Cardiotonic activity of the water soluble forskolin derivative 8,13-epoxy-6 beta-(piperidinoacetoxy)- 1 alpha, 7 beta, 9 alpha-trihydroxy-labd- 14en-11-one.
8,13-Epoxy-6 beta-(piperidinoacetoxy)-1 alpha,7 beta, 9 alpha-trihydroxy-labd -14en-11-one (HL 706, CAS 114376-11-3) is a water soluble derivative of forskolin with positive inotropic and vasodilating properties. In both in vitro and in vivo preparations, it exhibited significant positive inotropic activity with concomitant increase in heart rate and decrease in mean blood pressure. Though its potency is lower than that of forskolin, its duration of action is more prolonged. In conscious dog experiments, HL 706, administered orally, also showed a dose related increase in LV dP/dtmax. A significant reversal of cardiac failure was attained in anaesthetised dogs subjected to propranolol induced cardiac insufficiency. HL 706, like forskolin increased cAMP by virtue of its adenylate cyclase stimulant activity. Through increase in cAMP it also exhibited non-specific smooth muscle relaxant activity in isolated vascular and ileal preparations. Its therapeutic ratio is quite favourable.
Rajagopalan
R
R
Hoechst India Limited, Bombay India.
Ghate
A V
AV
Subbarayan
P
P
Linz
W
W
Schoelkens
B A
BA
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000758:Anesthesia; D000818:Animals; D002316:Cardiotonic Agents / Q000494:pharmacology* / Q000633:toxicity; D002415:Cats; D005576:Colforsin / Q000031:analogs & derivatives* / Q000494:pharmacology; D006224:Cricetinae; D004285:Dogs; D004562:Electrocardiography; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006333:Heart Failure / Q000188:drug therapy / Q000503:physiopathology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007262:Infusions, Intravenous; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male; D008647:Mesocricetus; D009130:Muscle, Smooth / Q000187:drug effects; D015428:Myocardial Reperfusion Injury / Q000503:physiopathology; D010210:Papillary Muscles / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D011433:Propranolol / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012039:Regional Blood Flow / Q000187:drug effects
D002316:Cardiotonic Agents; C066607:6-((piperidino)acetoxy)-7-desacetylforskolin; D005576:Colforsin; D000244:Adenosine Diphosphate; D011433:Propranolol; D007545:Isoproterenol