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苯甲丁氮酮

苯甲丁氮酮用途

Nadolol (SQ-11725) 是一种非选择性的具有口服活性的 β-肾上腺素受体 (β-adrenergic receptors) 阻滞剂,也是有机阴离子转运多肽 1A2 (OATP1A2) 的一种底物。Nadolol 可用于高血压,心绞痛和血管性头痛的研究。
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苯甲丁氮酮名称

[ CAS 号 ]:
42200-33-9

[ 中文名 ]:
苯甲丁氮酮

[ 英文名 ]:
Nadolol

[中文别名 ]:

[英文别名 ]:

苯甲丁氮酮生物活性

[ 描述 ]:

Nadolol (SQ-11725) 是一种非选择性的具有口服活性的 β-肾上腺素受体 (β-adrenergic receptors) 阻滞剂,也是有机阴离子转运多肽 1A2 (OATP1A2) 的一种底物。Nadolol 可用于高血压,心绞痛和血管性头痛的研究。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[体外研究]

在人胚肾293细胞中,(-)-表没食子儿茶素没食子酸酯(EGCG)竞争性地抑制OATP1A2介导的纳多洛尔摄取,Ki值为19.4μM。相对于纳多洛尔,OATP1A2的Km为84μM[2]。

[体内研究]

在携带B16F10肿瘤细胞的1只雄性小鼠中,通过给予纳多洛尔(20mg/kg)阻断神经内分泌反应,导致暴露于急性社会压力的受试者的肺转移灶越来越小[3]。

[参考文献]

[1]. Johannes C von Alvensleben, et al. Nadolol for Treatment of Supraventricular Tachycardia in Infants and Young Children. Pediatr Cardiol. 2017 Mar;38(3):525-530.

[2]. Osamu Abe, et al. Role of (-)-Epigallocatechin Gallate in the Pharmacokinetic Interaction Between Nadolol and Green Tea in Healthy Volunteers. Eur J Clin Pharmacol. 2018 Jun;74(6):775-783.

[3]. O Vegas, et al. Effects of Antalarmin and Nadolol on the Relationship Between Social Stress and Pulmonary Metastasis Development in Male OF1 Mice. Behav Brain Res. 2009 Dec 14;205(1):200-6.

苯甲丁氮酮物理化学性质

[ 密度 ]:
1.189g/cm3

[ 沸点 ]:
526.4ºC at 760mmHg

[ 熔点 ]:
125-130ºC

[ 分子式 ]:
C17H27NO4

[ 分子量 ]:
309.40100

[ 闪点 ]:
272.2ºC

[ 精确质量 ]:
309.19400

[ PSA ]:
81.95000

[ LogP ]:
1.02570

[ 外观性状 ]:
白色固体

[ 折射率 ]:
1.573

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
Slightly soluble in water, freely soluble in ethanol (96 per cent), practically insoluble in acetone.

苯甲丁氮酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QJ4870000
CHEMICAL NAME :
2,3-Naphthalenediol, 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-1,2 ,3,4-tetrahydro-
CAS REGISTRY NUMBER :
42200-33-9
LAST UPDATED :
199506
DATA ITEMS CITED :
19
MOLECULAR FORMULA :
C17-H27-N-O4
MOLECULAR WEIGHT :
309.45
WISWESSER LINE NOTATION :
L66&TJ BO1YQ1MX1&1&1 HQ IQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
571 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - visual field changes
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 97,454,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
64 mg/kg/4W-I
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of endocrine pancreas
REFERENCE :
BJCPAT British Journal of Clinical Practice. (Medical News Group, 1 Bedford St., London WC2E 9HD, UK) V.10(10)- 1956- Volume(issue)/page/year: 43,74,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
5300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
43NDAD "Pharmacology of Antihypertensive Drugs," Scriabine, A., ed., New York, Raven Press, 1980 Volume(issue)/page/year: -,295,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
322 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: 16,1461,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 9,527,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
59200 ug/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: 16,1461,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3800 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 9,527,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
270 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
43NDAD "Pharmacology of Antihypertensive Drugs," Scriabine, A., ed., New York, Raven Press, 1980 Volume(issue)/page/year: -,295,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 9,527,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
47100 ug/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: 16,1461,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>500 mg/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: -,767,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
182 gm/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 4,360,1984
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
72 gm/kg/30D-I
TOXIC EFFECTS :
Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 9,527,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
29120 mg/kg/26W-I
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 4,360,1984 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
550 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - behavioral
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 11,5119,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1650 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 11,5119,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
42 gm/kg
SEX/DURATION :
male 9 week(s) pre-mating female 14 day(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - sex ratio
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 11,5119,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
13 gm/kg
SEX/DURATION :
male 9 week(s) pre-mating female 14 day(s) pre-mating - 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 11,5119,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1300 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 44,379,1978
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苯甲丁氮酮安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
2

[ RTECS号 ]:
QJ4870000

[ 海关编码 ]:
2922509090

苯甲丁氮酮海关

[ 海关编码 ]: 2922509090

[ 中文概述 ]:
2922509090. 其他氨基醇酚、氨基酸酚及其他含氧基氨基化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:AB. 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, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

苯甲丁氮酮文献

Direct doping analysis of beta-blocker drugs from urinary samples by on-line molecularly imprinted solid-phase extraction coupled to liquid chromatography/mass spectrometry.

Analyst 140(8) , 2696-703, (2015)

The use of beta-blockers to enhance performance in some sports is forbidden. Based on this regulation, there is a demand for dynamic analytical procedures for analyzing these compounds quickly and wit...

Versatile ene-thiol photoclick reaction for preparation of multimodal monolithic silica capillary columns.

J. Chromatogr. A. 1365 , 140-7, (2014)

This paper presents a photografting process of monolithic silica capillary columns based on the ene-thiol click chemistry. This study is performed on a generic vinyl-functionalized silica monolith (Hm...

The Janus kinase 2 inhibitor fedratinib inhibits thiamine uptake: a putative mechanism for the onset of Wernicke's encephalopathy.

Drug Metab. Dispos. 42(10) , 1656-62, (2014)

The clinical development of fedratinib, a Janus kinase (JAK2) inhibitor, was terminated after reports of Wernicke's encephalopathy in myelofibrosis patients. Since Wernicke's encephalopathy is induced...


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推荐生产厂家/供应商:

公司名:上海源溪生物科技有限公司

区域:上海市浦东新区

价格:
¥需询单/1g

联系人:赖经理

产品详情:Nadolol


公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

价格:
¥998.9/25mg ¥514.9/1ml ¥2777.9/100mg ¥需询单/1g

联系人:阿拉丁李高志

产品详情:纳多洛尔


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标题:苯甲丁氮酮_用途_密度_熔点_苯甲丁氮酮CAS号【42200-33-9】_化源网 地址:https://m.chemsrc.com/mip/cas/42200-33-9_672897.html