Cinanserin hydrochloride

Cinanserin hydrochloride用途

Cinanserin hydrochloride (SQ 10643) 是一种有效,选择性和高度亲和力的 5-HT2 受体拮抗剂,Ki 为 41 nM。Cinanserin hydrochloride 对 5-HT2 的结合亲和力比对 5-HT1 受体 (Ki 为 3500 nM) 的结合亲和力高得多。Cinanserin hydrochloride 还是严重急性呼吸系统综合症冠状病毒的 3C 样蛋白酶 (3C-like proteinase) 的抑制剂,可大大减少体外的病毒复制。

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Cinanserin hydrochloride名称

[ CAS 号 ]:
54-84-2

[ 英文名 ]:
Cinanserin hydrochloride

[英文别名 ]:

maptc
Cinnanserin
sq10,643
CINANSERIN
DPTC HYDROCHLORIDE
DPTC

Cinanserin hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 抗感染 >> 流感病毒

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

Ki: 41 nM (5-HT2 receptor)[3]; 3C-like proteinase[1]

[体外研究]

辛那西林/盐酸辛那西林与SARS冠状病毒3CLpro、HCoV-229e3clpro具有结合亲和力,SARS冠状病毒3CLpro和人冠状病毒229E的KD分别为49.4μM/78.0μM和18.2μM/36.6μM[1]。计算了辛那西林和盐酸辛那西林抑制SARS-CoV 3CLpro催化活性的IC50值分别为4.92μM和5.05μM,HCoV-229e3clpro的IC50值分别为4.68μM和5.68μM,在200μM浓度范围内没有一种化合物对HRV-143cpro有抑制作用[1]。

[体内研究]

辛那西林(5mg/kg；静脉注射；2小时；雄性Wistar大鼠)治疗可显著降低全身烧伤水肿至shamburn水平。使用辛那西林后,白细胞与内皮细胞的相互作用显著降低[2]。动物模型：雄性Wistar大鼠(250g)遭受热损伤[2]剂量：5mg/kg给药：静脉注射；2小时结果：显著降低全身烧伤水肿至shamburn水平。。

[参考文献]

[1]. Chen L, et al. Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro. J Virol. 2005 Jun;79(11):7095-103.

[2]. Hernekamp JF, et al. Cinanserin reduces plasma extravasation after burn plasma transfer in rats. Burns. 2013 Sep;39(6):1226-33.

[3]. Leysen JE, et al. Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors. Life Sci. 1981 Mar 2;28(9):1015-22.

Cinanserin hydrochloride物理化学性质

[ 沸点 ]:
519.5ºC at 760mmHg

[ 分子式 ]:
C₂₀H₂₅ClN₂OS

[ 分子量 ]:
376.94300

[ 闪点 ]:
268ºC

[ 精确质量 ]:
376.13800

[ PSA ]:
57.64000

[ LogP ]:
5.25730

[ 储存条件 ]:
2-8°C，干燥，密封

Cinanserin hydrochloride毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GD7478000

CHEMICAL NAME :: Cinnamanilide, 2'-((3-(dimethylamino)propyl)thio)-, monohydrochloride

CAS REGISTRY NUMBER :: 54-84-2

LAST UPDATED :: 199709

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C20-H24-N2-O-S.Cl-H

MOLECULAR WEIGHT :: 376.98

WISWESSER LINE NOTATION :: 1N1&3SR BMV1U1R &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 480 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 8 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 152,132,1964