Document Detail

TP receptor as a therapeutic target in atherosclerosis and related cardiovascular diseases.
MedLine Citation:
PMID:  18221089     Owner:  NLM     Status:  MEDLINE    
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.
Toshiaki Ishizuka; Hideaki Higashino
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Recent patents on cardiovascular drug discovery     Volume:  1     ISSN:  1574-8901     ISO Abbreviation:  Recent Pat Cardiovasc Drug Discov     Publication Date:  2006 Nov 
Date Detail:
Created Date:  2008-01-28     Completed Date:  2008-02-15     Revised Date:  2011-11-10    
Medline Journal Info:
Nlm Unique ID:  101263805     Medline TA:  Recent Pat Cardiovasc Drug Discov     Country:  United Arab Emirates    
Other Details:
Languages:  eng     Pagination:  241-7     Citation Subset:  IM    
Department of Pharmacology, Kinki University School of Medicine, Osaka-Sayama, Osaka 589-8511, Japan.
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MeSH Terms
Atherosclerosis / drug therapy*
Cardiovascular Diseases / drug therapy*
Hydrazines / therapeutic use
Lipoxygenase Inhibitors
Naphthalenes / therapeutic use
Oxidative Stress
Propionic Acids / therapeutic use
Receptors, Thromboxane A2, Prostaglandin H2 / antagonists & inhibitors*,  physiology
Signal Transduction
Reg. No./Substance:
0/3-((6-amino-(4-chlorobenzenesulfonyl)-2-methyl-5,6,7,8-tetrahydronapht)-1-yl)propionic acid; 0/Hydrazines; 0/Lipoxygenase Inhibitors; 0/Naphthalenes; 0/Propionic Acids; 0/Receptors, Thromboxane A2, Prostaglandin H2; 98299-61-7/SQ 29548

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