Indiplon
Chemical Name: N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide
Purity: ≥99%
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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors.
Soderhielm et al.
Biochem.Pharmacol., 2018;158:339 -
Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.
Sullivan et al.
J.Pharmacol.Exp.Ther., 2004;311:537 -
In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic.
Foster et al.
J.Pharmacol.Exp.Ther., 2004;311:547 -
Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors.
Petroski et al.
J.Pharmacol.Exp.Ther., 2006;317:369
Product Datasheets
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Citations for Indiplon
The citations listed below are publications that use Tocris products. Selected citations for Indiplon include:
2 Citations: Showing 1 - 2
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Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors.
Authors: Soderhielm Et al.
Biochem Pharmacol 2018;158:339
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CB1 cannabinoid receptor stimulation during adolescence impairs the maturation of GABA function in the adult rat prefrontal cortex.
Authors: Cass Et al.
Mol Psychiatry 2014;19:536
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