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卡维地洛

卡维地洛用途

Carvedilol(BM14190)是非选择性β和α1阻断剂,能抑制LDL的氧化,IC50为3.8 μM。

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卡维地洛名称

[ CAS 号 ]:
72956-09-3

[ 中文名 ]:
卡维地洛

[ 英文名 ]:
Carvedilol

[中文别名 ]:

[英文别名 ]:

Coropress
Dilatrend
Carvedilolum
Kredex
Coreg
Dimitone
Carvedilolum [Latin]
MFCD00864692
Querto
Carvedilol

卡维地洛生物活性

[ 描述 ]:

Carvedilol(BM14190)是非选择性β和α1阻断剂,能抑制LDL的氧化,IC50为3.8 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 内分泌

[参考文献]

[1]. Chen J, Huang C, Zhang B, et al. The effects of carvedilol on cardiac structural remodeling: The role of endogenous nitric oxide in the activity of carvedilol. Mol Med Rep. 2013 Apr;7(4):1155-8.

[2]. Stafylas PC, Sarafidis PA. Carvedilol in hypertension treatment. Vasc Health Risk Manag. 2008;4(1):23-30.

[3]. Othman AA, Tenero DM, Boyle DA et al. Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate. AAPS J. 2007 Jun 15;9(2):E208-1

[4]. Koshimizu TA, Tsujimoto G, Hirasawa A et al. Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72.

[相关活性小分子]

卡维地洛物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
655.2±55.0 °C at 760 mmHg

[ 熔点 ]:
113-117ºC

[ 分子式 ]:
C₂₄H₂₆N₂O₄

[ 分子量 ]:
406.474

[ 闪点 ]:
350.1±31.5 °C

[ 精确质量 ]:
406.189270

[ PSA ]:
75.74000

[ LogP ]:
4.11

[ 外观性状 ]:
无色结晶粉末

[ 蒸汽压 ]:
0.0±2.1 mmHg at 25°C

[ 折射率 ]:
1.657

[ 储存条件 ]:
Store at +4°C

卡维地洛MSDS

卡维地洛毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UA8670000

CHEMICAL NAME :: 2-Propanol, 1-(9H-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl )amino)-

CAS REGISTRY NUMBER :: 72956-09-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C24-H26-N2-O4

MOLECULAR WEIGHT :: 406.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - weight loss or decreased weight gain

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: 20,1181,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 769 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - acute pulmonary edema

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Liver - other changes

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - body temperature decrease

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: 20,1181,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 364 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - acute pulmonary edema

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 27 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Liver - other changes

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

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: 20,1181,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 gm/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3101,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1620 mg/kg

SEX/DURATION :: female 16-21 day(s) after conception lactating female 1-21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3109,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 gm/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3071,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 gm/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - live birth index (measured after birth)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3071,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 gm/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3071,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1950 mg/kg

SEX/DURATION :: female 7-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,127,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 975 mg/kg

SEX/DURATION :: female 7-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,127,1991

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卡维地洛安全信息

[ 符号 ]:

GHS09

[ 危害声明 ]:
H411

[ 警示性声明 ]:
P273

[ 个人防护装备 ]:
Eyeshields;Gloves

[ 危害码 (欧洲) ]:
N: Dangerous for the environment;Xn: Harmful;

[ 风险声明 (欧洲) ]:
51/53-36/37/38-20/21/22

[ 安全声明 (欧洲) ]:
61-36-26

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ RTECS号 ]:
UA8670000

[ 海关编码 ]:
2933990090

卡维地洛合成路线

卡维地洛上下游产品

卡维地洛上游产品

卡维地洛下游产品

卡维地洛制备

1,3-环己二酮溶于水，在氮气保护下，缓慢滴加苯肼水溶液，搅拌。过滤，水洗，乙醇重结晶，得苯腙物。将苯腙物加入冰乙酸和二氯化锌的溶液中反应，经保温、冷却等处理咔唑衍生物。将其和氢氧化钾、水、乙醇和RaneyNi,在氮气下搅拌回流，得到还原产物。将得到的还原产物、氢氧化钠、水和三乙基苄铵盐(TEBA),搅拌下滴加环氧氯丙烷,室温搅拌。加水，搅拌。过滤，滤饼用0.1mol/L氢氧化钠和水洗，乙酸乙酯重结晶，得到的化合物再与邻甲氧苯氧基乙胺和异丙醇，一起回流。冷至室温，搅拌下加入甲苯，静置。用乙酸乙酯重结晶，得卡维地洛。

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卡维地洛海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

卡维地洛文献

Probiotic properties of lactic acid bacteria isolated from water-buffalo mozzarella cheese.

Probiotics Antimicrob Proteins 6 , 141-56, (2014)

This study evaluated the probiotic properties (stability at different pH values and bile salt concentration, auto-aggregation and co-aggregation, survival in the presence of antibiotics and commercial...

High-dose short-term administration of naringin did not alter talinolol pharmacokinetics in humans.

Eur. J. Pharm. Sci. 68 , 36-42, (2015)

Naringin is considered the major causative ingredient of the inhibition of intestinal drug uptake by grapefruit juice. Moreover, it is contained in highly dosed nutraceuticals available on the market....

Human and simulated intestinal fluids as solvent systems to explore food effects on intestinal solubility and permeability.

Eur. J. Pharm. Sci. 63 , 178-86, (2014)

The mixed micelles and vesicles present in the intraluminal environment of the postprandial state exhibit suitable solubilizing capacities for lipophilic drugs. This increase in solubility, however, i...

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卡维地洛相关知识

卡维地洛片说明书-作用-卡维地洛片副作用

2019-01-04 12:53:35

导读：卡维地洛，化学名称：（±）-1-(9H-咔唑-4-氧基)-3-[2-(2-甲氧基苯氧基乙基）-氨基]-2-丙醇。分子式：C24H26N2O4，分子量：406.49。卡维地洛片是一种适用于原发性高血压患者的药物，对高血压的治疗和预防是很有效果的。对于充血性心力衰竭也是可以进行治疗的，这样可以降...

卡维地洛

卡维地洛用途

卡维地洛名称

卡维地洛生物活性

卡维地洛物理化学性质

卡维地洛MSDS

详细MSDS(安全技术说明书)

卡维地洛毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

卡维地洛安全信息

卡维地洛合成路线

详细合成路线

卡维地洛上下游产品

卡维地洛上游产品

卡维地洛下游产品

卡维地洛制备

卡维地洛海关

卡维地洛文献

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