Description
Ozagrel HCl (78712-43-3) is a potent and selective inhibitor of thromboxane (TXA2) synthetase (IC50 = 4 nM).1?Does not inhibit prostacyclin (PGI2) synthase, cyclooxygenase or PGE2?isomerase (IC50 > 1 mM).1?Inhibits platelet aggregation2?in vitro?and arachidonate-induced arterial contraction?in vivo. Ozagrel HCl protects against arachidonate-induced sudden death in the rabbit3, and alleviates liver injury induced by acetaminophen overdose in mice4.
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
Antithrombotic;Thromboxane synthase inhibitor
Definition
ChEBI: Ozagrel hydrochloride is an organic molecular entity.
Synthesis
The main synthetic methods of ozagrel hydrochloride are as follows: 1) take p-toluylaldehyde as raw material, get methyl or ethyl p-toluyl cinnamate by Claisen condensation or by Knoevenagl reaction and then esterification, get alkyl p-bromomethyl cinn
References
1) Hiraku?et al. (1986),?Pharmacological studies on the TXA2?synthetase inhibitor (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046); Jpn. J. Pharmacol.,?41?393
2) Naito?et al. (1983), Effects of thromboxane synthetase inhibitors on aggregation of rabbit platelets; Eur. J. Pharmacol.,?91?41
3) Edmonds and Leffer (1984),?Protective actions of a new thromboxane synthetase inhibitor in arachidonate induced sudden death; Life Sci.,?35?1763
4) Tomishima?et al. (2013),?Ozagrel hydrochloride, a selective thromboxane A2?synthase inhibitor, alleviates liver injury induced by acetaminophen overdose in mice; BMC Gastroenterol.,?30?13
