منابع مشابه
Pharmacophore elucidation and molecular docking studies on phosphodiesterase-5 inhibitors
cGMP-binding cGMP-specific PDE, PDE5 plays a key role in the hydrolysis of cyclic guanidine monophosphate. Because cGMP mediates vascular functions, a PDE5 inhibitor that elevates cGMP level is an attractive means for vasodilatation and treatment of erectile dysfunction. In this paper we report the elucidation of the common pharmacophore hypothesis of different classes of PDE5 inhibitors. Using...
متن کاملStructure and function studies of the cGMP-stimulated phosphodiesterase.
Studies of cGMP binding to both the native cyclic GMP-stimulated phosphodiesterase and to two unique isolated chymotryptic fragments lacking the catalytic domain suggest that the enzyme contains two noncatalytic cGMP-binding sites/homodimer. In the presence of high concentrations of ammonium sulfate, 2 mol of cGMP are bound/mol of cGMP-stimulated phosphodiesterase homodimer. Under these conditi...
متن کاملStudies of phosphodiesterase effects on adipose tissue metabolism in obese subjects by the microdialysis technique.
The effect of non-selective (theophylline) inhibition of cyclic AMP breakdown on norepinephrine stimulated lipolysis rate was investigated in subcutaneous adipose tissue of obese subjects. In addition, changes in interstitial glucose and lactate concentration were assessed by means of the microdialysis technique. The interaction of endogenous released insulin and theophylline on adipocyte metab...
متن کاملStudies on polynucleotides. X. Enzymic degradation. Some properties and mode of action of spleen phosphodiesterase.
As a part of a program of studies aiming at the development of methods for the end group and sequential analysis of polynucleotides (l), we have been investigating the properties and mode of action of certain phosphodiesterases. Studies of this kind have been facilitated by the availability of a variety of substrates and, in particular, synthetic oligonucleotides of known size and structure (2)...
متن کاملStudies on mechanisms of low emetogenicity of YM976, a novel phosphodiesterase type 4 inhibitor.
YM976 is a novel and selective inhibitor of phosphodiesterase type 4 (PDE4) with a different chemical structure from rolipram. Orally administered YM976 showed anti-inflammatory activity (ED(50) = 2.8 mg/kg) similar to rolipram (3.5 mg/kg). On the other hand, the emetogenicity of YM976, one of the main adverse effects of PDE4 inhibitors, was lower (maximal non-emetic dose = 10 mg/kg) than that ...
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ژورنال
عنوان ژورنال: Proceedings of the Japanese Histochemical Association
سال: 1961
ISSN: 1883-9444
DOI: 10.1267/ahc1960.1961.115