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Aligeron

Aligeron用途

Aligeron是一种非选择性的prostaglandin (PG)拮抗剂,具有舒张血管的作用。

Aligeron名称

[ CAS 号 ]:
70713-45-0

[ 中文名 ]:
Aligeron

[ 英文名 ]:
Aligeron

[英文别名 ]:

1-benzhydryl-4-allyl-piperazine
1-(Diphenylmethyl)-4-(2-propenyl)piperazine
Aligeron
1-allyl-4-benzhydryl-piperazine
Piperazine,1-(diphenylmethyl)-4-(2-propenyl)
1-(diphenylmethyl)-4-(prop-2-en-1-yl)piperazine

Aligeron生物活性

[ 描述 ]:

Aligeron是一种非选择性的prostaglandin (PG)拮抗剂,具有舒张血管的作用。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 心血管疾病

[体外研究]

Aligeron显示出对不同分离器官中不同的spasmogens的广谱拮抗作用。对离体灌注的兔动脉进行的实验显示了aligeron对去甲肾上腺素和肾上腺素的血管收缩作用的拮抗作用[1]。在体外,aligeron的作用缺乏选择性,可能是由于干扰Ca2 +的作用[3]。

[体内研究]

在通气不足缺氧时,喷嚏(5mg/kg静脉注射)和桂利嗪增加皮质对缺氧的抵抗并加速皮质生物电活动的恢复。在KCl和AMP诱导的抑郁症中,aligeron显示出保护作用,表现为抑郁程度和持续时间的减少[2]。

[参考文献]

[1]. Miyares K, et al. Antagonistic activity of aligeron and papaverine against different smooth muscle stimuli. Methods Find Exp Clin Pharmacol. 1985 Sep;7(9):473-6.

[2]. Dimov S, et al. Effect of aligeron and cinnarizine in models of general and local depression of the cortical bioelectrical activity in cats. Methods Find Exp Clin Pharmacol. 1983;5(2):89-95.

[3]. Nikolov R, et al. Study on the prostaglandin antagonistic activity of aligeron and piracetam. Methods Find Exp Clin Pharmacol. 1982 Aug-Sep;4(6):387-95.

[相关活性小分子]

Aligeron物理化学性质

[ 分子式 ]:
C₂₀H₂₄N₂

[ 分子量 ]:
292.41800

[ 精确质量 ]:
292.19400

[ PSA ]:
6.48000

[ LogP ]:
3.45540

[ 储存条件 ]:
2-8℃

Aligeron毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TL6655000

CHEMICAL NAME :: Piperazine, 1-(diphenylmethyl)-4-(2-propenyl)-

CAS REGISTRY NUMBER :: 70713-45-0

BEILSTEIN REFERENCE NO. :: 0543456

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C20-H24-N2

MOLECULAR WEIGHT :: 292.46

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 202 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,1103,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 38500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,1103,1987