Trapidil derivatives as potent inhibitors of cyclic AMP phosphodiesterase from heart and coronary arteries.
New trapidil derivatives were found to be more potent inhibitors of cyclic AMP phosphodiesterase activity from heart and coronary arteries than trapidil itself. IC50 value of the derivative AR 12-456 was calculated to be 20 microM which is in the range of the inhibitory potency of 3-isobutyl-1-methylxanthine for the studied enzyme activities.
Bartel
S
S
Tenor
H
H
Krause
E G
EG
D015056:1-Methyl-3-isobutylxanthine / Q000494:pharmacology; D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D000697:Central Nervous System Stimulants / Q000494:pharmacology*; D003331:Coronary Vessels / Q000201:enzymology; D004285:Dogs; D066298:In Vitro Techniques; D007700:Kinetics; D009206:Myocardium / Q000201:enzymology; D011619:Psychotropic Drugs / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology*; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
D000697:Central Nervous System Stimulants; D011619:Psychotropic Drugs; D011743:Pyrimidines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D014192:Trapidil; D015056:1-Methyl-3-isobutylxanthine