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New indole amide derivatives as potent CRTH2 receptor antagonists.
Bioorg Med Chem Lett
June 2011
Medicinal Chemistry, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1.
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave as a full antagonists, exhibiting good selectivity over related prostaglandin receptors.
View Article and Find Full Text PDFAccess and perceived need for physical and occupational therapy in chronic arthritis.
Disabil Rehabil
January 2011
Université de Montréal, Ecole de Réadaptation, C.P. 6128, Succ. Centre-Ville, Pavillon 7077 du Parc, Montreal, Quebec, Canada H3C3J7.
Purpose: Physical and occupational therapy are beneficial for persons with chronic arthritis; however, access is problematic. The goal was to examine issues related to access to these services for patients with chronic arthritis.
Methods: We used two data sources: 1) questionnaires sent to a random sample of 600 family physicians and to all 85 rheumatologists in the province of Quebec; and 2) interviews of 211 patients with physician-confirmed chronic arthritis recruited from 34 primary care settings in Quebec.
In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites.
Bioorg Med Chem Lett
January 2007
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Que., Canada H9R 4P8.
Metabolites of the potent DP antagonist, MK-0524, were generated using in vitro systems including hepatic microsomes and hepatocytes. Four metabolites (two hydroxylated diastereomers, a ketone and an acyl glucuronide) were characterized by LC-MS/MS and 1H NMR. Larger quantities of these metabolites were prepared by either organic synthesis or biosynthetically to be used as standards in other studies.
View Article and Find Full Text PDFMobilization by either cyclophosphamide or granulocyte colony-stimulating factor transforms the bone marrow into a highly proteolytic environment.
Exp Hematol
May 2002
Stem Cell Biology Laboratory, Peter MacCallum Cancer Institute, Melbourne, Victoria, Australia.
Objective: Hematopoietic stem and progenitor cells normally reside in the bone marrow but can be mobilized into the peripheral blood following treatment with granulocyte colony-stimulating factor (G-CSF) or myelosuppressive chemotherapy. Although the number of transplants performed with mobilized blood currently exceeds those performed with bone marrow, little is known of the molecular mechanisms responsible for this phenomenon. We sought to determine whether mobilization induced by G-CSF or chemotherapy was triggered by common or distinct mechanisms.
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