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See detailPharmacological effects of tiludronate in horses after immobilisation
Delguste, Catherine ULg; Lepage, Olivier M; Doucet, Michèle et al

Poster (2006)

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See detailPharmacological effects of tiludronate in horses after long-term immobilization
Delguste, Catherine ULg; Amory, Hélène ULg; Doucet, Michèle et al

in BONE (2007), 41(3), 414-421

Introduction: Tiludronate, a bisphosphonate, has recently been introduced in veterinary medicine to treat orthopedic conditions in the horse. This study was designed to evaluate its effects on biochemical ... [more ▼]

Introduction: Tiludronate, a bisphosphonate, has recently been introduced in veterinary medicine to treat orthopedic conditions in the horse. This study was designed to evaluate its effects on biochemical biomarkers of bone metabolism and on bone density and structure in an experimental model of disuse osteoporosis induced by cast application in horses. Methods: Two groups of eight horses were immobilized during 8 weeks. The first group (P-group) received a placebo, and the second group (T-group) received tiludronate 1 mg/kg by slow IV infusion. Both treatments were administered twice, 28 days apart. Immobilization consisted of stall rest with the left forelimb packed in a fiberglass cast. It was followed by a 4-week remobilization period and an 8-week standardized training protocol. One biomarker of bone resorption, the C-telopeptides of type 1 collagen cross-links (CTX-1) and one biomarker of bone formation, the bone isoenzyme of alkaline phosphatase (bone ALP), were assessed. Metacarpus III (MCIII) bone mineral density (BMD) and speed of sound (SOS) were evaluated respectively by dual energy X-ray absorptiometry (DEXA) and quantitative ultrasonography (QUS). Lameness was regularly assessed during the remobilization and training periods. Group- and time-related effects were tested by analysis of variance on repeated measurements. Results: A rapid, transient and significant decrease in CTX-1 concentration was seen after each treatment in the T-group only. No significant differences between groups were seen in the evolution of bone ALP activity. At the end of the experiment, the loss of MCIII BMD measured by DEXA in the immobilized limb was significantly less in the T-group than in the P-group. The MCIII SOS measured by QUS did not significantly vary within or between groups throughout the study. Discussion and conclusions: Tiludronate was found to significantly reduce bone resorption during immobilization, as well as to prevent long-term osteopenia in the immobilized limb. Disuse osteopenia did not affect the lateral superficial cortex of MCIII. (C) 2007 Elsevier Inc. All rights reserved. [less ▲]

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See detailPharmacological evaluation of 3-alkylsulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxides structurally related to the KATP channel opener diazoxide
Boverie, S.; Nguyen, Q.-A.; De Tullio, Pascal ULg et al

in Fundamental & Clinical Pharmacology (1999), 13

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See detailPharmacological evaluation of BM-573, a dual thromboxane A(2) receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent
de Leval, X. J.; Dassesse, T.; Benoit, V. et al

in Blood (2003, November 16), 102(11, Part 2), 72

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See detailPharmacological evaluation of BM-573, a dual thromboxane A2 receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent
De Leval, X.; Dassesse, T.; Benoît, V. et al

Poster (2003, December)

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See detailPharmacological evaluation of cromakalim analogues: towards the discovery of new inhibitors of insulin secretion from rat pancreatic Beta-cells
Sebille, S.; becker, B.; Antoine, M. H. et al

in Fundamental & Clinical Pharmacology (2002)

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See detailPharmacological evaluation of cromakalim analogues: towards the discovery of new inhibitors of insulin secretion from rat pancreatic Beta-cells
Sebille, S.; Becker, B.; Antoine, M. H. et al

in Fundamental & Clinical Pharmacology (2002)

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See detailPharmacological evaluation of cromakalim analogues: towards the discovery of new inhibitors of insulin secretion from rat pancreatic β-cells
Sebille, S.; Becker, B.; Antoine, M. H. et al

Poster (2002, March 02)

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See detailPharmacological evaluation of cromakalim analogues: towards the discovery of new inhibitors of insulin secretion from rat pancreatic -cells
Sebille, S.; Becker, B.; Antoine, M. H. et al

in Fundamental & Clinical Pharmacology (2002)

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See detailPharmacological evaluation of original sulfonylureas as thromboxane A2 antagonists
Dogne, J. M.; De Leval, X.; Neven, P. et al

Poster (2000, March 04)

See detailPharmacological evaluation of original sulfonylureas as thromboxane A2 antagonists
Dogne, J.-M.; De Leval, X.; Neven, P. et al

in Fundamental & Clinical Pharmacology (2000), 14

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function
Dogné, Jean-Michel ULg; De Leval, X.; Kolh, Philippe ULg et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003)

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function
Dogne, J. M.; de Leval, X.; Kolh, Philippe ULg et al

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 ▲]

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (II/II). Effects of BM-567 on osteogenic sarcoma-cell-induced platelet aggregation
De Leval, X.; Benoit, V.; Delarge, J. et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003)

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See detailPharmacological evaluation of the thromboxane A2 receptor antagonist BM-613
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, May)

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