[The effect of the antidepressant pyrazidol and its nitro analog on cGMP-dependent phosphodiesterase from the soluble fractions of the human cerebral cortex].
The effects of the antidepressant pyrazidol (pirlindole) and its nitro analog on cGMP-dependent phosphodiesterase from the soluble fraction of human brain cortex have been studied. Pirlindole inhibits the cGMP-induced activity of phosphodiesterase (IC50 = 1585 microM) without influencing the basal activity; its action is noncompetitive in respect of the substrate and the activator. Nitropirlindole is a more potent inhibitor of cGMP-dependent phosphodiesterase (IC50 = 115 microM) competing with the substrate for the catalytic site (K(i) = 70 microM). There is no direct interaction of pirlindole (pyrazidol) and its nitro analog with the cGMP-specific site in phosphodiesterase.
M V
MV
Medvedeva
O A
OA
Fedotova
V I
VI
Shvedov
A A
AA
Belov
A E
AE
Medvedev
I D
ID
Bobruskin
D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000928:Antidepressive Agents / Q000737:chemistry / Q000494:pharmacology*; D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology*; D002384:Catalysis; D002540:Cerebral Cortex / Q000187:drug effects / Q000201:enzymology*; D006152:Cyclic GMP / Q000378:metabolism; D006801:Humans; D009574:Nitro Compounds / Q000737:chemistry*; D013379:Substrate Specificity
D000928:Antidepressive Agents; D002227:Carbazoles; D009574:Nitro Compounds; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D006152:Cyclic GMP; C009830:pirlindole