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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-88
filingDate 2001-12-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2003-12-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_23f417e5c56a80319b61634e490cbd4e
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publicationDate 2003-12-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2218399-C2
titleOfInvention Inhibitor of no-dependent activation of soluble form of guanylate cyclase
abstract FIELD: organic chemistry, biochemistry, enzymes. SUBSTANCE: invention can be used in biochemistry for study of regulatory effects of nitrogen oxide and mechanism of action of peroxide-containing sesquiterpenoids of artemisinine order on activity of soluble form of guanylate cyclase (sGC). Invention relates to artemisinine and its derivatives of the general formula (I): wherein if is a simple bond then R is OH, (lower alkyl)-hydroxy-group or OC(O)CH 2 CH 2 C(O)ONa; or if is a double bond then R is oxygen atom. These compounds in the concentration 1-100 mcM show inhibitory effect of NO-dependent activation of sGC partially purified from human platelets caused by donor of nitrogen oxide - sodium nitroprusside. Concentration of artemisinine providing 50% of reduction of activating effect of sodium nitroprusside (IC 50 ) is 4.2 mcM being "basal" activity of enzyme (in the absence of sodium nitroprusside) is increased insignificantly (by 20-24%). Methylene blue as the nearest structural analogue in the concentration 10 mcM under the same conditions inhibits NO-dependent activation of sGC by 27% and reduces "basal" activity of enzyme by 10- 15%. Peroxide-containing sesquiterpenoids of artemisinine order of the general formula (I) are new effective inhibitors of NO-dependent activation of sGC. EFFECT: valuable biochemical properties of inhibitor, expanded assortment of modulating agents for this enzyme. 2 dwg, 1 tbl, 4 ex
priorityDate 2001-12-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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