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盐酸索他洛尔

盐酸索他洛尔用途

Sotalol盐酸盐是肾上腺素受体拮抗剂,可作用于威胁生命的心律失常。

盐酸索他洛尔名称

[ CAS 号 ]:
959-24-0

[ 中文名 ]:
盐酸索他洛尔

[ 英文名 ]:
Sotalol hydrochloride

[中文别名 ]:

4'-(1-羟基-2-异丙胺乙基)甲磺酸苯胺盐酸盐

[英文别名 ]:

MFCD00242937
Sotacor
Sotalol hydrochloride
Betapace
(±)-Sotalol hydrochloride
EINECS 213-496-0
b-Cardone
β-Cardone
Sotalol Monohydrochloride
Sotalol (hydrochloride)

盐酸索他洛尔生物活性

[ 描述 ]:

Sotalol盐酸盐是肾上腺素受体拮抗剂,可作用于威胁生命的心律失常。

[ 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 >> 心血管疾病

[参考文献]

[1]. Antonaccio, M.J. and A. Gomoll, Pharmacologic basis of the antiarrhythmic and hemodynamic effects of sotalol. Am J Cardiol, 1993. 72(4): p. 27A-37A.

[2]. Bertrix, L., et al., Protection against ventricular and atrial fibrillation by sotalol. Cardiovasc Res, 1986. 20(5): p. 358-63.

[相关活性小分子]

盐酸索他洛尔物理化学性质

[ 沸点 ]:
443.3ºC at 760 mmHg

[ 熔点 ]:
218-220°C

[ 分子式 ]:
C₁₂H₂₁ClN₂O₃S

[ 分子量 ]:
308.825

[ 闪点 ]:
221.9ºC

[ 精确质量 ]:
308.096130

[ PSA ]:
86.81000

[ LogP ]:
3.43620

[ 外观性状 ]:
白色至灰白色粉末

[ 储存条件 ]:
库房低温通风干燥

[ 水溶解性 ]:
H2O: 20 mg/mL

盐酸索他洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PB0826000

CHEMICAL NAME :: Methanesulfonanilide, 4'-(1-hydroxy-2-(isopropylamino)ethyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 959-24-0

LAST UPDATED :: 199609

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C12-H20-N2-O3-S.Cl-H

MOLECULAR WEIGHT :: 308.86

WISWESSER LINE NOTATION :: WS1&MR DYQ1MY1&1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 45714 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 43,221,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 64 mg/kg/2W-I

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction)

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 291,544,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3450 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) 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: 149,161,1965

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 680 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) 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: 149,161,1965

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2600 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) 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: 149,161,1965

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 670 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) 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: 149,161,1965

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 330 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) 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: 149,161,1965

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) 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: 149,161,1965 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 69450 mg/kg/30D-I

TOXIC EFFECTS :: Liver - changes in liver weight 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: 23,2895,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 281 gm/kg/1Y-I

TOXIC EFFECTS :: Cardiac - changes in heart weight Kidney, Ureter, Bladder - urine volume increased Endocrine - changes in spleen weight

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: 23,2913,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 126 gm/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

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: 23,1995,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 280 mg/kg

SEX/DURATION :: female 8-21 day(s) after conception

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

REFERENCE :: EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967- Volume(issue)/page/year: 195,75,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8085 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

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: 23,2007,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 24960 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects 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: 23,2031,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2340 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal 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: 23,2023,1995 *** REVIEWS *** TOXICOLOGY REVIEW FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 6,395,1986

盐酸索他洛尔安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
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 ]:
PB0826000

[ 海关编码 ]:
2942000000

盐酸索他洛尔制备

1. 甲磺酰苯胺的制备

在反应瓶中加入苯胺15.5g(0.16mol)、三乙胺12ml和乙醇150ml冰盐浴冷却下搅拌滴加甲烷磺酰氯20g(0.17mol),控制滴加速度以保持内温在-5~0ºC之间为准,滴加毕,于室温搅拌反应4h.过滤#滤液浓缩至原体积的1/2,冷却至0ºC下析晶,过滤,用乙醇重结晶,干燥,得白色晶体甲磺酰苯胺23g,收率84%,mp>293ºC.Rf0.7[展开剂:氯仿/甲醇(3:1)]

2. 4’-(2-溴乙酰基)甲磺酰苯胺的制备

在反应瓶中加入上步制备的化合物甲磺酰苯胺8.55g(0.055mol)、溴乙酰溴15g(0.07mol)和二硫化碳70ml,于冰水浴冷却下搅拌加入无水AlCl3 17g,控制内温在15ºC以下,加毕,于室温搅拌反应2h.搅拌回流反应1h. 蒸除溶剂,将剩余浓缩液倾入冰水中,析出固体,过滤,得粗品4’-(2-溴乙酰基)甲磺酰苯胺,为浅红色颗粒状结晶,将其用乙醇重结晶,得白色晶体,干燥后得4’-(2-溴乙酰基)甲磺酰苯胺14.1g,收率96.6%,mp191~192ºC(分解).

3. 4’-(2-异丙氨基乙酰基)甲磺酰苯胺盐酸盐的制备

在反应瓶中加入异丙胺10.0g(0.17mol)和甲醇30ml,搅拌和冰盐浴冷却下,于-5ºC左右加入4’-(2-溴乙酰基) 甲磺酰苯胺4’-(2-溴乙酰基)甲磺酰苯胺14.6g(0.05mol),继续在同温度下搅拌反应2h.将反应液减压蒸除溶剂,剩余物加入丙酮200ml,通入氯化氢气体至pH=2,冷却,过滤,结晶用无水乙醇重结晶#得白色晶体4’-(2-异丙氨基乙酰基)甲磺酰苯胺盐酸盐13.6g,收率65%,mp223~225ºC.

4. N-[4-[1-羟基-2-[(1-甲基乙基)氨基]乙基]苯基]甲磺酰胺盐酸盐(盐酸索他洛尔)的合成

在氢化反应瓶中加入上步制备的化合物4’-(2-异丙氨基乙酰基)甲磺酰苯胺盐酸盐19.01g(0.65mol)、甲醇200ml和10%Pd/C1.14g.用N2置换瓶中空气3次,用氢气置换N2 2次,于室温下搅拌通H2反应至不吸氢为止(常压下反应),过滤,滤液浓缩至干,得粗品,将粗品加甲醇200ml加热至全溶,加适量活性炭脱色15min.抽滤,冷却析晶,过滤,得白色晶体17g,mp206.5~207ºC,收率85%[Pd/C回收:将Pd/C置于稀盐酸中回流,再通氢气活化数小时即可]

盐酸索他洛尔海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

盐酸索他洛尔文献

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Heart 99(23) , 1755-60, (2013)

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