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Action of antiestrogens on the (Ca 2+ + Mg 2+)-ATPase and Na +/Ca 2+ exchange of brain cortex membranes

Malva, Joāo O. ; Lopes, M.Celeste F. ; Vale, M.Graça P. ; Carvalho, Arsélio P.

Biochemical pharmacology, 1990-10, Vol.40 (8), p.1877-1884 [Periódico revisado por pares]

Elsevier Inc

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  • Título:
    Action of antiestrogens on the (Ca 2+ + Mg 2+)-ATPase and Na +/Ca 2+ exchange of brain cortex membranes
  • Autor: Malva, Joāo O. ; Lopes, M.Celeste F. ; Vale, M.Graça P. ; Carvalho, Arsélio P.
  • É parte de: Biochemical pharmacology, 1990-10, Vol.40 (8), p.1877-1884
  • Descrição: The effect of tamoxifen (TAM) and other antiestrogens on the Ca 2+ transport activity of synaptic plasma membranes (SPM) and microsomal membranes isolated from sheep brain cortex was investigated. The maximal (Ca 2+ + Mg 2+)-ATPase activity of SPM, which is reached at a pCa of about 6.0–6.5, is decreased by about 30% in the presence of 50 μ;M TAM, whereas the (Ca 2+ + Mg 2+-ATPase activity of microsomes, which is maximal at a pCa of about 5.0. is decreased by about 90% by 50 μ;m TAM. In parallel experiments, we observed that the ATP-dependent Ca 2+ uptake is also affected differently by TAM in the two membrane preparations. We found that 50 μ;M TAM inhibits SPM Ca 2+ uptake by about 25–30%, whereas the ATP-dependent Ca 2+ uptake by the microsomal fraction is inhibited by about 60%. No significant effect of TAM was observed on the Na +/Ca 2+ exchange of either membrane system. The results indicate that TAM is a more potent inhibitor of the active, calmodulin-independent Ca 2+ transport system of the intracellular membranes than of that of the plasma membranes, which is calmodulin-dependent. It appears that TAM inhibits calmodulin-mediated reactions, probably through its binding to calmodulin, as we showed previously. However, the Ca 2+ transport system of microsomes, which does not depend on calmodulin, is also particularly sensitive to TAM.
  • Editor: Elsevier Inc
  • Idioma: Inglês
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  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

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