4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール

4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール 化学特性,用途語,生産方法

• 化学的特性

  solid

• 抗菌性

  Pyronaridine is active against the asexual erythrocytic stage of P. falciparum with little or no activity against gametocytes or the hepatic stage. In-vitro blood schizonticide activities are in the range of 0.001–0.03 mg/L, showing a moderate correlation to chloroquine resistance. However, this correlation varies between studies and does not seem to be clinically significant. It is also active against P. vivax, P. ovale and P. malariae. Antagonistic interactions with artemisinins were reported in vitro, but synergy with artesunate has been observed in rodent models.

• 獲得抵抗性

  Decreasing in-vitro sensitivity has been observed in China.

• 応用例（製薬）

  An aza-aminoacridine formulated for oral use. A Mannichbase derivative of mepacrine.

• 薬物動態学

  Peak plasma concentrations are reached after 3–14 h depending upon the formulation; there is also considerable interindividual variation. Elimination half-lives of 63–190 h have been reported, again dependent upon the formulation.

• 臨床応用

  Treatment of uncomplicated P. falciparum and P. vivax malaria
  A fixed-dose combination with artesunate (Pyramax) is being developed for uncomplicated P. falciparum and P. vivax malaria.

• 副作用

  It is well tolerated and no outstanding toxic effects have been reported.

4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール 生産企業

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74847-35-1, 4-[(7-クロロ-2-メトキシベンゾ[b]-1,5-ナフチリジン-10-イル)アミノ]-2,6-ビス(1-ピロリジニルメチル)フェノール キーワード