• International Journal of Oral Biology
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• v.35 no.4
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• pp.159-167
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• 2010

To provide a basis for studying the pharmacological actions of tetracaine HCl, we analyzed the membrane activities of this local anesthetic. The n-(9-anthroyloxy) stearic and palmitic acid (n-AS) probes (n = 2, 6, 9, 12 and 16) have been used previously to examine fluorescence polarization gradients. These probes can report the environment at a graded series of depths from the surface to the center of the membrane bilayer structure. In a dosedependent manner, tetracaine HCl decreased the anisotropies of 6-AS, 9-AS, 12-AS and 16-AP in the hydrocarbon interior of synaptosomal plasma membrane vesicles isolated from bovine cerebral cortex (SPMV), and liposomes derived from total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. However, this compound increased the anisotropy of 2-AS at the membrane interface. The magnitude of the membrane rotational mobility reflects the carbon atom numbers of the phospholipids comprising SPMV, SPMVTL and SPMVPL and was in the order of the 16, 12, 9, 6, and 2 positions of the aliphatic chains. The sensitivity of the effects of tetracaine HCl on the rotational mobility of the hydrocarbon interior or surface region was dependent on the carbon atom numbers in the descending order 16-AP, 12-AS, 9-AS, 6-AS and 2-AS and on whether neuronal or model membranes were involved in the descending order SPMV, SPMVPL and SPMVTL.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.43-52
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• 1988

To elucidate the mechanism of action of local anesthetics, the effects of local anethetics on the microenvironment of the lipid bilayers of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine brain and dimyristoylphosphatidylcholine (DMPC) multilamellar liposomes were investigated employing the intermolecular excimer fluorescence technique and differential scanning calorimetry (DSC). The relative intensities of excimer and monomer fluorescence of pyrene are a simple linear function of the viscosity of a homologous series of solvents. The microviscosity(${\eta}$)of the hydrocarbon region of SPMV was measured by this method and the value was $57.3{\pm}5.3\;cP$ at $37^{\circ}C$. In the presence of lidocaine-HCl and procaine-HCl, the values decreased to $46.5{\pm}5.1\;cP$ and $54.7{\pm}4.8\;cP$, respectvely. The differential scanning thermograms of DMPC multilamellar liposomes showed that local anesthetics significantly lowered the phase transition temperature, broadened the thermogram peaks, and reduced the size of the cooperative unit. These results indicate that local anesthetics have significant fluidizing effects on biomembranes and perturbation of membrane lipids may produce some, but not all, of their pharmacological actions.