6 results match your criteria placing radiolabel

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Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450.

Drug Metab Dispos 2017 05 10;45(5):430-440. Epub 2017 Feb 10.

Departments of Drug Metabolism and Pharmacokinetics (R.H.T., J.S.H., Y.C., C.E.C.A.H., S.C.K., S.M.), and Discovery Chemistry (M.S.), Genentech, Inc., 1 DNA Way, South San Francisco, California.

GDC-0425 [5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile] is an orally bioavailable small-molecule inhibitor of checkpoint kinase 1 that was investigated as a novel cotherapy to potentiate chemotherapeutic drugs, such as gemcitabine. In a radiolabeled absorption, distribution, metabolism, and excretion study in Sprague-Dawley rats, trace-level but long-lived C-labeled thiocyanate was observed in circulation. This thiocyanate originated from metabolic decyanation of GDC-0425 and rapid conversion of cyanide to thiocyanate. Read More

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Transport of sucrose, not hexose, in the phloem.

J Exp Bot 2012 Jun 2;63(11):4315-20. Epub 2012 May 2.

Department of Plant Biology, Cornell University, Ithaca, New York 14853, USA.

Several lines of evidence indicate that glucose and fructose are essentially absent in mobile phloem sap. However, this paradigm has been called into question, especially but not entirely, with respect to species in the Ranunculaceae and Papaveraceae. In the experiments in question, phloem sap was obtained by detaching leaves and placing the cut ends of the petioles in an EDTA solution. Read More

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Radioiodination of humic substances via azocoupling with 3-[125I] iodoaniline.

Environ Sci Technol 2008 Jun;42(11):4083-7

Institute of Interdisciplinary Isotope Research, Permoserstrasse 15, 04318 Leipzig, Germany.

A new method is described for radiolabeling humic substances (HS) with iodine radioisotopes. The method radiolabels the electron-rich aromatic moieties of HS with the 3-[125I]iodobenzenediazonium ion via azocoupling. The method uses four steps: (i) 3-aminobenzenetrimethylstannane is synthesized and isolated by using a silica gel column, (ii) 3-[125I]iodoaniline is synthesized and isolated by HPLC, with radiochemical yields of up to 60%, (iii) 3-[125I]iodobenzenediazonium chloride is synthesized, and the reaction mixture from this step is used in step iv to radioiodinate HS with radiochemical yields of up to 95% (with reference to 3-[125I]iodoaniline). Read More

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Pretargeting of bacterial endocarditis in rats with streptavidin and 111In-labeled biotin.

J Nucl Med 1999 Mar;40(3):484-90

Department of Nuclear Medicine, University of Massachusetts Medical Center, Worcester 01655, USA.

Unlabelled: A radioimaging approach for the detection of endocarditis has been investigated using two-step pretargeting with streptavidin and radiolabeled biotin.

Methods: Hemodynamic alterations within the rat heart were induced by placing an in-dwelling catheter into the left ventricle through the aortic valves. The animals were subsequently infected with Staphylococcus aureus through a tail vein. Read More

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