Description
Ozagrel HCl (78712-43-3) is a potent and selective inhibitor of thromboxane A2 (TXA2) synthetase (IC50 = 4 nM). It does not inhibit prostacyclin (PGI2) synthase, cyclooxygenase, or PGE2 isomerase (IC50 > 1 mM)[1]. Ozagrel HCl inhibits platelet aggregation in vitro[2] and arachidonate-induced arterial contraction in vivo. It protects against arachidonate-induced sudden death in rabbits[3] and alleviates liver injury induced by acetaminophen overdose in mice[4].
History
Ozagrel hydrochloride was initially developed jointly by Ono Pharmaceutical Co., Ltd. and Kissei Pharmaceutical Co., Ltd. in Japan. Approved for marketing in Japan in 1988, it became the world's first commercially available potent thromboxane A2 (TXA2) synthase inhibitor. This medication is primarily indicated for the treatment of patients with ischaemic cerebrovascular disease, as it exhibits dual effects of inhibiting platelet aggregation and dilating blood vessels, thereby effectively preventing thrombus formation.
Uses
Ozagrel Hydrochloride is a selective thromboxane A2 synthase inhibitor, which alleviates liver injury induced by acetaminophen overdose in mice.
Definition
ChEBI: Ozagrel hydrochloride is an organic molecular entity.
References
[1] SEIJI HIRAKU . Pharmacological Studies on the TXA2 Synthetase Inhibitor (E)-3-[p(1H-lmidazol-1-Ylmethyl)Phenyl]-2-Propenoic Acid (OKY-046)[J]. Japanese journal of pharmacology, 1986, 41 3: Pages 393-401. DOI:
10.1254/jjp.41.393[2] JUN NAITO . Effects of thromboxane synthetase inhibitors on aggregation of rabbit platelets[J]. European journal of pharmacology, 1983, 91 1: Pages 41-48. DOI:
10.1016/0014-2999(83)90359-x[3] LEE C. EDMONDS Allan M L. Protective actions of a new thromboxane synthetase inhibitor in arachidonate induced sudden death[J]. Life sciences, 1984, 35 17: Pages 1763-1768. DOI:
10.1016/0024-3205(84)90273-x[4] YOSHIRO TOMISHIMA. Ozagrel hydrochloride, a selective thromboxane A₂ synthase inhibitor, alleviates liver injury induced by acetaminophen overdose in mice.[J]. BMC Gastroenterology, 2013, 13: 21. DOI:
10.1186/1471-230x-13-21
