Inhibition of beef-brain and dog-heart (Na+ + k+) activated adenosine triphosphatase by carbon-3 branched cardenolides.
Twenty-two C-3 branched cardenolides were investigated as inhibitors of beef-brain and dog-heart (Na+ + k+) activated adenosine triphosphatase. The synthetic compounds had lower inhibitory strength than digitoxigenin, and there was no indication of an improved safety index. Structure--activity relationships show that increased steric shielding of the 3-OH group results in reduced inhibition.
D000818:Animals; D001921:Brain / Q000201:enzymology; D002298:Cardenolides / Q000494:pharmacology*; D002417:Cattle; D004073:Digitoxigenin / Q000031:analogs & derivatives / Q000494:pharmacology; D004285:Dogs; D066298:In Vitro Techniques; D008861:Microsomes / Q000201:enzymology; D009206:Myocardium / Q000201:enzymology; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D002298:Cardenolides; D004073:Digitoxigenin; D000254:Sodium-Potassium-Exchanging ATPase