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(±)-SDZ-201 106

(±)-SDZ-201 106用途

DPI 201-106(SDZ 201106)是一种强心剂,具有协同肌膜和细胞内作用机制。DPI 201-106显示了对电压门控钠通道(VGSC)的心脏选择性调节,从而产生正性肌力效应[1][2][3]。

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(±)-SDZ-201 106名称

[ CAS 号 ]:
97730-95-5

[ 中文名 ]:
SDZ-201106(±),(DPI-201106)

[ 英文名 ]:
DPI 201-106

[英文别名 ]:

Dpi 201-106

(±)-SDZ-201 106生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 心血管疾病

[ 靶点 ]

Sodium Channel[3]

[体外研究]

DPI 201-106增加了猪隔缘小梁皮肤纤维的Ca2+敏感性,EC50为0.2 nM[2]。DPI 201-106在豚鼠和大鼠左心房、小猫、兔和豚鼠乳头肌以及0.1至3μM之间的兔Langendorff灌注心脏中产生浓度依赖性正性肌力效应[2]。

[体内研究]

在麻醉狗中,DPI 201-106 0.2 mg/kg静脉注射增加了左心室dP/dtmax。在地高辛预处理的麻醉猫中,DPI 201-106静脉注射的累积剂量为12.22 mg/kg[3]。

[参考文献]

[1]. G Scholtysik, et al. DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn Schmiedebergs Arch Pharmacol.1985 May;329(3):316-25.

[2]. G Scholtysik, et al. Interaction of DPI 201-106 with cardiac glycosides. J Cardiovasc Pharmacol. 1989 Feb;13(2):342-7.

[3]. M Mevissen, et al. Identification of a cardiac sodium channel insensitive to synthetic modulators. J Cardiovasc Pharmacol Ther. 2001 Apr;6(2):201-12.

(±)-SDZ-201 106物理化学性质

[ 密度 ]:
1.29g/cm3

[ 沸点 ]:
702.6ºC at 760mmHg

[ 分子式 ]:
C₂₉H₃₀N₄O₂

[ 分子量 ]:
466.57400

[ 闪点 ]:
378.7ºC

[ 精确质量 ]:
466.23700

[ PSA ]:
75.52000

[ LogP ]:
4.06228

[ 折射率 ]:
1.692

[ 储存条件 ]:
-20°C，密闭，干燥

(±)-SDZ-201 106毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NL5993340

CHEMICAL NAME :: 1H-Indole-2-carbonitrile, 4-(3-(4-(diphenylmethyl)-1-piperazinyl)-2-hydroxyprop oxy-, (+-)-

CAS REGISTRY NUMBER :: 97730-95-5

LAST UPDATED :: 199512

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C29-H30-N4-O2

MOLECULAR WEIGHT :: 466.63

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

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

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 40 mg/kg

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

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5600 mg/kg

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

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 47 mg/kg

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

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987