ◽  
Animal Models ◽  
Gabab Receptor ◽  
Cocaine Addiction ◽  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator

Characterization of the Novel Positive Allosteric Modulator, LY2119620, at the Muscarinic M2and M4Receptors

2014 ◽  
Vol 86 (1) ◽  
pp. 106-115 ◽  
Author(s):  
Carrie H. Croy ◽  
Douglas A. Schober ◽  
Hongling Xiao ◽  
Anne Quets ◽  
Arthur Christopoulos ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
The Novel ◽  
Positive Allosteric Modulator
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