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- WILHELMI G.
- Pharmacological Laboratory, J.R. Geigy A.G.,
抄録
Already the change from the antipyretic antipyrine, synthesized by L. Knorr (1) in 1883, to aminopyrine, which has not only an antipyretic but also a powerful analgesic effect, was an important step in the development of the pyrazoles. Of the water-soluble aminopyrine analogues, the injectable phenyl-dimethylpyrazolone-methylamino methane sulfonic acid sodium (metamizole) and others had certain advantages with respect to the mode of application.<BR> When, amongst other pyrazolidines, 1, 2-diphenyl-3, 5-dioxo-4-n-butyl-pyrazolidine (phenylbutazone or Butazolidin) was synthesized by Stenzl (2) in 1946, hopes of having found a new analgesic were raised. As this preparation, similar to metamizole, was of acidic nature, it seemed probable that Butazolidin, like metamizole, would have a special anti-inflammatory effect in rheumatic and other inflammatory diseases. This effect was indeed so pronounced that the central analgesic effect lost in significance as compared with the beneficial effect observed in inflammatory states in experimental (3, 4) as well as in clinical trials. The great significance gained by the preparation is due to its antirheumatic action.<BR> Despite this almost specific effect, developments in the field of pyrazoles did not come to a stillstand. Through substitution in the Butazolidin molecule, preparations with other, particular effects were obtained. Thus the 4-(2'-phenyl-sulfinyl-ethyl)-derivative of Butazolidin (Anturan) has primarily uricosuric properties, whereas 1-phenyl-2(p-hydroxyphenyl)-3, 5-dioxo-4-n-butyl-pyrazolidine-monohydrate (oxyphenbutazone or Tanderil), synthesized by Pfister and Häfliger (5) in 1957, had pronounced anti-inflammatory but no definite central analgesic activity. The incidence of side-effects, e.g. from the stomach, was moreover low. Undoubtedly development is not yet terminated; already now new possibilities of action amongst the pyrazoles are being studied.
収録刊行物
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- Jpn.J.Pharmacol.
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Jpn.J.Pharmacol. 15 (2), 187-198, 1965
公益社団法人 日本薬理学会