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In vitro pharmacological selectivity profile of oseltamivir prodrug (tamiflu (r)) and active metabolite

Academic Article
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Overview

authors

  • Lindemann, L.
  • Jacobsen, H.
  • Schuhbauer, D.
  • Knoflach, F.
  • Gatti, S.
  • Wettstein, J. G.
  • Loetscher, H.
  • Chu, T.
  • Ebeling, M.
  • Paulson, James
  • Prinssen, E.
  • Brockhaus, M.

publication date

  • February 2010

journal

  • European Journal of Pharmacology  Journal

abstract

  • Neuropsychiatric adverse events have been reported in influenza patients with and without exposure to oseltamivir (Tamiflu), triggering speculation as to whether oseltamivir may be interacting with any human receptors and contributing to such neuropsychiatric events. In this study, the in vitro selectivity profile of oseltamivir prodrug and active metabolite was investigated. Both compounds lacked clinically relevant pharmacological activities on human, rodent and primate neuraminidases and on a panel of 155 other molecular targets, including those relevant for mood, cognition and behavior. Neuropsychiatric adverse events observed in influenza patients are likely a phenomenon caused by the infection rather than by oseltamivir.

subject areas

  • Animals
  • Antiviral Agents
  • Enzyme Inhibitors
  • Humans
  • Influenza A Virus, H3N2 Subtype
  • Neuraminidase
  • Oseltamivir
  • Phosphates
  • Primates
  • Prodrugs
  • Rats
  • Substrate Specificity
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Research

keywords

  • Influenza
  • Neuraminidase
  • Neuropsychiatric adverse event
  • Oseltamivir
  • Selectivity
  • Tamiflu
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Identity

International Standard Serial Number (ISSN)

  • 0014-2999

Digital Object Identifier (DOI)

  • 10.1016/j.ejphar.2009.11.020

PubMed ID

  • 19917275
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Additional Document Info

start page

  • 6

end page

  • 10

volume

  • 628

issue

  • 1-3

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