WR-1065, the active metabolite of amifostine, mitigates radiation-induced delayed genomic instability

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Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection

A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...

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The aminothiol WR-1065 protects T lymphocytes from ionizing radiation-induced deletions of the HPRT gene.

Aminothiols, such as WR-2721 and its active free thiol, WR-1065, reduce mutations from ionizing radiation in exponentially growing cells. In this study, human noncycling G0 T lymphocytes were exposed in vitro to gamma-irradiation in the presence or absence of WR-1065. The five treatment groups were: (a) control; (b) treatment with 4 mM WR-1065; (c) treatment with 3 Gy of gamma-radiation, from a...

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Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection

A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...

متن کامل

Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection

A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of amifostine (AMF) and/or its metabolite, WR-1065 in human plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite with o-phthaldialdehyde (OPA) and UVdetection at 340 nm. The derivatized AMF and WR-1065 were elut...

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Disposition of WR-1065 in the liver of tumor-bearing rats following regional vs systemic administration of amifostine.

PURPOSE Amifostine is a prodrug in which selectivity is largely determined by the preferential formation and uptake of its cytoprotective metabolite, WR-1065, in normal tissues as a result of differences in membrane-bound alkaline phosphatase activity. It was hypothesized that amifostine may be a good candidate for regional drug delivery to the liver because of its large hepatic extraction and ...

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ژورنال

عنوان ژورنال: Free Radical Biology and Medicine

سال: 2008

ISSN: 0891-5849

DOI: 10.1016/j.freeradbiomed.2008.09.004