• International Journal of Oral Biology
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• 제35권4호
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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.

• 대한약리학회지
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• 제24권1호
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• pp.43-52
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• 1988

국소마취제의 약리학적 작용기전을 탐구키 위하여 소의 신선한 대뇌피질로부터 synaptosomal plasma membrane vesicles(SPMV)를 분리한 후 그 소수성 중심부의 microviscosity에 미치는 국소마취제의 영향을 pyrene 형광 probe법으로 측정한 결과 lidocaine HCI과 procaine HCI이 microviscosity를 낮춘다는 것을 알았고 그 정도는 procaine HCI에 비하여 tidocaine.HCI이 더욱 컸다. 또 국소마취 제 가 dimyristoylphosphatidylcholine (DMPC) multilamellar liposomes의 상전 이온도를 낮추며 cooperative unit크기를 감소시킨다는 것도 시차 열량분석법으로 알게 되었다. 상전이온도와 cooperative unit 크기의 감소 정도는 dibucaine HCI>tetracaine HCI>lidocaine HCI > procaine HCI의 순이었다.