Mefloquine blockade of pannexin1 currents: Resolution of a conflict

Rodolfo Iglesias, David C. Spray, Eliana Scemes

Research output: Contribution to journalArticle

42 Scopus citations

Abstract

The authors' laboratory has reported potent block of Pannexin1 (Panx1) currents by the antimalarial quinine derivative mefloquine. However, other laboratories have found little or no mefloquine sensitivity of Panx1 currents or processes attributable to these channels. In order to resolve this issue, the authors have performed extensive dose-response studies on Panx1-transfected neuroblastoma (Neuro2A) and rat insulinoma (Rin) cells, comparing mefloquine obtained from three suppliers and also comparing the sensitivity to diastereomers. Results indicate a 20-fold difference in sensitivity to the (-)-threo-(11R/2R) diastereomer compared to the erythro enatiomers and much lower potency of (±)-erythro-(Rz.ast;/Sz.ast;)-mefloquine obtained from one of the commercial sources. This markedly lower efficacy presumably accounts for the disparity in results from different laboratories who have applied it in Panx1 studies.

Original languageEnglish (US)
Pages (from-to)131-137
Number of pages7
JournalCell Communication and Adhesion
Volume16
Issue number5-6
DOIs
StatePublished - Apr 26 2010

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Keywords

  • Hemichannel
  • Isomers
  • Lariam
  • Mefloquine
  • Pannexin
  • Voltage clamp

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Cell Biology

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