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康里新

康里新用途

Conessine是一种甾体生物碱,对人、狗、豚鼠和大鼠H3受体的Kis分别为5.4、6.0、5.7和25 nM,是一种有效和选择性的组胺H3受体拮抗剂。抗疟疾活动[1]。

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康里新名称

[ CAS 号 ]:
546-06-5

[ 中文名 ]:
止泻木碱

[ 英文名 ]:
Conessine

[中文别名 ]:

[英文别名 ]:

3β-(Dimethylamino)con-5-enine
3-β-(Dimethylamino)con-5-enine
CONESSIN
Conessine
Con-5-enin-3-amine, N,N-dimethyl-, (3β)-
Konessin
ROGUESSINE
Conessine,N,N-Dimethyl-con-5-enin-3-amine
(3β)-N,N-Dimethylcon-5-enin-3-amine
ROQUESSINE

康里新生物活性

[ 描述 ]:

Conessine是一种甾体生物碱,对人、狗、豚鼠和大鼠H3受体的Kis分别为5.4、6.0、5.7和25 nM,是一种有效和选择性的组胺H3受体拮抗剂。抗疟疾活动[1]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 感染

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H3 Receptor:5.4 nM (Ki)

rat H3 receptor:25 nM (Ki)

Guinea pig H3 Receptor:6.0 nM (Ki)

Dog H3 Receptor:5.7 nM (Ki)

[参考文献]

[1]. Santora VJ, et al. A new family of H3 receptor antagonists based on the natural product Conessine. Bioorg Med Chem Lett. 2008;18(4):1490-1494.

[2]. Kim H, et al. Conessine treatment reduces dexamethasone-induced muscle atrophy by regulating MuRF1 and atrogin-1 expression [published online ahead of print, 2018 Feb 1]. J Microbiol Biotechnol. 2018;10.4014.jmb.1711.11009.

康里新物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
450.4±45.0 °C at 760 mmHg

[ 熔点 ]:
126-127ºC

[ 分子式 ]:
C₂₄H₄₀N₂

[ 分子量 ]:
356.588

[ 闪点 ]:
199.6±16.5 °C

[ 精确质量 ]:
356.319153

[ PSA ]:
6.48000

[ LogP ]:
5.71

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.564

[ 储存条件 ]:
-20°C，密闭，干燥

康里新MSDS

详细MSDS(安全技术说明书)

康里新毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GK7621000

CHEMICAL NAME :: Con-5-enine, 3-beta-(dimethylamino)-

CAS REGISTRY NUMBER :: 546-06-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C24-H40-N2

MOLECULAR WEIGHT :: 356.66

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 208 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 58,373,1936

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 138 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 58,373,1936

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康里新安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26

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

[ RTECS号 ]:
GK7621000

康里新文献

[New orientation and new therapeutic weapons in the therapy of intestinal amebiasis].

Minerva Med. 43(59-60) , 129-33, (1952)

Highly enantioselective construction of fused pyrrolidine systems that contain a quaternary stereocenter: concise formal synthesis of (+)-conessine.

Angew. Chem. Int. Ed. Engl. 43(19) , 2543-6, (2004)

High-performance thin layer chromatography method for estimation of conessine in herbal extract and pharmaceutical dosage formulations.

J. Pharm. Biomed. Anal. 46(2) , 391-4, (2008)

A new, simple, sensitive, precise and robust high-performance thin layer chromatographic (HPTLC) method was developed for the estimation of conessine in herbal extracts and pharmaceutical dosage forms...

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