The isoenzyme selectivity of AH 21-132 as an inhibitor of cyclic nucleotide phosphodiesterase activity.
The smooth muscle relaxant, AH 21-132, was tested for its inhibitory effect on the cyclic nucleotide phosphodiesterase (PDE) activities fractionated from guinea-pig cardiac ventricle and bovine trachealis muscle. Both tissues yielded significant PDE-I and PDE-II activities. The cardiac ventricle also contained a significant amount of PDE-III whilst the trachealis contained PDE-IV. AH 21-132 inhibited PDE-III and PDE-IV selectively (Ki values 0.30-0.55 microM) compared with PDE-I and PDE-II (Ki values 20-140 microM).
Elliott
K R
KR
Department of Biochemistry and Molecular Biology, Medical School, University of Manchester, U.K.
Berry
J L
JL
Bate
A J
AJ
Foster
R W
RW
Small
R C
RC
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D000818:Animals; D002417:Cattle; D002852:Chromatography, Ion Exchange; D006168:Guinea Pigs; D006352:Heart Ventricles; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D007700:Kinetics; D009130:Muscle, Smooth / Q000201:enzymology; D009206:Myocardium / Q000201:enzymology; D009287:Naphthyridines / Q000737:chemistry / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D014132:Trachea / Q000201:enzymology
D007527:Isoenzymes; D009287:Naphthyridines; D010726:Phosphodiesterase Inhibitors; C044843:AH 21-132; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D015106:3',5'-Cyclic-GMP Phosphodiesterases