Glycosidation of chlormadinol acetate alters its actions on Na+/K+-transporting ATPase and cardiac contractility: a contribution to the endogenous digitalis problem.
Compared to the progesterone derivative chlormadinol acetate 1, the arabinofuranoside 2, rhamnoside 3 and glucoside 4 of 1 are less potent in the Na/K-ATPase assay, but evoke, contrary to 1, positive inotropy in vivo. In anaesthetized cats the circulation effects of 2 and 3 appear to be more favourable than those of the digitalis glycoside digitoxin. Hence, the progestin 1 is transformed through glycosidation into an interesting cardioactive steroid.
Weiland
J
J
Central Institute of Molecular Biology, Academy of Sciences of G.D.R., Berlin.
Schwabe
K
K
Hübler
D
D
Schönfeld
W
W
Repke
K R
KR
D000818:Animals; D002415:Cats; D002715:Chlormadinone Acetate / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004074:Digitoxin / Q000494:pharmacology; D007700:Kinetics; D009200:Myocardial Contraction / Q000187:drug effects*; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D002715:Chlormadinone Acetate; C059105:3-O-glucosylchlormadinol acetate; C059236:chlormadinol acetate; C059104:3-O-arabinofuranosylchlormadinol acetate; C059106:3-O-rhamnosylchlormadinol acetate; D004074:Digitoxin; D000254:Sodium-Potassium-Exchanging ATPase