TS-011

TS-011 is a selective inhibitor of 20-Hydroxyeicosatetraenoic acid synthesis.

Signaling Pathways >> Others >> Others

Research Areas >> Cardiovascular Disease

TS-011 is a selective inhibitor of 20-Hydroxyeicosatetraenoic acidsynthesis. TS-011 at a dose of 0.3 mg/kg inhibits the reduction in the blood flow velocities at 1 and 7 h after reperfusion (P<0.001). In addition, TS-011 inhibits the increase in the blood flow velocity at 24 h after reperfusion (P<0.01). TS-011 protects the microvascular perfusion area from the loss observed in vehicle-treated mice. TS-011, at a dose of 0.3 mg/kg, also reduces the infarct volume by almost 40% (P<0.05)[1]. In 9 dogs with delayed vasospasm, acute blockade of the synthesis of 20-HETE with TS-011 (1 mg/kg IV) significantly increases the diameter of the basilar artery by 39%[2].

The studies are performed using 58 male C57BL/6J mice (8 weeks old) weighing 20 to 26 g. TS-011 (0.3 mg/kg) or a vehicle is infused intravenously for 1 h every 6 h in a mouse model of stroke, induced by transient occlusion of the middle cerebral artery occlusion following photothrombosis. The cerebral blood flow velocity and the vascular perfusion area of the peri-infarct microvessels are measured using in vivo two-photon imaging[1].

[1]. Marumo T, et al. The inhibitor of 20-HETE synthesis, TS-011, improves cerebral microcirculatory autoregulation impaired by middle cerebral artery occlusion in mice. Br J Pharmacol. 2010 Nov;161(6):1391-402.

[2]. Hacein-Bey L, et al. Reversal of delayed vasospasm by TS-011 in the dual hemorrhage dog model of subarachnoid hemorrhage. AJNR Am J Neuroradiol. 2006 Jun-Jul;27(6):1350-4.

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