rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
12
|
pubmed:dateCreated |
1993-1-28
|
pubmed:abstractText |
8-(4-Chlorophenyl)thio-cyclic AMP (8-CPT-cAMP), extensively used as selective activator of cyclic AMP-dependent protein kinase, has been found to be a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA). Indeed, 8-CPT-cAMP (IC50 = 0.9 microM) inhibited PDE VA with a potency identical to that of zaprinast. 8-CPT-cAMP was also metabolized by PDE VA at a rate half that of cyclic GMP. The cyclic GMP-inhibited phosphodiesterase (PDE III) (IC50 = 24 microM) and the cyclic AMP-specific phosphodiesterase (PDE IV) (IC50 = 25 microM) were also inhibited by 8-CPT-cAMP. In contrast, most of the other cAMP-derivative studies showed little inhibition of any phosphodiesterase isoenzyme. These observations provide further reasons why the mechanism of the physiological effects of 8-CPT-cAMP should be interpreted with caution.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
0006-2952
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
15
|
pubmed:volume |
44
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2303-6
|
pubmed:dateRevised |
2007-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1335252-3',5'-Cyclic-GMP Phosphodiesterases,
pubmed-meshheading:1335252-Cyclic AMP,
pubmed-meshheading:1335252-Cyclic GMP,
pubmed-meshheading:1335252-Humans,
pubmed-meshheading:1335252-Infant, Newborn,
pubmed-meshheading:1335252-Isoenzymes,
pubmed-meshheading:1335252-Kinetics,
pubmed-meshheading:1335252-Mathematics,
pubmed-meshheading:1335252-Purinones,
pubmed-meshheading:1335252-Thionucleotides
|
pubmed:year |
1992
|
pubmed:articleTitle |
8-(4-Chlorophenyl)thio-cyclic AMP is a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA).
|
pubmed:affiliation |
SmithKline Beecham Pharmaceuticals, Welwyn, Herts, U.K.
|
pubmed:publicationType |
Journal Article
|