Amphiphilic effects of local anesthetics on rotational mobility in neuronal and model membranes

Il Yun, Eun Soo Cho, Hye Ock Jang, Uk Kyu Kim, Chang Hwa Choi, In Kyo Chung, Inn Se Kim, W. Gibson Wood

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Abstract

To provide a basis for studying the molecular mechanism of pharmacological action of local anesthetics, we carried out a study of the membrane actions of tetracaine, bupivacaine, lidocaine, prilocaine and procaine. Fluorescence polarization of 12-(9-anthroyloxy)stearic acid (12-AS) and 2-(9-anthroyloxy)stearic acid (2-AS) were used to examine the effects of local anesthetics on differential rotational mobility between polar region and hydrocarbon interior of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex, and liposomes of total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. The two membrane components differed with respect to 2 and 12 anthroyloxy stearate (2-AS, 12-AS) probes, indicating that a difference in the membrane fluidity may be present. In a dose-dependent manner, tetracaine, bupivacaine, lidocaine, prilocaine and procaine decreased anisotropy of 12-AS in the hydrocarbon interior of the SPMV, SPMVTL and SPMVPL, but tetracaine, bupivacaine, lidocaine and prilocaine increased anisotropy of 2-AS in the membrane interface. These results indicate that local anesthetics have significant disordering effects on hydrocarbon interior of the SPMV, SPMVTL and SPMVPL, but have significant ordering effects on the membrane interface, and thus they could affect the transport of Na+ and K+ in nerve membranes, leading to anesthetic action.

Original languageEnglish (US)
Pages (from-to)123-132
Number of pages10
JournalBiochimica et Biophysica Acta - Biomembranes
Volume1564
Issue number1
DOIs
StatePublished - Aug 19 2002

Keywords

  • Biomembranes
  • Fluorescent probe technique
  • Hydrocarbon interior
  • Local anesthetic
  • Membrane interface
  • Rotational mobility

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    Yun, I., Cho, E. S., Jang, H. O., Kim, U. K., Choi, C. H., Chung, I. K., Kim, I. S., & Wood, W. G. (2002). Amphiphilic effects of local anesthetics on rotational mobility in neuronal and model membranes. Biochimica et Biophysica Acta - Biomembranes, 1564(1), 123-132. https://doi.org/10.1016/S0005-2736(02)00409-1