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曲洛司坦

曲洛司坦用途

Trilostane(Win 24540; Modrastane)是3 β-羟化类固醇脱氢酶抑制剂，可作用于库兴氏综合征。

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曲洛司坦名称

[ CAS 号 ]:
13647-35-3

[ 中文名 ]:
曲洛斯坦

[ 英文名 ]:
Trilostane

[中文别名 ]:

[英文别名 ]:

MODRASTANE
2a-Cyano-4a,5a-epoxyandrostan-17b-ol-3-one
Desopan
Trilostane
MFCD00199295
Modrenal
Modrefen
Vetoryl
EINECS 237-133-0
Trilostane(Win 24540; Modrastane)

曲洛司坦生物活性

[ 描述 ]:

Trilostane(Win 24540; Modrastane)是3 β-羟化类固醇脱氢酶抑制剂,可作用于库兴氏综合征。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 内分泌

[参考文献]

[1]. Helm JR, et al. A comparison of factors that influence survival in dogs with adrenal-dependent hyperadrenocorticism treated with mitotane or trilostane. J Vet Intern Med. 2011 Mar-Apr;25(2):251-60.

[2]. Feldman EC, et al. Trilostane dose versus body weight in the treatment of naturally occurring pituitary-dependent hyperadrenocorticism in dogs. J Vet Intern Med. 2012 Jul-Aug;26(4):1078-80.

[相关活性小分子]

曲洛司坦物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
497.8±45.0 °C at 760 mmHg

[ 熔点 ]:
264ºC

[ 分子式 ]:
C₂₀H₂₇NO₃

[ 分子量 ]:
329.433

[ 闪点 ]:
254.8±28.7 °C

[ 精确质量 ]:
329.199097

[ PSA ]:
76.78000

[ LogP ]:
3.61

[ 外观性状 ]:
黄褐色晶体

[ 蒸汽压 ]:
0.0±2.9 mmHg at 25°C

[ 折射率 ]:
1.610

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：不溶；微溶：二甲基甲酰胺；极微溶：甲醇,乙醇；不溶：二乙醚,氯仿

曲洛司坦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BV8044200

CHEMICAL NAME :: 5-alpha-Androstane-2-alpha-carbonitrile, 4-alpha,5-epoxy-17-beta-hydroxy-3-oxo-

CAS REGISTRY NUMBER :: 13647-35-3

LAST UPDATED :: 199603

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C20-H27-N-O3

MOLECULAR WEIGHT :: 329.48

WISWESSER LINE NOTATION :: T E5 D6663 1A R AX PV RO QHTTTT&J HQ I1 M1 OCN

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 :: >15 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,752,1990

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1055 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 37,1637,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7050 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,365,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 102 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,365,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >15 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,752,1990

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1205 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 37,1637,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >15 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,752,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 109 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 17,365,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 54750 mg/kg/1Y-I

TOXIC EFFECTS :: Cardiac - pulse rate Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 37,1637,1986 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 48 mg/kg

SEX/DURATION :: male 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,754,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1050 mg/kg

SEX/DURATION :: male 7 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,754,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 mg/kg

SEX/DURATION :: female 25-29 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 32,464,1979

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曲洛司坦安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H361

[ 警示性声明 ]:
P281-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38-62

[ 安全声明 (欧洲) ]:
26-36/37

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

[ 海关编码 ]:
2937290090

曲洛司坦海关

[ 海关编码 ]: 2937290090

曲洛司坦文献

Disturbances in production of progesterone and their implications in plant studies.

Steroids 96 , 153-63, (2015)

Progesterone is a mammalian hormone that has also been discovered in plants but its physiological function in plants is not explained. Experiments using inhibitors of progesterone synthesis and bindin...

Guanosine triphosphate can directly regulate cortisol production by activating Ca(2+)-messenger systems in bovine adrenal fasciculata cells.

Endocr. J. 63 , 77-85, (2016)

Adenosine triphosphate (ATP) is known to stimulate cortisol production in vitro, however, the effect of guanosine triphosphate (GTP) on cortisol production is not known. We studied the effect of GTP o...

Trilostane dose versus body weight in the treatment of naturally occurring pituitary-dependent hyperadrenocorticism in dogs.

J. Vet. Intern. Med. 26(4) , 1078-80, (2012)

Trilostane is commonly used in the treatment of dogs with naturally occurring pituitary-dependent hyperadrenocorticism (PDH). Dose recommendations have varied from the manufacturer and the literature....

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