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酮咯酸氨丁三醇

酮咯酸氨丁三醇用途

Ketorolac tromethamine salt 是一种非甾体抗炎剂,为非选择性的 COX 抑制剂,对 COX-1 和 COX-2 的 IC50 值分别为 20 nM 和 120 nM。

酮咯酸氨丁三醇名称

[ CAS 号 ]:
74103-07-4

[ 中文名 ]:
酮咯酸氨丁三醇

[ 英文名 ]:
Ketorolac tromethamine

[中文别名 ]:

辛太克斯(浮选剂)

[英文别名 ]:

Ketorolac tromethamine
Ketorolac tris salt
rac Ketorolac Tromethamine Salt
(±)-Ketorolac Tromethamine Salt
MFCD00887595
Ketorolac (tromethamine salt)

酮咯酸氨丁三醇生物活性

[ 描述 ]:

Ketorolac tromethamine salt 是一种非甾体抗炎剂,为非选择性的 COX 抑制剂,对 COX-1 和 COX-2 的 IC50 值分别为 20 nM 和 120 nM。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

[ 靶点 ]

COX-1:20 nM (IC50)

COX-2:120 nM (IC50)

[体外研究]

Ketorolac是一种非甾体类抗炎药,作为非选择性COX抑制剂,COX-1的IC50为20 nM,COX-2的IC50为120 nM [1]。

[体内研究]

酮咯酸氨丁三醇(0.4％)引起LPS内毒素诱导的前房FITC-葡聚糖增加几乎完全抑制,并且兔房水中PGE2水溶液浓度增加[1]。酮黄素(30 mg/kg,iv)迅速逆转大鼠的痛觉过敏。酮咯酸还可以减少角叉菜胶诱导的痛觉过敏和爪子PG的产生,并导致大鼠PGE2水平降低[1]。酮咯酸(4mg/kg /天,口服)对大鼠肺泡窝内形成的骨小梁的体积分数没有不利影响[2]。酮咯酸(60μg/10μL)可减少组织学变化,如缺血性细胞死亡,包括细胞质嗜酸粒细胞增多,细胞结构崩解和大鼠核固缩。酮咯酸还可有效减少神经元死亡,改善后肢运动功能,长期生存与对照组相似[3]。

[动物实验]

大鼠[2]治疗的大鼠接受口服剂量的1mL对乙酰氨基酚水溶液（80mg / kg /大鼠/天），酮咯酸（4mg / kg /天）或etoricoxib（10mg / kg /天）通过管饲法给予手术当天直到死亡，2周后。对照大鼠接受自来水（通过管饲法1mL /天）。将动物饲养在气候控制的环境中（12小时光照/ 12小时黑暗，20-24℃），可自由进入标准实验室饲料和自来水[2]。

[参考文献]

[1]. Waterbury LD, et al. Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40.

[2]. Fracon RN, et al. Treatment with paracetamol, ketorolac or etoricoxib did not hinder alveolar bone healing: a histometric study in rats. J Appl Oral Sci. 2010 Dec;18(6):630-4.

[3]. Hsieh YC, et al. Intrathecal ketorolac pretreatment reduced spinal cord ischemic injury in rats. Anesth Analg. 2005 Apr;100(4):1134-9.

[相关活性小分子]

酮咯酸氨丁三醇物理化学性质

[ 沸点 ]:
493.2ºC at 760 mmHg

[ 熔点 ]:
160-161ºC

[ 分子式 ]:
C₁₉H₂₄N₂O₆

[ 分子量 ]:
376.404

[ 闪点 ]:
252.1ºC

[ 精确质量 ]:
376.163422

[ PSA ]:
146.01000

[ LogP ]:
0.65210

[ 外观性状 ]:
结晶

[ 储存条件 ]:
Hygroscopic, Refrigerator, Under Inert Atmosphere

[ 水溶解性 ]:
H2O: 15 mg/mL stable at least one month at −20 °C., soluble

酮咯酸氨丁三醇MSDS

详细MSDS(安全技术说明书)

酮咯酸氨丁三醇毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY7759900

CAS REGISTRY NUMBER :: 74103-07-4

LAST UPDATED :: 199712

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C15-H13-N-O3.C4-H11-N-O3

MOLECULAR WEIGHT :: 376.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 15 mg/kg/6D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - changes in potassium Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 153,1000,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 19853 ug/kg/12D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 27,1055,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 857 ug/kg

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 32,305,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 8400 ug/kg/3D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - changes in potassium

REFERENCE :: AJKDDP American Journal of Kidney Diseases. (Grune & Stratton, Inc., Journal Subscription Dept., POB 6280, Duluth, MN 55806) V.1- 1981- Volume(issue)/page/year: 24,578,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1200 ug/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Lungs, Thorax, or Respiration - bronchiolar constriction Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: SMJOAV Southern Medical Journal. (Southern Medical Assoc., POB 2446, Birmingham, AL 35205) V.1- 1908- Volume(issue)/page/year: 87,282,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 858 ug/kg

TOXIC EFFECTS :: Cardiac - pulse rate increase, without fall in BP Lungs, Thorax, or Respiration - dyspnea Immunological Including Allergic - anaphylaxis

REFERENCE :: APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 26,1237,1992

酮咯酸氨丁三醇安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335

[ 警示性声明 ]:
P261-P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R25;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S45

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
UY7759900

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2942000000

酮咯酸氨丁三醇海关

[ 海关编码 ]: 2942000000

酮咯酸氨丁三醇文献

Topical cyclosporine a 1% for the treatment of chronic ocular surface inflammation.

Eye Contact Lens 40(5) , 283-8, (2014)

To evaluate the use of topical cyclosporine A (CsA) 1% emulsion in the treatment of chronic ocular surface inflammation (OSI).We conducted a retrospective chart review of patients with various forms o...

Ketorolac eye drops reduce inflammation and delay re-epithelization in response to corneal alkali burn in rabbits, without affecting iNOS or MMP-9.

Arq. Bras. Oftalmol. 78 , 67-72, (2015)

To assess the effects of 0.5% ketorolac tromethamine without preservatives on the expression of iNOS and MMP-9 in alkali burn ulcers.Twelve eyes of 120-day-old male rabbits were treated (TG) every 6 h...

Ketorolac tromethamine pharmacokinetics and metabolism after intravenous, intramuscular, and oral administration in humans and animals.

Pharmacotherapy 10(6 ( Pt 2)) , 33S-39S, (1990)

In humans, ketorolac is completely bioavailable and its kinetics are linear. It is absorbed rapidly (half-life for absorption 3.8 min) after oral (fasting) and intramuscular administration; food delay...

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