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The α2,3-selective potentiators of GABA<sub>A</sub> receptors, KRM-II-81 and MP-III-80, produce anxiolytic-like effects and block chemotherapy-induced hyperalgesia in mice without tolerance development.

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R-(-)-ketamine modifies behavioral effects of morphine predicting efficacy as a novel therapy for opioid use disorder<sup>1</sup>.

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The α2,3-selective potentiator of GABA<sub>A</sub> receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats.

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Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABA<sub>A</sub> receptors: Improved bioavailability enhances anticonvulsant efficacy.

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An antidepressant-related pharmacological signature for positive allosteric modulators of α2/3-containing GABA<sub>A</sub> receptors.

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Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABA<sub>A</sub> receptors.

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Obituary: J. David LEander, Ph.D. : (April 8, 1944-November 14, 2014)

J M Witkin1, S D Gleason, R B Carter

  • 1Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN, 46285-0501, USA, jwitkin@lilly.com.

Psychopharmacology
|February 21, 2015
PubMed
Summary

No abstract available in PubMed .

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