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苯并恶唑胺

苯并恶唑胺用途

Zoxazolamine 被广泛用于药物测试,可作为啮齿动物细胞色素 P-450 活性变化的方便指标。

苯并恶唑胺名称

[ CAS 号 ]:
61-80-3

[ 中文名 ]:
2-氨基-5-氯苯并噁唑

[ 英文名 ]:
Zoxazolamine

[中文别名 ]:

[英文别名 ]:

EINECS 200-519-4
MFCD00005770
5-chloro-1,3-benzoxazol-2-amine
Zoxazolamine

苯并恶唑胺生物活性

[ 描述 ]:

Zoxazolamine 被广泛用于药物测试,可作为啮齿动物细胞色素 P-450 活性变化的方便指标。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体内研究]

唑来膦胺广泛用于药理学试验,作为啮齿动物细胞色素P-450活性变化的方便指标。由测试浓度数据确定的时间平均血清清除率为7.28±1.01mL/min/kg,用于唑佐唑胺。在三种不同的速率下将唑佐唑胺输注到翻正反射(LRR)显示,随着输注速率的增加,血清和脑中的唑佐胺浓度增加。当Zoxazolamine输注持续超过LRR开始5分钟时,LRR偏移的脑脊液(CSF)中的唑嗪胺浓度与起始浓度基本相同[1]。

[动物实验]

在该研究中使用近交雄性Lewis大鼠。允许动物7至12天适应当地动物设施并恢复运输过程中可能产生的压力。为了比较起始时血清中的药物浓度和翻正反射丧失的偏移，在失去翻正反射开始后，将唑并胺以0.51mg / min的速率输注到股静脉中5分钟。输注溶液由1毫升生理盐水中的10毫克唑佐唑胺组成。然后，使用产生主流血液的程序，从开始时的四个速率和正常反射损失的偏移中获得来自颈静脉的血液样本[1]。

[参考文献]

[1]. Yasuhara M, et al. Pharmacodynamics of zoxazolamine and chlorzoxazone in rats. Pharm Res. 1988 Jul;5(7):401-7.

[相关活性小分子]

苯并恶唑胺物理化学性质

[ 密度 ]:
1.481 g/cm3

[ 沸点 ]:
316.8ºC at 760 mmHg

[ 熔点 ]:
181-184 °C(lit.)

[ 分子式 ]:
C₇H₅ClN₂O

[ 分子量 ]:
168.58000

[ 闪点 ]:
145.4ºC

[ 精确质量 ]:
168.00900

[ PSA ]:
52.05000

[ LogP ]:
2.64460

[ 折射率 ]:
1.692

[ 储存条件 ]:
库房通风低温干燥

苯并恶唑胺MSDS

详细MSDS(安全技术说明书)

苯并恶唑胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DM4550000

CHEMICAL NAME :: Benzoxazole, 2-amino-5-chloro-

CAS REGISTRY NUMBER :: 61-80-3

LAST UPDATED :: 199106

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C7-H5-Cl-N2-O

MOLECULAR WEIGHT :: 168.59

WISWESSER LINE NOTATION :: T56 BN DOJ CZ HG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1607 mg/kg/34W-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 176,874,1961

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 14 mg/kg/D

TOXIC EFFECTS :: Behavioral - stiffness

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 160,745,1956

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 782 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic)

REFERENCE :: FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 16,319,1957

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 102 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - muscle weakness Behavioral - ataxia

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: 129,75,1960

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 540 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 128,112,1960

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 mg/kg

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

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: AD277-689

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 376 mg/kg

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

REFERENCE :: 29QHAQ "Principles of Medicinal Chemistry," Foye, W.O., et al., eds., Philadelphia, Lea & Febiger, 1974 Volume(issue)/page/year: -,246,1974

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 117 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic)

REFERENCE :: FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 16,319,1957

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 670 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - muscle weakness Behavioral - ataxia

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: 129,75,1960

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 268 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - muscle weakness Behavioral - ataxia

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: 129,75,1960 *** REVIEWS *** TOXICOLOGY REVIEW AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 38,409,1965

苯并恶唑胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312-H315-H319-H332-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
DM4550000

[ 海关编码 ]:
2934999090

苯并恶唑胺合成路线

详细合成路线

苯并恶唑胺上下游产品

苯并恶唑胺上游产品

苯并恶唑胺下游产品

苯并恶唑胺海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

苯并恶唑胺文献

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The bioassay guided fractionation of the dried aerial part of Indigofera tinctoria Linn. led to the identification of an active fraction labelled as indigotin. On further chemical analysis, a compound...

Pharmacological activation of cloned intermediate- and small-conductance Ca(2+)-activated K(+) channels.

Am. J. Physiol. 278 , C570-C581, (2000)

We previously characterized 1-ethyl-2-benzimidazolinone (1-EBIO), as well as the clinically useful benzoxazoles, chlorzoxazone (CZ), and zoxazolamine (ZOX), as pharmacological activators of the interm...

Stimulation of Cl(-) secretion by chlorzoxazone.

J. Pharmacol. Exp. Ther. 292 , 778-787, (2000)

We previously demonstrated that 1-ethyl-2-benzimidazolone (1-EBIO) directly activates basolateral membrane calcium-activated K(+) channels (K(Ca)), thereby stimulating Cl(-) secretion across several e...

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