INFLUENCE OF THE ANTIDEPRESSANT PYRAZIDOLE AND ITS NITRO ANALOG ON CGMP-DEPENDENT PHOSPHODIESTERASE FROM THE SOLUBLE FRACTION OF HUMAN BRAIN CORTEX

Authors
MEDVEDEVA MV FEDOTOVA OA SHVEDOV VI BELOV AA MEDVEDEV AE BOBRUSKIN ID
Citation
Mv. Medvedeva et al., INFLUENCE OF THE ANTIDEPRESSANT PYRAZIDOLE AND ITS NITRO ANALOG ON CGMP-DEPENDENT PHOSPHODIESTERASE FROM THE SOLUBLE FRACTION OF HUMAN BRAIN CORTEX, Biochemistry, 58(5), 1993, pp. 523-531
Citations number
19
Categorie Soggetti
Biology
Journal title
Biochemistry → ACNP
ISSN journal
00062979
Volume
58
Issue
5
Year of publication
1993
Pages
523 - 531
Database
ISI
SICI code
0006-2979(1993)58:5<523:IOTAPA>2.0.ZU;2-6
Abstract
The influence of the antidepressant drug pyrazidole (pirlindole) and i ts nitro analog on cGMP-dependent phosphodiesterase from the soluble f raction of human brain cortex has been studied. Pyrazidole inhibits th e cGMP-induced activity of phosphodiesterase (IC50 = 1585 muM) without influencing the basal activity; its action is noncompetitive. with re spect to the substrate and the activator. Nitropyrazidole is a more po tent inhibitor of cGMP-dependent phosphodiesterase (IC50 = 115 muM), c ompeting with the substrate for the catalytic site (K(i) = 70 muM). Th ere is no direct interaction of pyrazidole or its nitro analog and the cGMP-specific allosteric site of the phosphodiesterase.