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Bretazenil

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].

Product Specifications

CAS Number

84379-13-5

Product Name Alternative

Ro 16-6028

UNSPSC

12352005

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/bretazenil.html

Purity

99.13

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC(C)(C)OC(C1=C2N(C=N1)C3=CC=CC(Br)=C3C(N4[C@@]2([H])CCC4)=O)=O

Molecular Formula

C19H20BrN3O3

Molecular Weight

418.28

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Available Sizes

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