Ocinaplon
Based on 1 Customer Validation
Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder.
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- Pureza: 99.58%
- No. CAS: 96604-21-6
- Fòrmula: C17H11N5O
- Peso molecular:301.30
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
GABAA receptor[1]
Ocinaplon acts as a low-affinity partial agonist at recombinant GABAA receptors[1].
Ocinaplon inhibits [3H]flunitrazepam binding to native GABAA receptors from rat cerebellar membranes with an IC50 of 1.2 μM, which is 3-fold more potent than its inhibition of binding to rat cortical membranes (IC50 3.8 μM)[2].
Ocinaplon (48 h) potentiates GABA-gated currents in 8 recombinant human GABAA receptor isoforms expressed in Xenopus laevis oocytes, with the highest relative efficacy (85% of diazepam) and an EC50 of 3.07 μM at the α1β2γ2S isoform, and lower efficacies at α2-, α3-, and α5-containing isoforms[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ocinaplon (9.6 mg/kg; p.o.; single dose; 1 hour pre-challenge) inhibits pentylenetetrazole-induced convulsions in rats with an oral ED50 of 9.6 mg/kg[2].
Ocinaplon (81.7-172.2 mg/kg; p.o.; single dose; 1 hour pre-test) impairs motor function in rats at oral ED50 values of 81.7 mg/kg (motor activity), 172.2 mg/kg (inclined screen), and 92 mg/kg (rod walking), which are 5- to 10-fold higher than its anxiolytic dose[2].
Ocinaplon (4-128 mg/kg; p.o.; single dose; 60 minutes pre-test) produces anxiolytic-like effects in squirrel monkeys at oral doses from 4 mg/kg to 64 mg/kg, with motor impairment-like effects only at the higher dose of 128 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD rats (male, 120-220 g)[2]
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Dosage:3.1 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Produced a statistically significant increase in punished responding (anxiolytic-like effect) comparable to diazepam.
Was fully blocked by flumazenil, eliminating its anticonflict effect.
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Animal Model:CD rats (male, 120-220 g)[2]
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Dosage:9.6 mg/kg
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Administration:p.o.; single dose; 1 hour pre-challenge
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Result:Exhibited anticonvulsant activity with an ED50 of 9.6 mg/kg, comparable in potency to diazepam.
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Animal Model:CD rats (male, 120-220 g)[2]
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Dosage:81.7 mg/kg (motor activity test); 172.2 mg/kg (inclined screen test); 92 mg/kg (rod walking test)
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Produced dose-dependent motor function deficits, with ED50 values of 81.7 mg/kg for reducing motor activity, 172.2 mg/kg for inclined screen failures, and 92 mg/kg for rod walking failures.
Was 5- to 10-fold less potent than diazepam in these motor impairment tests.
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Animal Model:Squirrel monkeys (adult male)[2]
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Dosage:4 mg/kg; 8 mg/kg; 16 mg/kg; 32 mg/kg; 64 mg/kg; 128 mg/kg
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Administration:p.o.; single dose; 60 minutes pre-test
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Result:Produced significant increases in punished responding at doses from 4 mg/kg to 64 mg/kg, with 4 mg/kg being the minimum effective dose.
Reduced both punished and unpunished responding at 128 mg/kg, with no overt sedation observed.
Chemical Information
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No. CAS 96604-21-6
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Appearance Solid
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Peso molecular 301.30
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Fòrmula C17H11N5O
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Color Light yellow to yellow
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SMILES
O=C(C1=NC=CC=C1)C2=C3N=CC=C(C4=CC=NC=C4)N3N=C2
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Synonyms
DOV 273547
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 2 mg/mL (6.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Czobor P, et al. A multicenter, placebo-controlled, double-blind, randomized study of efficacy and safety of ocinaplon (DOV 273,547) in generalized anxiety disorder. CNS Neurosci Ther. 2010;16(2):63-75. [Content Brief]
[2]. Lippa A, et al. Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator. Proc Natl Acad Sci U S A. 2005;102(20):7380-7385. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3190 mL | 16.5948 mL | 33.1895 mL | 82.9738 mL |
| 5 mM | 0.6638 mL | 3.3190 mL | 6.6379 mL | 16.5948 mL |
Ocinaplon Related Classifications
HY-W001692 Related Classifications
Powered by Bioz
- Ocinaplon
- 96604-21-6
- DOV 273547
- DOV273547
- DOV-273547
- GABA Receptor
- human α1β2γ3 isoform
- GABA-stimulated chloride currents
- GABAA receptor
- Xenopus laevis oocytes
- rat cerebellar membranes
- α1β2γ2S isoform
- human α1β2γ2 isoform
- generalized anxiety disorder
- pentylenetetrazole-induced convulsions
- rat cortical membranes
- Inhibitor
- inhibitor
- inhibit