基本信息

技术规格

物性(参考值)

安全信息

相关法规

基本信息

产品描述

Ozagrel HCl是选择性血栓素A2合成酶抑制剂，其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩，以及伴随的脑梗塞。

靶点（IC50 & Targe）

Thromboxane A2 synthetase,11nM

体内研究

在豚鼠体内，Ozagrel防止油酸(OA)诱导的血栓素A(2)产生和随后支气管肺灌洗液中总蛋白质浓度和巨噬细胞与嗜中性粒细胞数量的增加，以及全肺中单核细胞趋化蛋白1与白介素-8 mRNA表达的增加。[1] Ozagrel (3 mg/kg)减少大鼠大脑中动脉脑缺血再灌注后皮层脑梗死的面积和体积。在微血栓形成的大鼠模型中，Ozagrel也对神经功能缺损具有抑制作用。[2]在有意识的脑缺血再灌注小鼠模型中，Ozagrel改善退化的自发运动活性和运动协调梗阻。在猫体内，Ozagrel抑制脑缺血再灌注SHR模型中阻塞再灌注诱导的脑组织比重下降，并且在大脑中动脉闭塞再灌注后，恢复缺血后脑皮层PO(2)的减少。Ozagrel也会增加脑缺血再灌注后脑组织中6-keto-PGF(1alpha)，一种前列腺素I(2) (PGI(2))代谢物的水平，而PGI(2)给药提高有意识的脑缺血再灌注小鼠模型中降低的自发运动活性。[3] 在豚鼠体内，Ozagrel在注射油酸前30分钟静脉给药防止Pao(2)降低和肺血管高渗透性。在豚鼠体内，Ozagrel也会防止乳酸脱氢酶活性，肺细胞损伤的量度，TXB(2)，和支气管肺泡灌洗液中其与6-酮前列腺素F(1α)的比重的增加。[4]

参考文献

[1] Ishitsuka Y, et al. J Pharmacol Sci, 2009, 111(2), 211-215.

[2] Imamura T, et al. Arzneimittelforschung, 2003, 53(10), 688-694.

[3] Ichikawa K, et al. Pharmacology, 1999, 59(5), 257-265.

[4] Ishitsuka Y, et al. J Pharm Pharmacol, 2004, 56(4), 513-520.

[5] Naito J, et al. Eur J Pharmacol. 1983, 91(1), 41-48.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III
WGK	2
RTECS	UD3380000

产品说明

应用

Ozagrel hydrochloride hydrate has been used as a thromboxane synthase inhibitor:

• in high cholesterol-diet rats (HC) to test its effect on arteriolar constriction
• to pre-treat mice to test its effect on lipopolysaccharide (LPS)-induced behavioral changes
• to test its effect on arteriolar vasoconstriction in hyperglycemic mice

包装

5, 25 mg in glass bottle

生化/生理作用

Ozagrel is useful in treating lacunar and thrombotic stroke. It blocks vasoconstriction and platelet aggregation. Ozagrel aids in improving the prostacyclin (PGI2)/ thromboxane A2 (TXA2) in the acute phase of cerebral ischemia. It improves endothelial dysfunction in L-methionine-induced hyperhomocysteinemia (HHcy)-induced vascular cognitive impairment and dementia (VCID).
Ozagrel is a selective thromboxane A₂ synthase (TXA₂) inhibitor.

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: . P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see . on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to local regulations.