Bretazenil 是一种有效的苯二氮卓，是γ-氨基丁酸受体的部分激动剂，IC50(特异性[35S]TBPS 结合 IC50) 为 6.1 nM。它对重组 α1β1γ2 的 EC50为 10 nM。Bretazenil 显示抗惊厥作用。

Bretazenil is a GABAA benzodiazepine site partial agonist. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2.

Bretazenil was the most potent benzodiazepine examined, exhibiting an IC50 of 6.1 nM, compared to clonazepam (7.9 nM), flunitrazepam (13.6 nM) and diazepam (91.1 nM). The rank order of potency for inhibition of [35S]TBPS binding was identical to that for inhibition of [3H]flunitrazepam binding. However, Bretazenil was less efficacious in that it produced 27% inhibition of specific [35S]TBPS binding, compared to clonazepam (34%), flunitrazepam (41%) or diazepam (49%). Bretazenil antagonized the inhibition of [35S]TBPS binding produced by 10 microM diazepam. Bretazenil was also more potent and less efficacious than diazepam in potentiating GABA-stimulated 36Cl- uptake[2].

Bretazenil, was studied in 240 rats in five age groups: age 7, 12, 18, 25 and 90 days. Motor seizures induced by metrazol (pentamethylenetetrazol, PTZ, 100 mg/kg subcutaneously (s.c.) except for 18-day-old rats which received a dose of 90 mg/kg) served as a model. Animals were pretreated with Bretazenil in doses of 0.001-0.1 mg/kg intraperitoneally 10 min before metrazol. Both types of metrazol-induced seizures, minimal (mMS, predominantly clonic with preserved righting ability) and major (MMS, generalized tonic-clonic), were suppressed by Bretazenil in a dose-dependent manner. Major seizures were always more sensitive to Bretazenil than were minimal seizures. The youngest rats exhibited maximal effects of Bretazenil against major seizures. On the other hand, this drug increased the incidence of minimal seizures in 7- and 12-day-old rats, i.e., in age groups in which this type of seizure is rare under control conditions[3].

84379-13-5

C19H20BrN3O3

418.28

Bretazenil

Ethanol:<41.83mg/mL
DMSO:<41.83mg/ml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years