Effects of Local Anesthetics on Rotational Mobility of n-(9-Anthroyloxy)stearic Acid in Neuronal Membranes

  • Jang, Hye-Ock (Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University) ;
  • Lee, Chang (Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University) ;
  • Choi, Min-Gak (Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University) ;
  • Shin, Sang-Hun (Department of Oral and Maxillofacial Surgery and Clinical Pharmacology, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University) ;
  • Chung, In-Kyo (Department of Oral and Maxillofacial Surgery and Clinical Pharmacology, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University) ;
  • Yun, Il (Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University)
  • Published : 2003.06.21

Abstract

To elucidate the molecular mechanism of pharmacological action of local anesthetics, we studied membrane actions of tetracaine, bupivacaine, lidocaine, prilocaine and procaine. Fluorescence polarization of n-(9-anthroyloxy)stearic acid (n-AS) was used to examine the effects of these local anesthetics on differential rotational mobility of different positions of the number of synaptosomal plasma membrane vesicle (SPMV) phospholipid carbon atoms. The four membrane components differed with respect to 3, 6, 9 and 16-(9-anthroyloxy)stearic acid (3-AS, 6-AS, 9-AS and 16-AP) probes, indicating that differences in the membrane fluidity might be present. Degrees of the rotational mobility of 3-AS, 6-AS, 9-AS and 16-AP were different depending on depth of hydrocarbon interior. In a dose-dependentmanner, tetracaine, bupivacaine, lidocaine, prilocaine and procaine decreased anisotropy of 3-AS, 6-AS, 9-AS and 16-AP in the hydrocarbon interior of the SPMV. These results indicate that local anesthetics have significant disordering effects on hydrocarbon interior of the SPMV, thus affecting the transport of $Na^+$ and $K^+$ in nerve membranes and leading to anesthetic action.

Keywords

References

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