Korean J Physiol Pharmacol.  2003 Jun;7(3):119-124.

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

• Jang HO
• Lee C
• Choi MG
• Shin SH
• Chung IK
• Yun I

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-dependent manner, 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.

Keyword

Fluorescent probe technique; Rotational mobility; Hydrocarbon interior; Local anesthetics; Neuronal membranes; AS probes

MeSH Terms

Anesthetics, Local*
Anisotropy
Bupivacaine
Carbon
Cell Membrane
Fluorescence Polarization
Lidocaine
Membrane Fluidity
Membranes*
Neurons*
Prilocaine
Procaine
Tetracaine
Anesthetics, Local
Bupivacaine
Carbon
Lidocaine
Prilocaine
Procaine
Tetracaine