RESUMEN

Analogues of bradykinin were synthesized containing single substitutions by N alpha-methyl amino acids in the 1, 4, 5, 5, and 9 positions. [MeArg]Bradykinin possessed 60% of the muscle-contracting activity of the parent compound in a guinea pig ileum assay. The other analogues were very weak agonists (less than 2%) and, disappointingly, failed to show blocking activity except at very high doses.

Asunto(s)

Bradiquinina/análogos & derivados , Animales , Bradiquinina/antagonistas & inhibidores , Bradiquinina/síntesis química , Bradiquinina/farmacología , Cobayas , Técnicas In Vitro , Metilación , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos

Asunto(s)

Ácidos , Cetonas , Esteroides , Fenómenos Químicos , Química