selective inhibitor of thromboxane synthase
CAS：4238-71-5
分子式：C10H10N2
分子量：158.2
纯度：98%
存储：Store at -20°C

Background:

Benzylimidazole is a selective inhibitor of thromboxane synthase and a stimulator of UDP-glucuronosyltransferase [1,2].

Thromboxane synthase is a cytochrome P450 enzyme. The cytochrome P450 proteins have been involved in catalyzing many reactions involved in drug metabolism and synthesis of cholesterol, steroids, and other lipids. The enzyme plays an important role in several pathophysiological processes including hemostasis, cardiovascular disease, and stroke. The gene expresses two transcript variants [3].

1-Benzylimidazole selectively inhibited the activity of thromboxane synthase. 1-Benzylimidazole reduced TXB2 levels and increased blood flow in ischemia-reperfusion injury of rat brain [1]. In male Wistar rats, gastrically administration of 1-benzylimidazole (25, 75 and 100 mg/kg/day) caused a dose-dependent hepatomegaly. 1-Benzylimidazole decreased the plasma level in triglycerides by 60–70%. 1-benzylimidazole stimulated three distinct forms of UDP-glucuronosyltransferase. 1-benzylimidazole significantly increased the activities towards 4-methylumbelliierone, 1-naphthol, morphine or a monoterpenoid alcohol, nopol [2]. Benzylimidazole increased hepatocellular CYP1A catalytic activity and CYP1A mRNA in a concentration-dependent way [4].

参考文献:
[1] Pettigrew L C, Grotta J C, Rhoades H M, et al.  Effect of thromboxane synthase inhibition on eicosanoid levels and blood flow in ischemic rat brain[J]. Stroke, 1989, 20(5): 627-632
[2]. Magdalou J, Totis M, Boiteux-Antoine A F, et al. Effect of 1-benzylimidazole on cytochromes P-450 induction and on the activities of epoxide hydrolases and UDP-glucuronosyltransferases in rat liver[J]. Biochemical pharmacology, 1988, 37(17): 3297-3304.
Shen R F, Tai H H.  Thromboxanes: synthase and receptors[J]. Journal of biomedical science, 1998, 5(3): 153-172.
[3] Shen R F, Tai H H.  Thromboxanes: synthase and receptors[J]. Journal of biomedical science, 1998, 5(3): 153-172.
[4] Navas J M, Chana A, Herradón B, et al.  Induction of CYP1A by the N‐imidazole derivative, 1‐enzylimidazole[J]. Environmental toxicology and chemistry, 2003, 22(4): 830-836.