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42200-33-9生产厂家

42200-33-9价格

42200-33-9

42200-33-9结构式
42200-33-9结构式
  • 常用中文名:苯甲丁氮酮
  • 常用英文名:Nadolol
  • CAS号:42200-33-9
  • 分子式:C17H27NO4
  • 分子量:309.40100
  • 相关类别: 原料药 循环系统用药 抗心律失常药
  • 发布时间:2018-04-30 08:00:00
  • 更新时间:2024-01-09 00:10:04
  • 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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中文名 苯甲丁氮酮
英文名 (2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
中文别名 氢萘心安
英文别名 nadolol
5-[3-(tert-butylamino)-2-oxopropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
[14C]-Nadolol
Nadic
5-[3-[(1,1-dimethylethyl)-amino]-2-hydroxypropoxy]-1,2,3,4-tetrahydro-2,3-cis-naphthalenediol
Solgol
Nadololum
Nadololum [INN-Latin]
Corgaretic
1-tert.-butylamino-3-(1,2,3,4-tetrahydro-2,3-dihydroxy-5-napthyloxy)-2-propanol
Anabet
Corgard
(2R,3S)-5-(3-(tert-Butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydronaphthalene-2,3-diol
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
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.

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.

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

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
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%