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Abecarnil
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Abecarnil图片
CAS NO: 111841-85-1
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 名称
ZK 112119
半岛bd体育手机客户端 介绍
Abecarnil (ZK 112119) 是一种 benzodiazepine (BZ)受体的配体或部分激动剂。Abecarnil 具有抗焦虑和抗惊厥的特性。Abecarnil 可作为 GABAA受体的正变构调节剂。Abecarnil 可抑制 BZ [3H]lormetazepam 与大鼠大脑皮层膜的结合，其 IC50为 0.82 nM。Abecarnil 可用于癫痫的研究。
生物活性

Abecarnil (ZK 112119) is a ligand or a partial agonist forbenzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator ofGABAAreceptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with anIC50of 0.82 nM. Abecarnil can be used for epilepsy research[1][2][3][4].
体外研究
(In Vitro)

Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes[1].
Abecarnil exhibits a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP)[1].
体内研究
(In Vivo)

Abecarnil (0.3 mg/kg, IP, once) antagonizes the brain neuroactive steroid increase induced by foot shock[2].
Abecarnil (0-2.5 mg/kg, IP, once) dose dependently reduces epileptic activity[3].
Abecarnil is effective against sound-induced convulsions in DBA/2 mice, against air blast-induced generalized seizures in gerbils and against myoclonus in baboons Papio papio[4].
Abecarnil is 2-10 times more potent than DZP in most rodent tests of anxiolytic activity, and in reducing locomotor activity in mice and rats thoroughly habituated to the test chamber[1].

Animal Model: Male Sprague-Dawley CD rats (200-250 g)[2]
Dosage: 0.3 mg/kg
Administration: IP, once, given 30 min before sacrifice
Result: Failed to change the basal pregnenolone and progesterone, while only slightly decreased THDOC levels, but antagonized the brain neuroactive steroid increase induced by foot shock.
Animal Model: WAG/Rij rats (male and female, 190-380 g, age 13-19 weeks, 8 rats each group)[3]
Dosage: 0, 0.16, 0.4, 1.0, and 2.5 mg/kg; 1 mL/400 g
Administration: IP, once
Result: Reduced the duration of spike-wave discharges and increased immobile behavior. Dose dependently reduced epileptic activity, whether measured as number, mean duration, or total duration of spike-wave discharges. The ED50for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg.
分子量

404.46
Formula

C24H24N2O4
CAS 号

111841-85-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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