Importance of measuring pharmacologically active metabolites of edoxaban: development and validation of an ultra-high-performance liquid chromatography coupled with a tandem mass spectrometry method.

Although DOACs do not require regular measurements of their blood concentrations, clinical situations may require an assessment of their concentration. Among the factor Xa inhibitors, edoxaban is the only compound for which some metabolites (e.g.

Validation and standardization of the ETP-based activated protein C resistance test for the clinical investigation of steroid contraceptives in women: an unmet clinical and regulatory need.

Background Regulatory bodies recommend the use of an assay based on the assessment of the endogenous thrombin potential (ETP) for the investigation of the activated protein C resistance (APCr) in the development of steroid contraceptives in women. However, the assays described in the literature are home-made and not standardized regarding the method, the reagents, the reference plasma and the quality controls. In the absence of any commercially available method, we aimed at validating the ETP-based APCr assay.

Effects of leaf extracts from Croton zambesicus Müell. Arg. on hemostasis.

Ethnopharmacological Relevance: The leaf decoction of Croton zambesicus Müell. Arg. (Euphorbiaceae; syn.

Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor.

Thromboxane A(2) (TXA(2)) is an arachidonic acid metabolite involved in pathologies such as stroke, myocardial infarction, and atherosclerosis. Consequently, the design of TXA(2) receptor (TP) antagonists remains of great interest in cardiovascular medicine. The actions of TXA(2) are mediated by its specific G-protein coupled receptor of which two alternative spliced isoforms, TPalpha and TPbeta, have been described in humans.

Differential regulation of chondrocyte metabolism by oncostatin M and interleukin-6.

Objective: To determine the effects of interleukin (IL)-6 and oncostatin M (OSM) added separately or in combination with IL-1beta on human osteoarthritic (OA) chondrocytes in alginate beads.

Design: Human chondrocytes were isolated from OA cartilage and cultured in alginate beads for 12 days, in the absence or in the presence of increasing amounts of IL-6 (20-500ng/ml) with its soluble receptor or OSM (0.1-10ng/ml) and with or without IL-1beta (1.