Effect of heart failure on dipeptidyl peptidase IV activity in plasma of dogs.

in Journal of Veterinary Internal Medicine (2012)

Structure-based pharmacophore of COX-2 selective inhibitors and identification of original lead compounds from 3D database searching method

in European Journal of Medicinal Chemistry (2006), 41

Pharmacophore generation to design new leads for selective cyclooxygenase-2 inhibition

Poster (2004, October 07)

Identification d’un inhibiteur COX-2 sélectif », 18èmes Journées Franco-belges de Pharmacochimie

Poster (2004, June)

Identification of COX-2 selective inhibitor

in Fundamental & Clinical Pharmacology (2004)

Pyridinic sulfonamides as potential COX-2 inhibitors

Poster (2003, May)

Pharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003), 68(1), 49-54

The aim of this work was to evaluate the effects of BM-567 ( N-pentyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative. on both thromboxane A(2) (TXA(2)) receptors (TP) and ... [more ▼]

The aim of this work was to evaluate the effects of BM-567 ( N-pentyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative. on both thromboxane A(2) (TXA(2)) receptors (TP) and thromboxane synthase of human platelets. The drug affinity for TP receptors of human washed platelets has been determined. In this test BM-567 showed a high affinity (IC50: 1.1+/-0.1 nM) for the TP receptors in comparison with BM-531 (IC50: 7.8+/-0.7 nM) and sulotroban (IC50: 931+/-85 nM), two TXA(2) antagonists. We also demonstrated that BM-567 prevented platelet aggregation induced by arachidonic acid (AA) (600 muM) (ED100: 0.20+/-0.10muM), U-46619, a stable TXA(2) agonist (1 muM) (ED50: 0.30+/-0.04 muM) and collagen (1 mug ml(-1)) (% of inhibition: 44.3+/-4.3% at 10 muM) and inhibited the second wave of ADP (2 muM). Moreover, when BM-567 was incubated in whole blood from healthy donors, the closure time measured by the Platelet Function analyzer (PFA-100) was significantly prolonged (closure time: 215+/-21 s) by using collagen/epinephrine cartridges. Finally, at the concentration of 1 muM, BM-567 completely reduced the TXB2 production from human platelets stimulated with AA (600 muM). These results indicate that BM-567 is a novel combined TXA(2) receptor antagonist and thromboxane synthase inhibitor characterized by a powerful antiplatelet potency. (C) 2002 Elsevier Science Ltd. All rights reserved. [less ▲]

Rationalization of the binding mode of pyridinic compounds derived from nimesulide, a preferential cyclooxygenase-2 inhibitor

Poster (2002, November 15)

Rationalization of the binding mode of pyridinic compounds derived from nimesulide, a preferential cyclooxygenase-2 inhibitor

Poster (2002, September 26)

Effects of thromboxane A2 receptor antagonists and thromboxane synthase inhibitors on osteogenic sarcoma cell-induced platelet aggregation

Poster (2002, March 02)