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Peer Reviewed
See detailPharmacologic treatment of inner ear: from basic science to the patient.
Lefèbvre, Philippe ULg; Staecker, H.; Van de Water, T. et al

in Acta Oto-Rhino-Laryngologica Belgica (2002), 56(1), 45-9

Most of the deafness are of sensorineural origin and are characterized by a loss of hair cells and of spiral ganglion neurons. At the present time, hearing aids are the only treatment. However, in some ... [more ▼]

Most of the deafness are of sensorineural origin and are characterized by a loss of hair cells and of spiral ganglion neurons. At the present time, hearing aids are the only treatment. However, in some diseases of the inner ear, pharmacological treatment have been proposed and used successfully. In this paper, we will review some basic science aspects of the biology of the neurosensory structures of the inner ear, in particular of the auditory neurons, that lead to the rationale of some treatments for the inner ear diseases. Developmental studies, neuronal cell culture experiments, and analyses of gene knockout animals reveal a number of growth factors which are important for the rescue and repair of injured auditory neurons in the inner ear. These factors rescue the injured auditory neurons in vivo. Furthermore, perfusion of antioxydant to the cochlea prevented the hearing loss induced by cisplatin. These in vitro and in vivo experiments demonstrate that it is possible to manipulate the neurosensory structures of the inner ear and provide an effective treatment to prevent the degeneration of the neurons. The molecules or drugs can be administered locally to the inner ear through a direct perilymphatic perfusion or through the round window membrane. As an example, we will discuss the treatment of patients suffering from idiopathic sensorineural hearing loss which can be treated successfully by a perfusion through the round window membrane, improving their hearing threshold and their speech discrimination. [less ▲]

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See detailPharmacologic treatment of obesity, food intake, and reversal of metabolic disorders.
SCHEEN, André ULg; PAQUOT, Nicolas ULg

in Current Research in Nutrition & Food intake (2007), 3

The present paper is reviewing the current place of weight-reducing drugs in the overall management of overweight/obese subjects, especially those with metabolic disorders and type 2 diabetes. Anti ... [more ▼]

The present paper is reviewing the current place of weight-reducing drugs in the overall management of overweight/obese subjects, especially those with metabolic disorders and type 2 diabetes. Anti-obesity agents should be carefully evaluated in long-term (1-2 years) randomized controlled trials. Recent systematic reviews and meta-analysis assessed both the safety and efficacy of the two drugs currently used in the treatment of obesity, i.e. orlistat, a gastric and pancreatic lipase inhibitor that reduces fat absorption from the gut, and sibutramine, a combined norepinephrine and serotonin reuptake inhibitor that regulates food intake. Rimonabant, a new compound acting as selective blocker of CB1 receptors of the endocannabinoid system, raises much interest as it promotes weight reduction by a central effect and also exerts peripheral effects targeting cardiometabolic risk. Special attention will be paid to beneficial metabolic effects resulting from (even moderate) weight loss and to possible additional effects beyond weight reduction. [less ▲]

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Peer Reviewed
See detailPharmacological analysis of ATP-dependent potassium channel openers on the vascular smooth muscle
Fontaine, J.; Pirotte, Bernard ULg; Lebrun, P.

Poster (1997, February 15)

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Peer Reviewed
See detailPharmacological analysis of ATP-dependent potassium channels openers on vascular smooth muscle
Ouedraogo, R.; Somers, F.; De Tullio, Pascal ULg et al

Conference (1997, April)

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See detailPharmacological characterization of N-tert-butyl-N’-[2-(4’-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time
Dogné, Jean-Michel ULg; Hanson, Julien ULg; De leval, X. et al

in Journal of Pharmacology and Experimental Therapeutics (The) (2004), 309(2), 498-505

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined ... [more ▼]

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor in rats, and to determine its effects on mice bleeding time. Intraperitoneal injection of a single dose of 5 mg/kg BM-573 to rats inhibited U-46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin F-2)-induced washed platelet aggregation 30 min and 1, 2, and 4 h after drug administration with a maximum antiplatelet effect observed after 1 and 2 h. In a rat model of thrombosis induced by ferric chloride application on the abdominal aorta, BM-573 significantly reduced the thrombus weight by 92.53, 80.20, 64.75, and 18.21% at doses of 5, 2, 0.5, and 0.2 mg/kg, respectively. Time to occlusion of abdominal aorta in the BM-573-treated group (41.50+/-5.21 min) was significantly prolonged compared with the vehicle-treated rats (16.16+/-0.79 min). Like furegrelate, seratrodast, and acetylsalicylic acid, BM-573 did not affect the tail bleeding time induced by tail transection in mice compared with vehicle-treated mice. Moreover, BM-573, a close derivative of the loop diuretic torasemide, failed to induce a significant increase in diuresis in rat and did not produce a decrease in blood glucose concentration as observed with the sulfonylurea glibenclamide. In conclusion, we have demonstrated that the nitrobenzenic sulfonylurea BM-573, an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor, is a potent antithrombotic agent that does not affect bleeding time. Moreover, BM-573 lost the diuretic property of torasemide and has no impact on glycemia. [less ▲]

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Peer Reviewed
See detailPharmacological characterization of the enhancement of apomorphine-induced gnawing in mice by cocaine
Tirelli, Ezio ULg; Witkin, J. M.

in Pharmacology, Biochemistry & Behavior (1996), 55(1), 135-140

Characterized the behavioral and pharmacological mechanisms associated with cocaine potentiation of apomorphine (AP)-induced gnawing (AIG) in male C57BL/6J mice. Results showed that (-)-cocaine enhanced ... [more ▼]

Characterized the behavioral and pharmacological mechanisms associated with cocaine potentiation of apomorphine (AP)-induced gnawing (AIG) in male C57BL/6J mice. Results showed that (-)-cocaine enhanced AIG at doses devoid of effects on gnawing when given alone; (+)-cocaine or (-)-cocaine methiodide were also devoid of effects. Lidocaine, a local anesthetic without prominent dopaminergic actions, augmented the gnawing response to AP without increasing climbing or gnawing when given alone. (+)-Amphetamine enhanced AIG gnawing but only at a high dose that increased gnawing by itself. The selective dopamine (DA) uptake blocker, GBR 12909, augmented AIG by itself; however, it increased climbing at doses that augmented the gnawing response. These data indicate that the cocaine-augmented gnawing response to AP may be due to blockade of DA uptake and or the local anesthetic actions of cocaine. ((c) 1997 APA/PsycINFO, all rights reserved) [less ▲]

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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 ▲]

Detailed reference viewed: 15 (1 ULg)
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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

Detailed reference viewed: 4 (0 ULg)
Peer Reviewed
See detailPharmacological evaluation of 4,6-disubstituted 2,2-dimethylchromans structurally related to the KATP channel opener cromakalim
Sebille, S.; Becker, B.; Antoine, M. H. et al

Poster (2000, November 18)

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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

Detailed reference viewed: 13 (4 ULg)
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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)

Detailed reference viewed: 6 (1 ULg)
Peer Reviewed
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)

Detailed reference viewed: 2 (0 ULg)