SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 µmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 µmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 µmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
Molekulargewicht:
620.74
CAS Nummer:
[115766-42-2]
Formel:
C32H44N8O5
Target-Kategorie:
Renin
Anwendungsbeschreibung:
MCE Product type: Reference compound
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