Indiplon Is a High-Affinity Positive Allosteric Modulator with Selectivity for α1 Subunit-Containing GABAA Receptors

  title={Indiplon Is a High-Affinity Positive Allosteric Modulator with Selectivity for $\alpha$1 Subunit-Containing GABAA Receptors},
  author={Robert E. Petroski and Jordan E. Pomeroy and Ronnie Das and Heath Bowman and Weidong Yang and Adele Pin Chen and Alan Carl Foster},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={369 - 377}
Indiplon (NBI 34060) is a novel pyrazolopyrimidine currently in development for the treatment of insomnia. We have previously shown that indiplon exhibits high-affinity binding to native GABAA receptors from rat brain and acts as a positive allosteric modulator of GABAA receptor currents in cultured rat neurons (Sullivan et al., 2004). In this study, we examined the GABAA receptor α subunit selectivity of indiplon using electrophysiological techniques to record GABA-activated chloride currents… 

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