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Pharmacological And Antihyperalgesic Properties Of The Novel Α2/3 Preferring Gabaa Receptor Ligand Mp-Iii-024., Bradford D. Fischer, Raymond J. Schlitt, Bryan Z. Hamade, Sabah Rehman, Margot Ernst, Michael M. Poe, Guanguan Li, Revathi Kodali, Leggy A. Arnold, James M. Cook
Pharmacological And Antihyperalgesic Properties Of The Novel Α2/3 Preferring Gabaa Receptor Ligand Mp-Iii-024., Bradford D. Fischer, Raymond J. Schlitt, Bryan Z. Hamade, Sabah Rehman, Margot Ernst, Michael M. Poe, Guanguan Li, Revathi Kodali, Leggy A. Arnold, James M. Cook
Bradford Fischer
γ-Aminobutyric acid type A (GABAA) receptors are located in spinal nociceptive circuits where they modulate the transmission of pain sensory signals from the periphery to higher centers. Benzodiazepine-type drugs bind to GABAA receptors containing α1, α2, α3, and α5 subunits (α1GABAA, α2GABAA, α3GABAA and α5GABAA receptors, respectively) through which they inhibit the transmission of these signals. In the present study we describe the novel benzodiazepine site positive allosteric modulator modulator methyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate (MP-III-024). MP-III-024 displayed preference for α2GABAA and α3GABAA receptors relative to α1GABAA and α5GABAA receptors as well as an improved metabolic profile relative to subtype-selective positive modulators that are available currently. Administration of …