Source:http://linkedlifedata.com/resource/pubmed/id/10705507
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2000-4-18
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pubmed:abstractText |
A novel synthesis of a radioactive compound of 1 alpha-hydroxyvitamin D3 (1 alpha OHD3) (1) and its pharmacokinetics are described. Radioactive 1 alpha OHD3 tritiated at 22 and 23 positions ([22,23-(3)H4]1 alpha OHD3) (5) was prepared via key reactions of the reduction of acetylenic side chain in the ketone (12) with tritium gas in the presence of palladium-charcoal and the subsequent Wittig reaction with the A-ring synthon (16). [22,23-(3)H4]1 alpha OHD3 (5) showed high specific radioactivity (111.5 Ci/mmol) and was used successfully in pharmacokinetics studies with rats. In the pharmacokinetics studies, the plasma concentration level of the active form of vitamin D3, 1 alpha,25-dihydroxy-vitamin D3 [1 alpha,25(OH)2D3], after oral or intravenous administration of [22,23-(3)H4]1 alpha OHD3 (5), showed longer half-life, lower maximum concentration, and lower area under the curve than those after treatment of 1 alpha,25(OH)2D3 tritiated at 26 and 27 positions (4). These results might suggest a beneficial therapeutic utility of 1 alpha OHD3 (1) over the treatment of 1 alpha,25(OH)2D3 (2).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0009-2363
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
215-9
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:10705507-Administration, Oral,
pubmed-meshheading:10705507-Animals,
pubmed-meshheading:10705507-Area Under Curve,
pubmed-meshheading:10705507-Autoradiography,
pubmed-meshheading:10705507-Calcitriol,
pubmed-meshheading:10705507-Half-Life,
pubmed-meshheading:10705507-Hydroxycholecalciferols,
pubmed-meshheading:10705507-Injections, Intravenous,
pubmed-meshheading:10705507-Isotope Labeling,
pubmed-meshheading:10705507-Male,
pubmed-meshheading:10705507-Rats,
pubmed-meshheading:10705507-Rats, Sprague-Dawley,
pubmed-meshheading:10705507-Tritium
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pubmed:year |
2000
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pubmed:articleTitle |
Synthesis and pharmacokinetics of 1 alpha-hydroxyvitamin D3 tritiated at 22 and 23 positions showing high specific radioactivity.
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pubmed:affiliation |
Chugai Pharmaceutical Co., Ltd., Tokyo, Japan.
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pubmed:publicationType |
Journal Article
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