Quantitative structure-pharmacokinetic relationship analysis of pyrrole-imidazole polyamides in rats

• Project/Area Number: 24790174
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Nihon University
• Principal Investigator: AOYAMA Takahiko 日本大学, 薬学部, 助教 (70384633)
• Project Period (FY): 2012-04-01 – 2014-03-31
• Project Status: Completed (Fiscal Year 2013)
• Budget Amount: ¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000); Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000); Fiscal Year 2012: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
• Keywords: ピロール・イミダゾールポリアミド / 薬物動態 / ピロール-イミダゾールポリアミド

Research Abstract

Pyrrole-imidazole (PI) polyamides regulate gene expression to bind specific nucleotide sequences in the minor groove of double-helical DNA with high affinity. PI polyamides are potential therapeutic drugs. In this study, we investigate the quantitative structure-pharmacokinetics relationships of PI polyamides in rats. The distribution volume and plasma protein binding ratio of PI polyamides might be predicted by the molecular structure. The relationships between the clearance and the molecular structure were not detected. To describe the pharmacokinetic characteristics of PI polyamides, further study is needed.

Research Products

• [Presentation] ラットにおけるピロール-イミダゾールポリアミドの定量的構造-薬物動態相関解析 (2014)
  • Author(s): 青山隆彦、荻野知美、上野高浩、福田昇、永瀬浩喜、松本宜明
  • Organizer: 日本薬学会第134年会
  • Place of Presentation: 熊本
  • Year and Date: 2014-03-30
• [Presentation] ラットにおけるピロール - イミダゾールポリアミドの定量的構造-薬物動態相関解析
  • Author(s): 青山隆彦，荻野知美，上野高浩，福田昇，永瀬浩喜，松本宜明
  • Organizer: 日本薬学会第１３４年会
  • Place of Presentation: 熊本
• [Remarks]
  • URL: http://www.pha.nihon-u.ac.jp/page.jsp?id=1956
• [Remarks] 遺伝子発現抑制薬ピロール-イミダゾールポリアミドの構造-薬物動態相関モデルの構築
  • URL: http://www.pha.nihon-u.ac.jp/page.jsp?id=1956
• [Remarks] 薬学部の研究活動 科学研究補助金ケーススタディ.19
  • URL: http://www.pha.nihon-u.ac.jp/page.jsp?id=1956