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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 376.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.31 mL||26.57 mL||53.13 mL|
|2.5 mM||1.06 mL||5.31 mL||10.63 mL|
|5 mM||0.53 mL||2.66 mL||5.31 mL|
|25 mM||0.11 mL||0.53 mL||1.06 mL|
References are publications that support the biological activity of the product.
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
Foster et al (2004) In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J.Pharmacol.Exp.Ther. 311 547 PMID: 15256538
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
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 158 339 PMID: 30121248
If you know of a relevant reference for Indiplon, please let us know.
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Keywords: Indiplon, Indiplon supplier, Subtype-selective, GABAA, receptor, positive, allosteric, modulators, Receptors, NBI34060, PAM, NBI, 34060, 3597, Tocris Bioscience
2 Citations for Indiplon
Citations are publications that use Tocris products. Selected citations for Indiplon include:
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248
Cass et al (2014) CB1 cannabinoid receptor stimulation during adolescence impairs the maturation of GABA function in the adult rat prefrontal cortex. Mol Psychiatry 19 536 PMID: 24589887
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.