EFFECTS OF BUFALIN AND RELATED CARDIOTONIC STEROIDS IN THE NEUROMUSCULAR JUNCTION

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概要

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• Bufosteroids, bufalin (4-5×10<SUP>-5</SUP> g/ml), cinobufagin (7×10<SUP>-5</SUP>) and resibufogenin (1×10<SUP>-4</SUP>) showed a neuromuscular block in rat isolated diaphragm preparations, while digitoxigenin and ouabain showed no such block. A block of the twitch induced by direct stimulation was observed in the denervated preparations only. Presumably, bufalin can be classified as a depolarizing blocking agent such as succinylcholine, however, differed in the following: blocking effect was potentiated in a bath deficient in sodium ions; it was sensitive to stimulus frequency change; lower doses of bufalin increased the post-tetanic potentiation and antagonized the blocking effect induced by magnesium. These findings suggest that bufalin has a pre-synaptic effect presumably concerned with the bufalin-induced block.

著者

• Sakai Takeshi

  Division of Environmental Biology, The National Institute for Environmental Studies

• Yoshida Seiichiro

  Division of Pharmacology, Research Laboratories, Taisho Pharmaceutical Co., Ltd.

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