< 生产厂家价格 >

马来酸噻吗洛尔

马来酸噻吗洛尔用途

(S)-Timolol马来酸盐是非选择性β-肾上腺素受体拮抗剂,对β1和β2受体亚型的Ki分别为1.97和2.0 nM。

点击显示

马来酸噻吗洛尔名称

[ CAS 号 ]:
26921-17-5

[ 中文名 ]:
马来酸噻吗洛尔

[ 英文名 ]:
(S)-timolol maleate

[中文别名 ]:

[英文别名 ]:

Timolol maleate salt
Betim
Tenopt
Proflax
Aquanil
Timorom
(S)-Timolol maleate
Rysmon TG
EINECS 248-111-5
Optimol

马来酸噻吗洛尔生物活性

[ 描述 ]:

(S)-Timolol马来酸盐是非选择性β-肾上腺素受体拮抗剂,对β1和β2受体亚型的Ki分别为1.97和2.0 nM。

[ 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 >> 神经疾病

[参考文献]

[1]. Deepika Aggarwal, Indu P. Kaur. Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system. International Journal of Pharmaceutics. 2005, 290(1-2): 155-159.

[2]. Mandagere AK, Thompson TN, Hwang KK. Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. J Med Chem. 2002;45(2):304-11.

[3]. A.H El-Kamel. In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate. International Journal of Pharmaceutics. 2002, 241, (1) :47-55.

[4]. Konstas AG, Maltezos AC, Gandi S, et al. Comparison of 24-hour intraocular pressure reduction with two dosing regimens of latanoprost and timolol maleate in patients with primary open-angle glaucoma. American Journal of Ophthalmology .1999, 128(1):15-20.

[相关活性小分子]

马来酸噻吗洛尔物理化学性质

[ 沸点 ]:
704.6ºC at 760 mmHg

[ 熔点 ]:
202-203 °C(lit.)

[ 分子式 ]:
C₁₇H₂₈N₄O₇S

[ 分子量 ]:
432.492

[ 闪点 ]:
380ºC

[ 精确质量 ]:
432.167877

[ PSA ]:
182.58000

[ LogP ]:
0.67020

[ 外观性状 ]:
powder | white to off-white

[ 蒸汽压 ]:
7.7E-21mmHg at 25°C

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
H2O: soluble

马来酸噻吗洛尔MSDS

详细MSDS(安全技术说明书)

马来酸噻吗洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UA8475000

CAS REGISTRY NUMBER :: 26921-17-5

LAST UPDATED :: 199512

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C13-H24-N4-O3-S.C4-H4-O4

MOLECULAR WEIGHT :: 432.55

WISWESSER LINE NOTATION :: T6N DOTJ A- DT5NSNJ EO1YQ1MX1&1&1 &QV1U1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 39 mg/kg/87W-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 143,1627,1983

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 5 ug/kg

TOXIC EFFECTS :: Cardiac - other changes Lungs, Thorax, or Respiration - structural or functional change in trachea or bronchi

REFERENCE :: JFAPDE Journal of Family Practice. (Appleton and Lange, East Norwalk, CT) V.1- 1974- Volume(issue)/page/year: 32,97,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1028 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: 6,464,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 381 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1393,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 881 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: 6,464,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1137 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: 12,1204,1981

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 300 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1393,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 805 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: 12,1204,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52500 mg/kg/25W-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1393,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3500 mg/kg/5W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Liver - changes in liver weight Blood - changes in spleen

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1393,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3219 No. of Facilities: 82 (estimated) No. of Industries: 2 No. of Occupations: 11 No. of Employees: 5070 (estimated) No. of Female Employees: 2032 (estimated)

点击显示

马来酸噻吗洛尔安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UA8475000

[ 海关编码 ]:
2934999090

马来酸噻吗洛尔上下游产品

马来酸噻吗洛尔上游产品

马来酸噻吗洛尔下游产品

马来酸噻吗洛尔海关

[ 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%

马来酸噻吗洛尔文献

Different compartmentation of responses to brain natriuretic peptide and C-type natriuretic peptide in failing rat ventricle.

J. Pharmacol. Exp. Ther. 350(3) , 681-90, (2014)

We previously found a negative inotropic (NIR) and positive lusitropic response (LR) to C-type natriuretic peptide (CNP) in the failing heart ventricle. In this study, we investigated and compared the...

Dual drug delivery from vitamin E loaded contact lenses for glaucoma therapy.

Eur. J. Pharm. Biopharm. 94 , 312-21, (2015)

Glaucoma patients frequently instill eye drops multiple times each day, which is a cause for reduced compliance. Additionally, eye drops suffer from other limitations including low bioavailability, wh...

Author reply: To PMID 24576886.

Ophthalmology 121(12) , e68, (2014)

更多文献