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Found 2 translations.
Name | Current message text |
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h English (en) | Research investigators at [[Takeda Pharmaceutical Company|Takeda]] discovered in 1982 the weak nonpeptide Ang II antagonists S-8307 and S-8308 from a group of 1-[[Benzimidazole|benzylimidazole]]-5-acetic acid derivatives. S-8307 and S-8308 have moderate [[Potency (pharmacology)|potency]], short duration of action and limited oral bioavailability, however they are selective and competitive AT<sub>1</sub> receptor antagonists without partial agonist activity. A group at DuPont postulated that both Ang II and the Takeda leads were bound at the same receptor site. These two substances served as lead compounds for further optimization of AT<sub>1</sub> receptor blockers. |
h Japanese (ja) | [[Takeda Pharmaceutical Company|武田薬品]]の研究者らは1982年に1-[[Benzimidazole/ja|ベンジルイミダゾール]]-5-酢酸誘導体のグループから弱い非ペプチド性のAng II拮抗薬S-8307とS-8308を発見した。S-8307とS-8308は、中程度の[[Potency (pharmacology)/ja|効力]]、短い作用時間、限られた経口バイオアベイラビリティを持つが、部分作動薬活性を持たない選択的かつ競合的なAT<sub>1</sub>受容体拮抗薬である。DuPont社のグループは、Ang IIと武田薬品のリード化合物が同じ受容体部位に結合していると仮定した。これら2つの物質は、AT<sub>1</sub>受容体遮断薬のさらなる最適化のためのリード化合物となった。 |