Terutroban (S-18886) sodium is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist with an IC50 of 16.4 nM. Terutroban sodium inhibits TXA2 and prostaglandin endoperoxide receptors. Terutroban sodium is a potent antithrombotic agent and possesses anti-atherosclerotic and anti-vasoconstrictor properties [1] [2] [3].
In Vivo, Terutroban (30 mg/kg; i.g.; once a day; 6 weeks) sodium prevents aortic thickening, inhibits vascular cell proliferation, reduces vascular fibrosis, inhibits the expression of HSP47 and TGF-1β without affecting blood pressure in spontaneously hypertensive stroke-prone rats (SHRSPs)[2].
References:
[1]. Wang X, et al. Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists. ACS Med Chem Lett. 2014 Jul 24;5(9):1015-20.
[2]. Gelosa P, et al. Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, prevents hypertensive vascular hypertrophy and fibrosis. Am J Physiol Heart Circ Physiol. 2011 Mar;300(3):H762-8.
[3]. Lesault PF, et al. Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis. Br J Clin Pharmacol.2011 Jun;71(6):844-851.
In Vivo, Terutroban (30 mg/kg; i.g.; once a day; 6 weeks) sodium prevents aortic thickening, inhibits vascular cell proliferation, reduces vascular fibrosis, inhibits the expression of HSP47 and TGF-1β without affecting blood pressure in spontaneously hypertensive stroke-prone rats (SHRSPs)[2].
References:
[1]. Wang X, et al. Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists. ACS Med Chem Lett. 2014 Jul 24;5(9):1015-20.
[2]. Gelosa P, et al. Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, prevents hypertensive vascular hypertrophy and fibrosis. Am J Physiol Heart Circ Physiol. 2011 Mar;300(3):H762-8.
[3]. Lesault PF, et al. Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis. Br J Clin Pharmacol.2011 Jun;71(6):844-851.