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特比萘芬

特比萘芬用途

Terbinafine (TDT 067) 是治疗真菌感染的抗真菌药物。它是来自念珠菌属的角鲨烯环氧化酶有效的非竞争性抑制剂, Ki值为30 nM。

特比萘芬名称

[ CAS 号 ]:
91161-71-6

[ 中文名 ]:
特比萘芬

[ 英文名 ]:
Terbinafine

[中文别名 ]:

[英文别名 ]:

Lamasil
UNII-G7RIW8S0XP
S1725_Selleck
Terbinafine
Lamisil AT
Lamisil
Lamasil (TN)
SF-86-327
EINECS 245-385-8
MFCD00242672

特比萘芬生物活性

[ 描述 ]:

Terbinafine (TDT 067) 是治疗真菌感染的抗真菌药物。它是来自念珠菌属的角鲨烯环氧化酶有效的非竞争性抑制剂, Ki值为30 nM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

[ 靶点 ]

Ki: 30 nM (squalene epoxidase)[1]

[体外研究]

特比萘芬在体外对大多数真菌病原体具有主要的杀真菌作用,包括皮肤真菌,二形和丝状真菌。特比萘芬在角鲨烯环氧化作用下特异性地抑制真菌麦角甾醇的生物合成。处理过的真菌细胞迅速积累中间体角鲨烯并且缺乏麦角甾醇途径的最终产物[1]。

[体内研究]

特比萘芬不仅在局部施用后具有活性,而且在口服给药后对实验性皮肤癣菌非常有效。在真菌感染的豚鼠中,特比萘芬第四次治疗后皮肤温度急剧下降[2]。

[动物实验]

豚鼠：已经机械脱毛的豚鼠的背部（腰部）用含有106cfu的杜氏假丝酵母的0.1mL沙氏葡萄糖2％肉汤感染。接种后48小时开始治疗。将试验化合物（特比萘芬）悬浮于2％的tylose和吐温80中，连续9天每天一次通过胃管给药，或者溶解在聚乙二醇400和乙二醇的混合物中，并在身体的感染部位涂抹。用Hrigalski刮刀每天一次，连续1-7天，体积为0.4 mL [2]。

[参考文献]

[1]. Ryder NS, et al. Terbinafine: mode of action and properties of the squalene epoxidase inhibition. Br J Dermatol. 1992 Feb;126 Suppl 39:2-7.

[2]. Mieth H, et al. Preclinical evaluation of terbinafine in vivo. Clin Exp Dermatol. 1989 Mar;14(2):104-7.

[相关活性小分子]

特比萘芬物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
417.9±33.0 °C at 760 mmHg

[ 分子式 ]:
C₂₁H₂₅N

[ 分子量 ]:
291.430

[ 闪点 ]:
183.7±22.3 °C

[ 精确质量 ]:
291.198700

[ PSA ]:
3.24000

[ LogP ]:
6.61

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.586

[ 储存条件 ]:
室温，干燥

特比萘芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ8600000

CHEMICAL NAME :: 1-Naphthalenemethanamine, N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-, (E)-

CAS REGISTRY NUMBER :: 91161-71-6

LAST UPDATED :: 199709

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C21-H25-N

MOLECULAR WEIGHT :: 291.47

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 210 mg/kg/6W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Taste) - change in function

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,728,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3918 ug/kg

TOXIC EFFECTS :: Gastrointestinal - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,6087,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 200 mg/kg/40D-I

TOXIC EFFECTS :: Behavioral - anorexia (human) Liver - jaundice, cholestatic Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: JOHEEC Journal of Hepathology. (Elsevier Science, 655 Avenue of the Americas, New York, NY 10010) V.1- 1985- Volume(issue)/page/year: 24,753,1996

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4 gm/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,427,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 213 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: 53XPA8 "Proceedings of the International Congress of Chemotherapy, 13th, Vienna, 1983," Spitzy, K.H., and K. Karrer, eds., 18 vols., Vienna, Austria, Verlag H. Egermann, 1983 Volume(issue)/page/year: 6,116/52,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4 gm/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,427,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 393 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: 53XPA8 "Proceedings of the International Congress of Chemotherapy, 13th, Vienna, 1983," Spitzy, K.H., and K. Karrer, eds., 18 vols., Vienna, Austria, Verlag H. Egermann, 1983 Volume(issue)/page/year: 6,116/52,1983

特比萘芬安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37/39

[ 海关编码 ]:
2921499090

特比萘芬合成路线

详细合成路线

特比萘芬上下游产品

特比萘芬上游产品

特比萘芬下游产品

特比萘芬制备

以氯代叔丁烷和氯乙烷为原料，在三氯化铝存在下进行缩合反应。然后在氢氧化钾存在下，在二甲亚砜中高温加热，消去两分子的氯化氢。得到的物质先和乙基溴化镁在室温中反应，再和丙烯醛作用，生成6,6-二甲基-1-庚烯-4-炔-3-醇。最后溴代得顺反-1-溴-6,6-二甲基-2-庚烯-4-炔。将得到的产物和N-甲基-1-萘甲胺在碳酸钠作用下缩合，得特比萘芬和它的顺式异构体。两者可以用异丙醇重结晶来分离，也可用柱层析分离。

特比萘芬海关

[ 海关编码 ]: 2921499090

[ 中文概述 ]:
2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%