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BRIVARACETAM | BRIVARACETAM : Inhibitor of SV2A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SV2A
  • Kd:540 nM
  • IC50:80 nM
  • Kd:62 nM
  • INH:3.2 µM
  • Kd:152 ± 40 nM
Inhibitor
1–10 μM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Brivaracetam was profiled at 10 μM (a concentration > 100 fold higher than its affinity for SV2A) ag ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Results from SV2A−/− knock-out mice clearly show that up to concentrations of 600 nm, [3H]BRV specif ...

Potency
Cellular
In Vitro

SV2A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm030913e

In Vivo Validations

Rat
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 1.7 h
Systemic clearance: 4.67 mL/min/kg
Tmax: 0.5 h
Bioavailability: ~100%

DOI Reference: 10.1021/jm030913e

Chemical Information

Molecular Formula C11H20N2O2
SMILEs CCC[C@@H]1CC(=O)N([C@@H](CC)C(N)=O)C1
InChI InChI=1S/C11H20N2O2/c1-3-5-8-6-10(14)13(7-8)9(4-2)11(12)15/h8-9H,3-7H2,1-2H3,(H2,12,15)/t8-,9+/m1/s1
Molecular weight 212.15 Da
AlogP 0.0
HBond acceptors 4
HBond donors 2
Atoms 35

References

Publications

Cross References

canSARChEMBLBindingDB

Expert Reviews

by SERP
(on 7 Aug 2024 )
Cellular Use Rating
In Model Organisms
Matagne et al (2008) also dosed i.p. in various rat and mouse epilepsy models. Recommended dose would depend on the model but 10 mg/kg seems reasonable
by SERP
(on 24 Aug 2024 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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