Isoenzymes of cyclic nucleotide phosphodiesterase in the human aorta: characterization and the effects of E4021.
Eur J Pharmacol
; 284(1-2): 25-33, 1995 Sep 15.
Article
en En
| MEDLINE
| ID: mdl-8549633
ABSTRACT
In extracts of the human aorta, five isoenzymes of cyclic nucleotide phosphodiesterase, namely, phosphodiesterase I, phosphodiesterase II, phosphodiesterase III, phosphodiesterase IV and phosphodiesterase V, were identified exclusively in the cytosolic fraction, and no phosphodiesterase activity was detected in the particulate fraction. Phosphodiesterase V and phosphodiesterase I were the major cGMP-hydrolyzing enzymes in the human aorta. A novel vasorelaxant, sodium 1-[6-chloro-4-(3,4-methylenedioxybenzyl)aminoquinazolin-2-yl ]piperidine-4- carboxylate sesquihydrate (E4021), relaxed prostaglandin F2 alpha-precontracted strips of human pulmonary artery with an ED50 value of 0.5 microM. E4021 potently and highly selectively inhibited the activity of phosphodiesterase V from human aorta with a Ki value of 2.4 nM. These results suggest that there is a unique distribution of phosphodiesterase isoenzymes in the human aorta and that inhibitors of phosphodiesterase V might be useful as a new type of vasodilator in the treatment of clinical disorders.
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Banco de datos:
MEDLINE
Asunto principal:
Inhibidores de Fosfodiesterasa
/
Piperidinas
/
Quinazolinas
/
Vasodilatadores
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3',5'-GMP Cíclico Fosfodiesterasas
/
Isoenzimas
/
Músculo Liso Vascular
Límite:
Humans
Idioma:
En
Año:
1995
Tipo del documento:
Article