| pubmed-article:10534322 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10534322 | lifeskim:mentions | umls-concept:C0025519 | lld:lifeskim |
| pubmed-article:10534322 | lifeskim:mentions | umls-concept:C0247025 | lld:lifeskim |
| pubmed-article:10534322 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:10534322 | lifeskim:mentions | umls-concept:C0681829 | lld:lifeskim |
| pubmed-article:10534322 | pubmed:issue | 11 | lld:pubmed |
| pubmed-article:10534322 | pubmed:dateCreated | 1999-11-24 | lld:pubmed |
| pubmed-article:10534322 | pubmed:abstractText | Tirofiban hydrochloride [L-tyrosine-N-(butylsulfonyl)-O-[4-(4-piperidinebutyl)] monohydrochloride, is a potent and specific fibrinogen receptor antagonist. Radiolabeled tirofiban was synthesized with either (3)H-label incorporated into the phenyl ring of the tyrosinyl residue or (14)C-label in the butane sulfonyl moiety. Neither human liver microsomes nor liver slices metabolized [(14)C]tirofiban. However, male rat liver microsomes converted a limited amount of the substrate to a more polar metabolite (I) and a relatively less polar metabolite (II). The formation of I was sex dependent and resulted from an O-dealkylation reaction catalyzed by CYP3A2. Metabolite II was identified as a 2-piperidone analog of tirofiban. There was no evidence for Phase II biotransformation of tirofiban by microsomes fortified with uridine-5'-diphospho-alpha-D-glucuronic acid. After a 1 mg/kg i.v. dose of [(14)C]tirofiban, recoveries of radioactivity in rat urine and bile were 23 and 73%, respectively. Metabolite I and unchanged tirofiban represented 70 and 30% of the urinary radioactivity, respectively. Tirofiban represented >90% of the biliary radioactivity. At least three minor biliary metabolites represented the remainder of the radioactivity. One of them was identified as I. Another was identified as II. When dogs received 1 mg/kg i.v. of [(3)H]tirofiban, most of the radioactivity was recovered in the feces as unchanged tirofiban. The plasma half-life of tirofiban was short in both rats and dogs, and tirofiban was not concentrated in tissues other than those of the vasculature and excretory organs. | lld:pubmed |
| pubmed-article:10534322 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10534322 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10534322 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:10534322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10534322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10534322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10534322 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10534322 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:10534322 | pubmed:issn | 0090-9556 | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:VickersSS | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:DuncanC ACA | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:TheoharidesA... | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:VyasK PKP | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:EllisJ DJD | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:RamageP IPI | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:BalaniS KSK | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:CuiDD | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:Prueksaritano... | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:ArisonBB | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:SlaughterD... | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:GorhamL MLM | lld:pubmed |
| pubmed-article:10534322 | pubmed:author | pubmed-author:PolskyS LSL | lld:pubmed |
| pubmed-article:10534322 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10534322 | pubmed:volume | 27 | lld:pubmed |
| pubmed-article:10534322 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10534322 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10534322 | pubmed:pagination | 1360-6 | lld:pubmed |
| pubmed-article:10534322 | pubmed:dateRevised | 2004-11-17 | lld:pubmed |
| pubmed-article:10534322 | pubmed:meshHeading | pubmed-meshheading:10534322... | lld:pubmed |
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| pubmed-article:10534322 | pubmed:meshHeading | pubmed-meshheading:10534322... | lld:pubmed |
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| pubmed-article:10534322 | pubmed:meshHeading | pubmed-meshheading:10534322... | lld:pubmed |
| pubmed-article:10534322 | pubmed:meshHeading | pubmed-meshheading:10534322... | lld:pubmed |
| pubmed-article:10534322 | pubmed:meshHeading | pubmed-meshheading:10534322... | lld:pubmed |
| pubmed-article:10534322 | pubmed:year | 1999 | lld:pubmed |
| pubmed-article:10534322 | pubmed:articleTitle | In vitro and in vivo studies on the metabolism of tirofiban. | lld:pubmed |
| pubmed-article:10534322 | pubmed:affiliation | Merck Research Laboratories, West Point, Pennsylvania 19486-0004, USA. stanley_vickers@merck.com | lld:pubmed |
| pubmed-article:10534322 | pubmed:publicationType | Journal Article | lld:pubmed |
