Key result
TP receptor antagonists may restrict vascular inflammation and stabilize vulnerable plaques in atherosclerotic vessels.
Why the study?
TP receptor antagonists have shown potential in treating cardiovascular diseases and restricting vascular inflammation in atherosclerotic vessels, but further therapeutic development is ongoing.
Do TP receptor antagonists and modulators restrict vascular inflammation and cause regression of atherosclerosis in experimental models?
Do TP receptor antagonists and modulators restrict vascular inflammation and cause regression of atherosclerosis in experimental models?
Preclinical evidence suggests that TP receptor antagonists and novel dual-action modulators may be promising therapeutic agents for stabilizing vulnerable plaques and treating atherosclerosis.
TP receptor antagonism may curb vascular inflammation in atherosclerosis; leaves open translation of S18886 from animal models to clinical use.
It had already showed that several thromboxane A(2) receptor (TP receptor) antagonists might be utilized in the treatment of cardiovascular diseases. In addition, recent reports suggested that TP receptor antagonism may be able to restrict vascular inflammation in atherosclerotic vessels. In particular, S18886 has been developed as a non-prostanoid TP receptor antagonist derived from sulotroban that is characterized by a tetrahydronaphthalene ring as a spacer between the 4-cholophenylsulfonamide group and carboxylic acid. Several reports using experimental animal models of atherosclerosis indicated that S18886 caused a regression of advanced atherosclerosis. More recently, several studies and patents showed that new thromboxane modulators combined with another pharmacological activities have been developed. Ohtake et al. discovered TRA-418 (a benzene-condensed heterocyclic derivative) having a TP receptor antagonistic activity and a prostaglandin I(2) receptor agonistic activity. Cesagrande found that 4-methyl-N- (4-trans-nitrooxycyclohexyl)-N-(3-pyridinylmethyl)-1,3- benzenedicarboxamide is endowed with anti-thromboxane and NO-donor actions. Oketani et al. discovered that E3040, a novel benzothiazole derivative, inhibited TXA(2) synthase and 5-LO activities. EK112, a combined angiotensin II and TP receptor antagonist, was developed. These new compounds may be able to restrict further infiltration of inflammatory cells in atherosclerotic vessels, thus stabilizing vulnerable plaques in the related cardiovascular diseases.
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Ishizuka et al. (2006) conducted a review in Atherosclerosis and related cardiovascular diseases. TP receptor antagonists was evaluated. TP receptor antagonists, including novel compounds with combined pharmacological activities, may restrict vascular inflammation and stabilize vulnerable plaques in atherosclerotic vessels.
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