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Ro15-4513

Ro15-4513用途

Ro15-4513 是咪唑并苯二氮酮衍生物,是苯二氮卓受体 (BZR) 的部分反向激动剂。Ro15-4513 是有效的乙醇拮抗剂。Ro15-4513 具有抗焦虑作用。

Ro15-4513名称

[ CAS 号 ]:
91917-65-6

[ 英文名 ]:
Ro 15-4513

[英文别名 ]:

Tocriscreen Total

Ro15-4513生物活性

[ 描述 ]:

Ro15-4513 是咪唑并苯二氮酮衍生物,是苯二氮卓受体 (BZR) 的部分反向激动剂。Ro15-4513 是有效的乙醇拮抗剂。Ro15-4513 具有抗焦虑作用。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[ 靶点 ]

BZR[1]; ethanol[2];

[体外研究]

Ro15-4513通常作为GABAA受体的部分反激动剂,但含有α4和α6亚单位的激动剂除外[3]。

[体内研究]

Ro 15-4513(i.p.；3 mg/kg；试验前10 min)完全抑制乙醇诱导的(1.8 g/kg)总运动活性降低,部分抑制饲养的降低[2]。Ro 15-4513(1.5 g/kg乙醇给药前15 min；3 mg/kg)逆转乙醇诱导的GABAA受体δ亚单位缺陷小鼠的镇静作用[2]。动物模型：雄性C57BL/6J小鼠[2]剂量：3 mg/kg给药：I.p.；给药前10 min。结果：完全抑制乙醇诱导的小鼠总运动活性降低,部分抑制饲养。

[参考文献]

[1]. Bonetti EP, et al. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav. 1988 Nov;31(3):733-49.

[2]. Suzdak PD, et al. Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-inducedintoxication in the rat. J Pharmacol Exp Ther. 1988 Jun;245(3):880-6.

[3]. Linden AM, et al. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3.

Ro15-4513物理化学性质

[ 分子式 ]:
C₁₅H₁₄N₆O₃

[ 分子量 ]:
326.31000

[ 精确质量 ]:
326.11300

[ PSA ]:
114.18000

[ LogP ]:
1.96706

[ 储存条件 ]:
2-8°C，密封，干燥，避光

Ro15-4513MSDS

详细MSDS(安全技术说明书)

Ro15-4513安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

Ro15-4513文献

Rats with different thresholds for DMCM-induced clonic convulsions differ in the sleep-time of diazepam and [(3)H]-Ro 15-4513 binding.

Epilepsy Res. 98(2-3) , 216-22, (2012)

The current study investigated the possible inherent relationship between convulsions and sleep involving the GABA(A)/benzodiazepine site complex. The aim of this study was to determine if rats with h...

Antagonism of the ethanol-like discriminative stimulus effects of ethanol, pentobarbital, and midazolam in cynomolgus monkeys reveals involvement of specific GABA(A) receptor subtypes.

J. Pharmacol. Exp. Ther. 331(1) , 142-52, (2009)

The gamma-aminobutyric acid (GABA)(A) receptors mediating the discriminative stimulus effects of ethanol were studied by comparing the potency of ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazol(1...

Modulation of diazepam-insensitive GABA(A) receptors by micromolar concentrations of thyroxine and related compounds in vitro.

Brain Res. 1490 , 1-8, (2013)

The effects of thyroxine and its related compounds on the benzodiazepine-insensitive γ-aminobutyric acid type A (GABA(A)) receptors were studied. Thyroxine at micromolar concentrations potentiated the...

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