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On-Line Liquid Chromatography-Accurate Radioisotope Counting Coupled with a Radioactivity Detector and Mass Spectrometer for Metabolite Identification in Drug Discovery and Development

Autor: A E F Nassar, S M Bjorge, D Y Lee

Publikováno v: Analytical Chemistry. 75:785-790

A novel detection method combining on-line liquid chromatography-accurate radioisotope counting (LC-ARC, advanced stop flow controller) coupled with a radioactivity detector and mass spectrometer has been developed. One of the major benefits of this

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d28dcae53cc8200cfb34bed0078f9f8
https://doi.org/10.1021/ac025934f

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Metabolic disposition of the cognition activator tacrine in rats, dogs, and humans. Species comparisons

Autor: W F, Pool, M D, Reily, S M, Bjorge, T F, Woolf

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 25(5)

The metabolic fate of tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA)] was examined in rats, dogs, and humans. After administration of single oral doses of [14C]THA to rats, dogs, and humans, drug-derived material was w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::c9120cc01e4d802297c12f0bff4596a9
https://pubmed.ncbi.nlm.nih.gov/9152598

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In vitro and in vivo disposition of 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide (CI-976). Identification of a novel five-carbon cleavage metabolite in rats

Autor: M W, Sinz, A E, Black, S M, Bjorge, A, Holmes, B K, Trivedi, T F, Woolf

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 25(1)

The metabolism of CI-976, a potent inhibitor of liver and intestinal acyl coenzyme A:cholesterol acyltransferase, was investigated in isolated rat hepatocytes and Wistar rats after oral administration. The major metabolite observed both in vitro and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b42b737b6873a58e957db150bd353808
https://pubmed.ncbi.nlm.nih.gov/9010639

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Bioactivation and irreversible binding of the cognition activator tacrine using human and rat liver microsomal preparations. Species difference

Autor: T F, Woolf, W F, Pool, S M, Bjorge, T, Chang, O P, Goel, C F, Purchase, M C, Schroeder, K L, Kunze, W F, Trager

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 21(5)

Tacrine's [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate, (THA)] metabolic fate was examined using human and rat liver microsomal preparations. Following 1-hr incubations with human microsomes, [14C]THA (0.4 microM) was extensively

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::72ff76f74c6cd8072ef38710bc62592e
https://pubmed.ncbi.nlm.nih.gov/7902251

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Studies on the beta-oxidation of valproic acid in rat liver mitochondrial preparations

Autor: S M, Bjorge, T A, Baillie

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 19(4)

Incubation of valproic acid (VPA) with freshly isolated rat liver mitochondria led to the identification of the beta-keto acid, 3-oxo-VPA, together with three unsaturated metabolites, viz. delta 2(E)-VPA, delta 3-VPA, and delta 2(E),3'(E)-VPA. The co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::68f9abe9e77057fb28ab511fd9a0b755
https://pubmed.ncbi.nlm.nih.gov/1680661

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Metabolism of the acyl-CoA:cholesterol acyltransferase inhibitor 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide in rat and monkey. Omega-/beta-oxidation pathway

Autor: T F, Woolf, S M, Bjorge, A E, Black, A, Holmes, T, Chang

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 19(3)

2,2-Dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide (CI-976) is a newly developed hypocholesterolemic agent. In pharmacokinetic studies, CI-976 was found to have a much shorter elimination half-life in monkey (0.6 hr) compared to rat (8 hr). Radioact

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::55cf24744488714dd590c05c60906af4
https://pubmed.ncbi.nlm.nih.gov/1680639

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Organopalladium approaches to prostaglandins. 1. Synthesis of thiophene-containing prostaglandin endoperoxide analogs via thienylpalladation of bicycle olefins

Autor: D. R. Leach, S. M. Bjorge, Richard C. Larock

Publikováno v: Tetrahedron Letters. 23:715-718

Thiophene-containing prostaglandin endoperoxide analogs are readily available by addition of thienylpalladium species to bicyclic olefins and subsequent treatment with alkenyl or alkynyl organometallics. Hydrogenation affords bicyclic and tricyclic p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5b408f0d9c110889fc0e5b9a8e09a794
https://doi.org/10.1016/s0040-4039(00)86929-4

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Comparison of glycolysis and glutaminolysis in Onchocerca volvulus and Brugia pahangi by 13C nuclear magnetic resonance spectroscopy

Autor: N. E. MacKenzie, J. F. Williams, S. M. Bjorge, E. A. Van De Waa, P. R. Gooley, T. A. Baille, James L. Bennett, Timothy G. Geary

Publikováno v: Parasitology.

SummaryComparison of glycolysis in Brugia pahangi and Onchocerca volvulus by C nuclear magnetic resonance (NMR) spectroscopy showed that the former organism is predominantly a lactate fermenter and the latter resembles more closely the metabolism of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47789e49a033f582f8740febe4f30201
https://pubmed.ncbi.nlm.nih.gov/2608314

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