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1.
J Enzyme Inhib ; 9(2): 111-22, 1995.
Artigo em Inglês | MEDLINE | ID: mdl-8583249

RESUMO

A new p56lck tyrosine kinase inhibitor WIN 61651 [1,4-dihydro-7-(4-methyl-1-piperizinyl)-1-(4-(4-methyl-1-piperi zinyl))phenyl- 4-oxo-3-quinolinecarboxamide) is described. WIN 61651, which is competitive with ATP, demonstrates selectivity for the lymphoid restricted tyrosine kinase p56lck over serine/threonine kinases, such as protein kinase C and protein kinase A, and over some other tyrosine kinases, including erbB2, epidermal growth factor receptor, and insulin receptor; however, it is equipotent for inhibition of p56lck and the platelet derived growth factor receptor tyrosine kinases. WIN 61651 inhibits p56lck activity in cell-free assays, tyrosine kinase activity in a T lymphocytic cell line, and T cell activation, as measured by IL-2 production by purified CD4 positive peripheral blood T lymphocytes and the mixed lymphocyte reaction. WIN 61651 constitutes a new tool for studies on the role for tyrosine kinases in lymphocyte function.


Assuntos
Inibidores Enzimáticos/farmacologia , Piperazinas/farmacologia , Quinolinas/farmacologia , Linfócitos T/efeitos dos fármacos , Linfócitos T/enzimologia , Quinases da Família src/antagonistas & inibidores , Anticorpos/farmacologia , Complexo CD3/imunologia , Antígenos CD4/imunologia , Células Cultivadas , Humanos , Cinética , Proteína Tirosina Quinase p56(lck) Linfócito-Específica , Fosforilação , Linfócitos T/fisiologia , Tirosina/metabolismo
2.
Am J Obstet Gynecol ; 171(6): 1597-600, 1994 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-7802075

RESUMO

OBJECTIVE: Our purpose was to compare oral versus subcutaneous administration of danazol for its effect on elevated serum luteinizing hormone and follicle-stimulating hormone levels in castrated male rats. STUDY DESIGN: A single dose of danazol, either 100 or 400 mg/kg, was administered by gastric intubation or injected subcutaneously. Jugular venipuncture blood samples were taken at 0, 3, 24, and 48 hours and at 7, 10, 15, and 25 days, and serum levels of luteinizing hormone and follicle-stimulating hormone were determined by radioimmunoassay. RESULTS: Gonadotropin levels returned to control values 96 hours after oral administration, whereas 400 mg/kg of danazol administered subcutaneously resulted in suppression of gonadotropins for 25 days. CONCLUSIONS: Subcutaneous administration of danazol results in an unexpectedly prolonged suppression of serum gonadotropins compared with the same dose administered orally. A change from oral administration to a prolonged-release subcutaneous preparation of danazol may enhance the use of this drug in clinical situations and may lessen undesirable side effects.


Assuntos
Danazol/administração & dosagem , Hormônio Foliculoestimulante/antagonistas & inibidores , Hormônio Luteinizante/antagonistas & inibidores , Orquiectomia , Administração Oral , Animais , Danazol/farmacologia , Humanos , Injeções Subcutâneas , Masculino , Radioimunoensaio , Ratos , Fatores de Tempo
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