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Description: Positive allosteric modulator of GABAA; acts at benzodiazepine site
Alternative Names: NBI 34060
Chemical Name: N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide
Purity: ≥99% (HPLC)
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
| M. Wt | 376.43 |
| Formula | C20H16N4O2S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 325715-02-4 |
| PubChem ID | 6450813 |
| InChI Key | CBIAWPMZSFFRGN-UHFFFAOYSA-N |
| Smiles | CN(C(C)=O)C1=CC=CC(C3=CC=NC2=C(C(C4=CC=CS4)=O)C=NN23)=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.82 | 50 |
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 |
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References
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
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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:
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
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
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