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普拉洛尔

普拉洛尔用途

Practolol 是一种有效和选择性的 β1 肾上腺素能受体拮抗剂。Practolol 可用于心律失常的研究。

普拉洛尔名称

[ CAS 号 ]:
6673-35-4

[ 中文名 ]:
普拉洛尔

[ 英文名 ]:
Practolol

[中文别名 ]:

心得宁

[英文别名 ]:

rac Practolol

普拉洛尔生物活性

[ 描述 ]:

Practolol 是一种有效和选择性的 β1 肾上腺素能受体拮抗剂。Practolol 可用于心律失常的研究。

[ 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

[ 靶点 ]

β1-adrenergic receptor[1]

[体外研究]

普拉托洛尔(10μM；30分钟)优先对抗R0363在豚鼠自发收缩气管制剂中产生的舒张作用[1]。Practolol(10nm-100μM)以剂量依赖性方式阻断(-)肾上腺素诱导的颗粒细胞孕酮生成[2]。

[体内研究]

普拉托洛尔(0.5 mg/kg；静脉注射)可降低完整闭胸犬的心率、左室dP/dt max、心肌血流量和心输出量[3]。普拉托洛尔(0.5 mg/kg；静脉注射)可降低正常心肌血流量,但结扎冠状动脉后缺血区的血流量保持不变[3]。

[参考文献]

[1]. Iakovidis D, et, al. In vitro activity of RO363, a beta1-adrenoceptor selective agonist. Br J Pharmacol. 1980 Apr;68(4):677-85.

[2]. Adashi EY, et, al. Stimulation of beta 2-adrenergic responsiveness by follicle-stimulating hormone in rat granulosa cells in vitro and in vivo. Endocrinology. 1981 Jun;108(6):2170-8.

[3]. Marshall RJ, et, al. Comparative effects of propranolol and practolol in the early stages of experimental canine myocardial infarction. Br J Pharmacol. 1976 Jun;57(2):295-303.

普拉洛尔物理化学性质

[ 密度 ]:
1.0807 (rough estimate)

[ 沸点 ]:
409.54°C (rough estimate)

[ 熔点 ]:
134-136° (BuOAc)

[ 分子式 ]:
C₁₄H₂₂N₂O₃

[ 分子量 ]:
266.33600

[ 精确质量 ]:
266.16300

[ PSA ]:
70.59000

[ LogP ]:
1.84660

[ 折射率 ]:
1.5110 (estimate)

[ 储存条件 ]:
2-8°C

普拉洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AE4222000

CHEMICAL NAME :: Acetanilide, 4'-(2-hydroxy-3-(isopropylamino)propoxy)-

CAS REGISTRY NUMBER :: 6673-35-4

LAST UPDATED :: 199304

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C14-H22-N2-O3

MOLECULAR WEIGHT :: 266.38

WISWESSER LINE NOTATION :: 1Y1&M1YQ1OR DMV1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - conjunctive irritation Sense Organs and Special Senses (Eye) - effect, not otherwise specified

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,595,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7550 mg/kg/2Y

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - changes in extra-ocular muscles Gastrointestinal - peritonitis Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 1,44,1975

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3458 mg/kg

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

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 540 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7500 mg/kg

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

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 130 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3661 mg/kg

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

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 455 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 25,145,1973

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3357 mg/kg

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

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 67400 ug/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 20,126,1973 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

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 - physical

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 21,567,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12 gm/kg

SEX/DURATION :: female 7-12 day(s) after conception

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

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 21,567,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 600 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - physical

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 21,567,1974 *** 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

普拉洛尔安全信息

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

[ RTECS号 ]:
AE4222000

[ 海关编码 ]:
2924299090

普拉洛尔合成路线

详细合成路线

普拉洛尔上下游产品

普拉洛尔上游产品

普拉洛尔下游产品

普拉洛尔海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

普拉洛尔文献

Large-Scale Prediction of Drug Targets Based on Local and Global Consistency of Chemical-Chemical Networks.

Comb. Chem. High Throughput Screen 19 , 121-8, (2016)

It is crucial to identify the molecular targets of a compound during the course of the new drug discovery and drug development. Due to the complexity of biological systems, finding drug targets by bio...

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