Bretazenil_product_DataBase

Bioactivity

Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects[1][2][3].

In Vivo

Bretazenil (0.001-0.1 mg/kg intraperitoneally 10 min before metrazol; age 7, 12, 18, 25 and 90 days male and female albino rats)suppresses both types of metrazol-induced seizures, minimal (mMS, predominantly clonic with preserved righting ability) and major (MMS, generalized tonic-clonic) in a dose-dependent manner[3].

Name

Bretazenil

CAS

84379-13-5

Formula

C19H20BrN3O3

Molar Mass

418.28

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Puia G, et al. Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at gamma-aminobutyric acid type A receptor. Proc Natl Acad Sci U S A. 1992;89(8):3620-3624. [2]. Finn DA, et al. A comparison of Ro 16-6028 with benzodiazepine receptor 'full agonists' on GABAA receptor function. Eur J Pharmacol. 1993;247(3):233-237. [3]. Kubová H, et al. Anticonvulsant effects of bretazenil (Ro 16-6028) during ontogenesis. Epilepsia. 1993;34(6):1130-1134.

PeptideDB

Bretazenil

CAS: 84379-13-5 F: C19H20BrN3O3 W: 418.28