Thiocardenolides I: synthesis and biological actions of 3beta-thiocyanato-14beta-hydroxy-5beta-card-20(22)-enolide.
The synthesis of a 3beta-thiocyanatocardenolide is described. The compound exhibited about 0.1 times the cardiotonic effect of digitoxyigenin in the isolated frog heart preparation. At a dosage of 20 mg/kg in the intact rat, it elicited ECG changes similar to those seen with a 10-mg/kg dose of digitoxigenin. Studies also revealed the new cardenolide to be a reversible inhibitor of sodium- and potassium-activated adenosine triphosphatase.
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors; D000818:Animals; D001921:Brain / Q000201:enzymology; D002297:Cardanolides / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D010042:Ouabain / Q000378:metabolism; D051381:Rats; D013997:Time Factors
D002297:Cardanolides; D010042:Ouabain; D000251:Adenosine Triphosphatases