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盐酸黄酮哌酯

盐酸黄酮哌酯用途

Flavoxate(DW-61)盐酸盐是毒蕈碱受体AChR拮抗剂, IC50为12.2 μM。

盐酸黄酮哌酯作用

盐酸黄酮哌酯具有抑制腺苷酸环化酶、磷酸二酯酶的作用以及钙离子拮抗作用，能直接解除改善排尿、缓解痉挛性疼痛、提高生活质量有显著疗效，是近年治疗PD的药物。

盐酸黄酮哌酯名称

[ CAS 号 ]:
3717-88-2

[ 中文名 ]:
盐酸黄酮哌酯

[ 英文名 ]:
Flavoxate hydrochloride

[中文别名 ]:

[英文别名 ]:

Spasuret hydrochloride
Flavoxate Hydrochloride
MFCD00072099
EINECS 223-066-4
Flavoxate HCl

盐酸黄酮哌酯生物活性

[ 描述 ]:

Flavoxate(DW-61)盐酸盐是毒蕈碱受体AChR拮抗剂, IC50为12.2 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> 神经信号通路 >> mAChR

研究领域 >> 神经疾病

[参考文献]

[1]. Dansette, P.M., M. Jaoen, and C. Pons, HMG-CoA reductase activity in human liver microsomes: comparative inhibition by statins. Exp Toxicol Pathol, 2000. 52(2): p. 145-8.

[2]. Kimura, Y., et al., Mechanisms of the suppression of the bladder activity by flavoxate. Int J Urol, 1996. 3(3): p. 218-27.

[3]. Oka, M., et al., Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res, 1996. 727(1-2): p. 91-8.

[相关活性小分子]

盐酸黄酮哌酯物理化学性质

[ 密度 ]:
1.203g/cm3

[ 沸点 ]:
564.1ºC at 760 mmHg

[ 熔点 ]:
232-234°C

[ 分子式 ]:
C₂₄H₂₆ClNO₄

[ 分子量 ]:
427.921

[ 闪点 ]:
294.9ºC

[ 精确质量 ]:
427.155029

[ PSA ]:
59.75000

[ LogP ]:
5.15100

[ 外观性状 ]:
白色,固体

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
H2O: ~6.6 mg/mL

盐酸黄酮哌酯MSDS

详细MSDS(安全技术说明书)

盐酸黄酮哌酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DJ2450000

CHEMICAL NAME :: 4H-1-Benzopyran-8-carboxylic acid, 3-methyl-4-oxo-2-phenyl-, 2-piperidinoethyl ester, hydrochloride

CAS REGISTRY NUMBER :: 3717-88-2

LAST UPDATED :: 199504

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C24-H25-N-O4.Cl-H

MOLECULAR WEIGHT :: 427.96

WISWESSER LINE NOTATION :: T66 BO EVJ CR& D1 JVO2- AT6NTJ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1040 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 170 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - cyanosis Gastrointestinal - changes in structure or function of salivary glands

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1010 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 740 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - excitement

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - local anesthetic Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic) Behavioral - analgesia

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 610 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 28 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >6 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 30 gm/kg/30D-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in thymus weight Blood - pigmented or nucleated red blood cells

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4500 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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 gm/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)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9 gm/kg

SEX/DURATION :: female 7-12 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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1920 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Bacteria - Salmonella typhimurium

DOSE/DURATION :: 79 ug/plate

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: 19,773,1991 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6121 No. of Facilities: 36 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 357 (estimated) No. of Female Employees: 187 (estimated)

盐酸黄酮哌酯安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26

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

[ RTECS号 ]:
DJ2450000

[ 海关编码 ]:
2934999090

盐酸黄酮哌酯海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸黄酮哌酯文献

A review of flavoxate hydrochloride in the treatment of urge incontinence.

J. Int. Med. Res. 16(5) , 317-30, (1988)

This article provides a review of the use of flavoxate hydrochloride in the treatment of urge incontinence. It outlines the pharmacology, mode of action, toxicology and pharmacokinetic studies which h...

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