Renin inhibition by synthetic phosphatidyl and phosphorylethanolamines.
Renin inhibitory effects of about 30 kinds of newly synthesized Phosphatidyl-E and Phosphoryl-E were studied in vitro and in vivo. Among the synthetic Phosphatidyl-E, PE (SEE ARTICLE) SERies were the most potent and these were stronger than natural Phosphatidyl-E. We also confirmed that the converison from the original Phosphatidyl-E, so called prerenininhibitor, to lyso-form to exhibit renin inhibition as mentioned by Sen et al15,16 and Baggio et al.20 was not essential. But a stronger inhibition to renin was observed in PE-72, one of synthetic Phosphoryl-E analogues. PE-104, Phosphoryl-E without long fatty acid chain, was the most potent inhibitor in this study. PE-72 and PE-104 inhibited the reaction between dog renin and substrate in a competitive way. In dogs and rats, Phosphoryl-E decreased hypertensive responce and increase angiotensin I concentration induced by the exogenous renin. Hypotensive effects of Phosphatidyl-E and Phosphoryl-E were also demonstrated in renal hypertensive rats and not in normotensive rats.
D000808:Angiotensinogen; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D004983:Ethanolamines / Q000494:pharmacology; D009943:Organophosphorus Compounds / Q000494:pharmacology; D051381:Rats; D000092502:Renin Inhibitors
D000808:Angiotensinogen; D004983:Ethanolamines; D009943:Organophosphorus Compounds; D000092502:Renin Inhibitors; C005448:phosphorylethanolamine