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Datasheet of Brivaracetam

Description:
Brivaracetam(UCB-34714) is a 4-substituted pyrrolidone butanamide as agent with significant antiepileptic activity; high affinity
SV2A ligand and also shows an ability to inhibit Na+ channels. in vitro: Brivaracetam has been tested in a comprehensive safety
pharmacology, toxicology, developmental toxicology, and genotoxicity program. It is of low acute toxicity, target organ for toxic
effects is the hepatobiliary tract. Carcinogenicity studies are ongoing. Human pharmacology studies have shown that
brivaracetam has a half-life of 8 h and nearly complete bioavailability. CSD episodes were regularly elicited on slices upon
delivery of calibrated KCl drops and were recorded via two micropipette electrodes. After control CSDs, the drug was added to
the perfusion and five subsequent CSDs were elicited during drug perfusion. Effects were assessed via CSD amplitude (Ampl)
and duration at half-amplitude (D(1/2)). BRV, 10 and 32 microM reduced the Ampl and transiently the D(1/2). Levetiracetam, 32
and 100 microM had no effect on either Ampl or D(1/2). Brivaracetam bound selectively with 20 fold higher affinity than
levetiracetam to SV2A. BRV produced a concentration-dependent inhibition of voltage-dependent Na(+) currents with IC(50)
values of 41microM at the holding potential of -100mV, and of 6.5microM at the holding potential of -60mV. in vivo: BRV (2.1,
6.8 or 21.0mg/kg i.p.) was injected daily, 60min before each session. Results indicated that in both normal and amygdala-kindled
rats BRV did not alter the latency to find the hidden platform or swimming speed during the four consecutive days of learning.
brivaracetam (0.3 mg/kg, the minimal effective dose) was more potent than levetiracetam (3 mg/kg, the minimal effective dose)
against post-hypoxic seizures.The anti-seizure activity of both compounds occurred 30 min following intraperitoneal (i.p.)
administration and was maintained over the entire 150 min post-dose observation period. Both brivaracetam and levetiracetam
significantly reduced auditory stimulated post-hypoxic myoclonus from a dose 0.3 mg/kg.

Chemical Information
Catalog

DC9535

Purity of current batch:

>98%

Molecular Weight (MW)

212.29

Molecular Formula

C11H20N2O2

CAS No.

357336-20-0

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.