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匹立昔尔

匹立昔尔用途

Pirinixil 是一种低毒性降血脂药。

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匹立昔尔名称

[ CAS 号 ]:
65089-17-0

[ 中文名 ]:
匹立昔尔

[ 英文名 ]:
Pirinixil

[英文别名 ]:

Pirinixil
BR-931
Pirinixilo [Spanish]
Pirinixilum [INN-Latin]
Pirinixilo [INN-Spanish]

匹立昔尔生物活性

[ 描述 ]:

Pirinixil 是一种低毒性降血脂药。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[体内研究]

Pirinixil是一种低毒的降血脂药。 Pirinixi在大鼠的脾脏,肾脏和心脏中降低总胆固醇。 Pirinixil使估计的总体内胆固醇降低约40％[1]。 Pirinixil可显着提高血浆胆固醇水平,而不会影响血浆甘油三酯。 Pirinixil显着降低肝脏胆固醇和甘油三酯,而血浆和肝脏脂质水平降低约20％。肝脏HMG-CoA还原酶活性不受影响,但Pirinixil可显着降低胆固醇7α-羟化酶[2]。

[动物实验]

在所有研究中使用在每个实验开始时重220-230g的雄性Sprague-Dawley大鼠。它们被保存在空调环境中，拥有可控的照明和免费供水。膳食治疗是（A）大鼠的标准饮食和（B）2％胆固醇+ 2％胆酸方案。两种饮食分别随意给药1周和2周（标准饮食）和2周（胆固醇酸饮食）。在3个实验的每一个中的5只大鼠组（标准饮食1周和2周，胆固醇 - 胆酸饮食2周）通过胃插管每天在羧甲基纤维素载体中以20mg / kg的剂量施用Pirinixil。通过插管[1]每天给予对照相似体积的载体。

[参考文献]

[1]. D'Atri G, et al. Clofibrate, pirinixil (BR 931) and WY-14,643 do not affect body cholesterol in Sprague-Dawley rats. Atherosclerosis. 1980 Nov;37(3):475-83.

[2]. Kritchevsky D, et al. Increased plasma cholesterol and decreased body lipid levels in Wistar rats following pirinixil(BR 931) treatment. Pharmacol Res Commun. 1979 Jun;11(6):475-82.

[相关活性小分子]

匹立昔尔物理化学性质

[ 密度 ]:
1.37g/cm3

[ 沸点 ]:
609.6ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₁₉ClN₄O₂S

[ 分子量 ]:
366.86600

[ 闪点 ]:
322.5ºC

[ 精确质量 ]:
366.09200

[ PSA ]:
112.44000

[ LogP ]:
3.15490

[ 折射率 ]:
1.642

[ 储存条件 ]:
2-8℃

匹立昔尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AB5860000

CHEMICAL NAME :: Acetamide, 2-((4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thio)-N-( 2-hydroxyethyl)-

CAS REGISTRY NUMBER :: 65089-17-0

BEILSTEIN REFERENCE NO. :: 0845588

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H19-Cl-N4-O2-S

MOLECULAR WEIGHT :: 366.90

WISWESSER LINE NOTATION :: T6M CN BHJ BS1VM2Q DG FMR B1 C1

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 :: >5 gm/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1575 mg/kg/21D-C

TOXIC EFFECTS :: Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - catalases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 gm/kg/81W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 137 gm/kg/81W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Rodent - mouse Cells - not otherwise specified

DOSE/DURATION :: 25 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 40,36,1980

匹立昔尔

匹立昔尔用途

匹立昔尔名称

匹立昔尔生物活性

匹立昔尔物理化学性质

匹立昔尔毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

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