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SHR Neuro Krebs Kardio Lipid

Philipose, S; Konya, V; Lazarevic, M; Pasterk, LM; Marsche, G; Frank, S; Peskar, BA; Heinemann, A; Schuligoi, R.
Laropiprant Attenuates EP3 and TP Prostanoid Receptor-Mediated Thrombus Formation.
PLoS One. 2012; 7(8):e40222-e40222 [OPEN ACCESS]
Web of Science PubMed PUBMED Central FullText FullText_MUG

 

Autor/innen der Med Uni Graz:
Frank Saša
Heinemann Akos
Konya Viktoria
Marsche Gunther
Philipose Sonia
Schuligoi Rufina
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Number of Figures: 6
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Abstract:
The use of the lipid lowering agent niacin is hampered by a frequent flush response which is largely mediated by prostaglandin (PG) D(2). Therefore, concomitant administration of the D-type prostanoid (DP) receptor antagonist laropiprant has been proposed to be a useful approach in preventing niacin-induced flush. However, antagonizing PGD(2), which is a potent inhibitor of platelet aggregation, might pose the risk of atherothrombotic events in cardiovascular disease. In fact, we found that in vitro treatment of platelets with laropiprant prevented the inhibitory effects of PGD(2) on platelet function, i.e. platelet aggregation, Ca(2+) flux, P-selectin expression, activation of glycoprotein IIb/IIIa and thrombus formation. In contrast, laropiprant did not prevent the inhibitory effects of acetylsalicylic acid or niacin on thrombus formation. At higher concentrations, laropiprant by itself attenuated platelet activation induced by thromboxane (TP) and E-type prostanoid (EP)-3 receptor stimulation, as demonstrated in assays of platelet aggregation, Ca(2+) flux, P-selectin expression, and activation of glycoprotein IIb/IIIa. Inhibition of platelet function exerted by EP4 or I-type prostanoid (IP) receptors was not affected by laropiprant. These in vitro data suggest that niacin/laropiprant for the treatment of dyslipidemias might have a beneficial profile with respect to platelet function and thrombotic events in vascular disease.
Find related publications in this database (using NLM MeSH Indexing)
Blood Coagulation - drug effects
Blood Platelets - cytology
Calcium - metabolism
Dyslipidemias - drug therapy
Female -
Gene Expression Regulation - drug effects
Humans -
Hypolipidemic Agents - therapeutic use
Indoles - pharmacology
Male -
Niacin - therapeutic use
P-Selectin - biosynthesis
Platelet Aggregation - drug effects
Platelet Glycoprotein GPIIb-IIIa Complex - biosynthesis
Prostaglandin D2 - metabolism
Receptors, Prostaglandin E, EP3 Subtype - biosynthesis
Thrombosis - metabolism

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