Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1983-2-25
pubmed:abstractText
The inhibitory effect of hydroflumethiazide (HFT) and its metabolite, 2,4-disulfamyl-5-trifluoromethylaniline (DTA) on cyclic AMP phosphodiesterase and the binding of HFT and DTA to carbonic anhydrase was studied in vitro. Significant inhibition of rat kidney low-Km cyclic AMP phosphodiesterase was observed with DTA concentration above 2.5 X 10(-4) mol/l and with HFT concentration above 1 X 10(-4) mol/l. 50% inhibition was observed at a DTA concentration of 1 X 10(-3) mol/l. Binding of DTA and HFT to commercially obtained bovine erythrocyte carbonic anhydrase was demonstrated by equilibrium dialysis. Data were consistent with one class of binding sites. The product of n (number of binding sites) and Kass (association constant) was 5 X 10(5) M for DTA and 3.3 X 10(4) M for HFT at 2 degrees. In human blood in vitro at 37 degrees, the equilibrium erythrocyte/plasma concentration ratio was 18 for DTA and 1.6 for HFT. It is concluded that HFT and DTA have approximately the same potency as cyclic AMP phosphodiesterase inhibitors, whereas DTA is more extensively bound by erythrocyte carbonic anhydrase.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0001-6683
pubmed:author
pubmed:issnType
Print
pubmed:volume
51
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
273-7
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1982
pubmed:articleTitle
Interaction of hydroflumethiazide and 2,4-disulfamyl-5-trifluoromethylaniline with cyclic AMP phosphodiesterase and carbonic anhydrase.
pubmed:publicationType
Journal Article, In Vitro