In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B2 receptor antagonist in clinical development

Anne Lesage,François Marceau,Christoph Gibson,Brigitte Loenders,Werner Katzer,Horst-Dieter Ambrosi,Jörn Saupe,Alexander Faussner, Evangelia Pardali,Jochen Knolle

International Immunopharmacology（2022）

引用 7|浏览5

暂无评分

摘要

•PHA-022121 is a small molecule antagonist of the bradykinin B2 receptor.•Its in vitro pharmacology is described, as well as that of one of its metabolites.•It has a subnanomolar affinity and is a surmountable and reversible antagonist.•PHA-022121 is highly selective over a wide range of molecular targets.•PHA-022121, orally bioavailable, is ∼20-fold more potent than icatibant.

查看译文

关键词

Bradykinin,B2 receptor,Icatibant,Human umbilical vein,PHA-022121

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要