Use of stable-isotope-labelled compounds in pharmaceutical research

Vandenheuvel, W.J.A.

doi:10.1007/978-1-349-03328-7_6

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B Isotope Effects1

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1982

1986

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Cited by 5 publications

(1 citation statement)

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“…16), where the introduction of deuterium at the 2-position diminished the metabolism of the amino acid. And since labeled and unlabeled forms have equivalent antibacterial activity, the isotope effect resulted in a product with an enhanced pharmacological effect on the basis of an equivalent dose (67).…”

Section: B Isotope Effectsmentioning

confidence: 99%

Determination of drug bioavailability by mass spectrometry

Vink¹

1982

Mass Spectrometry Reviews

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Section: B Isotope Effectsmentioning

confidence: 99%

Determination of drug bioavailability by mass spectrometry

Vink¹

1982

Mass Spectrometry Reviews

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The application of stable isotopes in biomedical research

Haskins¹

1982

Biol. Mass Spectrom.

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Many of the ways in which isotopes are used in biomedical research are reviewed. The use of stable isotopes in stable isotope dilution assays, for metabolite identification and in pharmacokinetic studies, is discussed and relevant examples are given to illustrate the various points made. Isotope effects and their implications for future drug design are considered. Some of the toxicity problems associated with the use of stable isotopes are also considered. Finally, a brief subjective view of possible future advances is made.

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Drug Metabolite Identification: Stable Isotope Methods

Vandenheuvel

1986

The Journal of Clinical Pharma

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This paper focuses on stable isotope labeling of drugs, in combination with mass spectrometry (MS)-based methods, to facilitate the recognition and identification of metabolites and the employment of stable isotope-labeled derivatization reagents (e.g., bis-trimethylsilylacetamide-d18) in the structure elucidation of metabolites from unlabeled drugs via gas-liquid chromatography-MS techniques. In both cases, it is the so-called isotope peak shift that permits generation of data useful for metabolite identification. Furthermore, judicious labeling of a drug permits characterization of drug-related species (metabolites) by MS-based recognition of isotope cluster signatures. Studies using stable isotope-labeled drugs are exemplified by work on aminopyrine and isopropylantipyrine metabolism; examples of the derivatization peak shift approach include those from studies of timolol and cyproheptadine.

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Use of stable-isotope-labelled compounds in pharmaceutical research

Cited by 5 publications

References 41 publications

Determination of drug bioavailability by mass spectrometry

Determination of drug bioavailability by mass spectrometry

The application of stable isotopes in biomedical research

Drug Metabolite Identification: Stable Isotope Methods

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