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62232-46-6

中文名称 Bifemelane HCl
英文名称 Bifemelane HCl
CAS 62232-46-6
分子式 C18H23NO.ClH
分子量 305.847
MOL 文件 62232-46-6.mol
更新日期 2024/08/19 13:26:56
62232-46-6 结构式 62232-46-6 结构式

基本信息

中文别名
盐酸双芬麦兰
4-(2-苄基苯氧基)-N-甲基丁-1-胺盐酸盐
化合物BIFEMELANE HYDROCHLORIDE
英文别名
Bifemelane HCl
Bifemelan hydrochloride
Bifemelane hydrochloride
MEAHDXWXNNDSAK-UHFFFAOYSA-N
4-(2-Benzylphenoxy)-N-methylbutan-1-amine hydrochloride
inhibit,Inhibitor,Monoamine Oxidase,MAO-A,MAO,MCI 2016,Bifemelane hydrochloride,antidepressant,Bifemelane,monoamine,MCI-2016,MCI2016,oxidase,MAO-B
所属类别
生物化工:抑制剂

物理化学性质

熔点117-121°
溶解度Soluble to 100 mM in water and to 100 mM in DMSO
形态粉末
颜色White to yellow

安全数据

毒性LD50 in mice, rats (mg/kg): 1000, 1080 orally; 173, 130 i.p. (Tobe, 1981)

常见问题列表

生物活性
Bifemelane hydrochloride (MCI-2016) 是一种有效,选择性和竞争性的单胺氧化酶 A (MAO-A) 抑制剂,Ki 值为 4.20 μM,它也非竞争性地抑制 MAO-B,Ki 为 46.0 μM。Bifemelane hydrochloride 具有很强的抗抑郁活性,可用于研究与脑血管疾病有关的认知和情绪障碍。
靶点

MAO-A

4.2 μM (Ki)

MAO-B

46 μM (Ki)

体外研究

Bifemelane inhibits MAO-A in a dose-dependent manner, with K i s of 4.2±0.2 and 14.1±0.7 μM in human brain synaptosomes and human liver mitochondria respectively.
Bifemelane inhibits MAO-B activities in a dose-dependent manner, with K i s of 46.0±3.6 and 65.2±7.0 μM in human brain synaptosomes and human liver mitochondria respectively.

体内研究

Bifemelane (20-80 mg/kg; i.p.) dose-dependently decreases exploratory activity in the open field test.
Bifemelane (20-80 mg/kg; i.p.) decreases immobility time in the forced swim test, although is not clearly dosedependent and has already reached ceiling at 20 mg/kg.

Animal Model: Wistar male rats (230-270 g) are induced hypothermia by Reserpine
Dosage: 20, 40, 80 mg/kg
Administration: A single i.p.
Result: Attenuated the Reserpine-induced hypothermia by a maximum of 10 ℃.
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