scholarly journals The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain

2016 ◽  
Vol 173 (16) ◽  
pp. 2506-2520 ◽  
Author(s):  
Deniz Bagdas ◽  
Jenny L Wilkerson ◽  
Abhijit Kulkarni ◽  
Wisam Toma ◽  
Shakir AlSharari ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Mouse Models ◽  
Nicotinic Receptor ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator

scholarly journals A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects

2015 ◽  
Vol 40 (13) ◽  
pp. 2948-2959 ◽  
Author(s):  
Bogna M Ignatowska-Jankowska ◽  
Gemma L Baillie ◽  
Steven Kinsey ◽  
Molly Crowe ◽  
Sudeshna Ghosh ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Cb1 Receptor ◽  
Allosteric Modulator ◽  
Cannabinoid Cb1 Receptor ◽  
Positive Allosteric Modulator ◽  
Psychoactive Effects

A positive allosteric modulator of mGluR5 promotes neuroprotective effects in mouse models of Alzheimer's disease

2019 ◽  
Vol 160 ◽  
pp. 107785 ◽  
Author(s):  
Paula Maria Quaglio Bellozi ◽  
Giovanni Freitas Gomes ◽  
Maria Carolina Machado da Silva ◽  
Isabel Vieira de Assis Lima ◽  
Carla Ribeiro Álvares Batista ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mouse Models ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Neuroprotective Effects

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.

Sign in / Sign up

Export Citation Format

Share Document