IndiplonCat. No. 3597 |
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Alternative Name: NBI 34060 Chemical Name: N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide |
Biological Activity
Potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively). Displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6, 24, 60 and 77 nM for α1β2γ2, α2β2γ2, α3β3γ2 and α5β2γ2 receptors respectively). Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.Certificate of Analysis / Safety Data Sheet
References
Foster et al (2004) In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J.Pharmacol.Exp.Ther. 311 547. PMID: 15256538.
Sullivan et al (2004) Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. J.Pharmacol.Exp.Ther. 311 537. PMID: 15256540.
Petroski et al (2006) Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors. J.Pharmacol.Exp.Ther. 317 369. PMID: 16399882.
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Keywords: Indiplon, supplier, Subtype-selective, GABAA, receptor, positive, allosteric, modulators, Receptors, NBI34060
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