84379-13-5
Chemical Structure
Bretazenil
Synonym(s): Ro 16-6028
- CAS No.: 84379-13-5
- Formula:C19H20BrN3O3
- Molecular Weight:418.28
IUPAC Name: tert-butyl (S)-8-bromo-9-oxo-11,12,13,13a-tetrahydro-9H-benzo[e]imidazo[5,1-c]pyrrolo[1,2-a][1,4]diazepine-1-carboxylate
InChIKey: LWUDDYHYYNNIQI-ZDUSSCGKSA-N
SMILES: CC(C)(C)OC(C1=C2N(C=N1)C3=CC=CC(Br)=C3C(N4[C@@]2([H])CCC4)=O)=O
Biological Activity: 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].
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Bretazenil | 99.13% | 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. | ||||||||||||||||||||
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Bretazenil (Standard) | ≥98% | Bretazenil (Standard) is the analytical standard of Bretazenil (HY-105056). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [3]. Kubová H, et al. Anticonvulsant effects of bretazenil (Ro 16-6028) during ontogenesis. Epilepsia. 1993;34(6):1130-1134. [Content Brief]
