Indiplon
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.
Compound Libraries
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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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.82 | 50 | |
| ethanol | 1.88 | 5 |
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.66 mL | 13.28 mL | 26.57 mL |
| 5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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References
References are publications that support the products' biological activity.
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
If you know of a relevant reference for Indiplon, please let us know.
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Keywords: Subtype-selective GABAA receptor positive allosteric modulators Receptors NBI34060 NBI 34060 GABAA Receptors
Citations for Indiplon
Citations are publications that use Tocris products.
Currently there are no citations for Indiplon. Do you know of a great paper that uses Indiplon from Tocris? If so please let us know.
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