2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Ocinaplon

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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Ocinaplon

Ocinaplon Chemical Structure

CAS No. : 96604-21-6

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Ocinaplon Related Antibodies

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Description

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[1][2].

IC50 & Target

GABAA receptor[1]
In Vitro

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 Related Antibodies
In Vivo

Ocinaplon (3.1 mg/kg; p.o.; single dose; 1 hour pre-test) produces a Flumazenil (HY-B0009)-sensitive anxiolytic effect in the thirsty rat conflict test[2].
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.

Animal Model: CD rats (male, 120-220 g)[2]
Dosage: 3.1 mg/kg
Administration: p.o.; single dose; 1 hour pre-test
Result: Produced a statistically significant increase in punished responding (anxiolytic-like effect) comparable to diazepam.
Was fully blocked by flumazenil, eliminating its anticonflict effect.
Animal Model: CD rats (male, 120-220 g)[2]
Dosage: 9.6 mg/kg
Administration: p.o.; single dose; 1 hour pre-challenge
Result: Exhibited anticonvulsant activity with an ED50 of 9.6 mg/kg, comparable in potency to diazepam.
Animal Model: CD rats (male, 120-220 g)[2]
Dosage: 81.7 mg/kg (motor activity test); 172.2 mg/kg (inclined screen test); 92 mg/kg (rod walking test)
Administration: p.o.; single dose; 1 hour pre-test
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.
Animal Model: Squirrel monkeys (adult male)[2]
Dosage: 4 mg/kg; 8 mg/kg; 16 mg/kg; 32 mg/kg; 64 mg/kg; 128 mg/kg
Administration: p.o.; single dose; 60 minutes pre-test
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.
Molecular Weight

301.30

Formula

C17H11N5O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC=CC=C1)C2=C3N=CC=C(C4=CC=NC=C4)N3N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3190 mL 16.5948 mL 33.1895 mL
5 mM 0.6638 mL 3.3190 mL 6.6379 mL
View the 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.

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Purity & Documentation
References

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
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Ocinaplon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ocinaplon96604-21-6DOV 273547DOV273547DOV-273547GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorhuman α1β2γ3 isoformGABA-stimulated chloride currentsGABAA receptorXenopus laevis oocytesrat cerebellar membranesα1β2γ2S isoformhuman α1β2γ2 isoformgeneralized anxiety disorderpentylenetetrazole-induced convulsionsrat cortical membranesInhibitorinhibitorinhibit

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