| pubmed-article:2021530 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0027651 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0031327 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0443315 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0596402 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0242184 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0348080 | lld:lifeskim |
| pubmed-article:2021530 | lifeskim:mentions | umls-concept:C0073647 | lld:lifeskim |
| pubmed-article:2021530 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:2021530 | pubmed:dateCreated | 1991-6-4 | lld:pubmed |
| pubmed-article:2021530 | pubmed:abstractText | The acute toxicity, pharmacokinetics and hypoxic cytotoxicity of RSU-1069 were investigated using the subcutaneous (sc) rat 9L tumour model. The pharmacokinetics were studied after i.p. injection of RSU-1069 (20 mg kg-1 or 100 mg kg-1). For both doses, the elimination of RSU-1069 followed first-order kinetics in both plasma and unclamped tumours. After 100 mg kg-1, the peak plasma concentration of RSU-1069 was 40 micrograms ml-1; the elimination t1/2 was 39.3 +/- 11.1 min. After 20 mg kg-1, the peak plasma concentration was 3 micrograms ml-1; the elimination t1/2 was 47.8 +/- 6.3 min. In unclamped tumours, the peak concentration was 50 micrograms g-1 with an elimination t1/2 of 36.1 +/- 9.6 min for the 100 mg kg-1 dose, and 4 micrograms g-1 with an elimination t1/2 of 41.9 +/- 6.1 min for the 20 mg kg-1 dose. The tumour and plasma elimination half-times were not significantly different (P greater than 0.2) for the two doses. Clamping the tumour 30 min after administration of 100 mg kg-1 of RSU-1069 decreased the tumour elimination t1/2 to 10.9 +/- 1.4 min. After releasing the clamp, RSU-1069 returned rapidly to the unclamped tumour concentration. The unclamped tumour/plasma ratio reached a maximum of 4-6, then decreased to a constant value of about 2 for both doses, indicating that RSU-1069 accumulates in these 9L tumours. RSU-1069 kills hypoxic sc 9L cells more efficiently than oxic sc 9L cells; at a surviving fraction of 0.5, the SER was 4.8. For in vitro 9L cells, the SER was approximately 50 when the comparison was between those treated in 2.1% 0(2) and those treated in less than 7.5 x 10(-3)% 0(2); it was approximately 100 when the comparison was between those treated in 21% 0(2) and those treated in less than 7.5 x 10(-3)% 0(3). Tumours treated with RSU-1069 and clamped for various times exhibited biphasic cell-kill kinetics; at 50 mg kg-1, little additional cell kill was achieved after 40 min of clamping. Our data also indicate that RSU-1069 is 300-1000 fold more efficient than misonidazole or SR2508 for killing hypoxic sc 9L tumour cells in situ. | lld:pubmed |
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| pubmed-article:2021530 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2021530 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2021530 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2021530 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2021530 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:2021530 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2021530 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:2021530 | pubmed:issn | 0007-0920 | lld:pubmed |
| pubmed-article:2021530 | pubmed:author | pubmed-author:HULLR WRW | lld:pubmed |
| pubmed-article:2021530 | pubmed:author | pubmed-author:WongK HKH | lld:pubmed |
| pubmed-article:2021530 | pubmed:author | pubmed-author:WheelerK TKT | lld:pubmed |
| pubmed-article:2021530 | pubmed:author | pubmed-author:WallenC ACA | lld:pubmed |
| pubmed-article:2021530 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2021530 | pubmed:volume | 63 | lld:pubmed |
| pubmed-article:2021530 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2021530 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2021530 | pubmed:pagination | 484-8 | lld:pubmed |
| pubmed-article:2021530 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
| pubmed-article:2021530 | pubmed:meshHeading | pubmed-meshheading:2021530-... | lld:pubmed |
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| pubmed-article:2021530 | pubmed:meshHeading | pubmed-meshheading:2021530-... | lld:pubmed |
| pubmed-article:2021530 | pubmed:year | 1991 | lld:pubmed |
| pubmed-article:2021530 | pubmed:articleTitle | Pharmacokinetics and cytotoxicity of RSU-1069 in subcutaneous 9L tumours under oxic and hypoxic conditions. | lld:pubmed |
| pubmed-article:2021530 | pubmed:affiliation | Department of Radiology, Bowman Gray School of Medicine, Winston-Salem, North Carolina 27103. | lld:pubmed |
| pubmed-article:2021530 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2021530 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2021530 | lld:pubmed |
