• Archives of Pharmacal Research
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• v.15 no.2
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• pp.152-161
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• 1992

Selective quenching of 1, 6-diphenyl-1, 3, 5-hexatriene (DPH) by trinitrophenyl groups was utilized to examine the transbilayer fluidity asymmetry of model membranes of phospholipids (SPMVPL) extracted from synaptosomal plasma membrane vesicles (SPMV). The polarization (P), anisotropy (r), limiting anisotropy $(r_\infty$), and order parameter (S) of DPH in the inner monolayer were 0.019, 0.014, 0.018, and 0.047, respectively, greater than calculated for the outer monolayer of SPMVPL. Selective quenching of DPH by trinitrophenyl groups was also utilized to examine the effects of n-alkanols on the individual monolayer structure of SPMVPL. n-Alkanols fluidized the hydrocarbon region of bulk SPMVPL and the potencies of n-alkanols up to 1-nonanon increased with carbon chain length. It appears that the potencies in bilayer fluidization increase by 1 order of magnitude as the carbon chain length increases by two carbon atoms. The cut-off phenomenon was reached at 1-decanol, where further increase in hydrocarbon length resulted in a decrease in pharmacological activity. The n-alkanols had greater fluidizing effects on the outer monolayer as compared to the inner monolayer of SPMVPL, even though these selective effects tended to become weaker as the carbon chain length increased. Thus, it has been proven that n-alkanols exhibit selective rather than nonselective fludizing effects within transbilayer domains of SPMVPL.

• Archives of Pharmacal Research
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• v.16 no.2
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• pp.118-122
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• 1993

The effects of n-alkanols on the rotational relaxation time of 1, 6-dipheny-1, 3, 5-hexatriene (DPH) in synaptosomal plasma membrane vesicles isolate from fresh bovine cerbral contex were investigated. n-Alknols decreased the rotational relaxation time of 1, 6-diphenyl-1, 3, 5-hexatriene in the native membranes and the potencies of n-alkanols up to 1-nonanol increased by 1 order of magnitude as the carbon chain length increases by two carbon atoms, The cut-off phenomenon was reached at 1-decanol, where further increase in hydocabon length resulted in an increase in the rotational relaxation time of DPH in the native membranes.

• The Korean Journal of Pharmacology
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• v.28 no.2
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• pp.191-199
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• 1992

Selective quenching of 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups was utilized to examine the transbilayer fluidity asymmetry of model membranes of total lipids (SPMVTL) extracted from synaptosomal plasma membrane vesicles (SPMV). The polarization (P), anisotropy (r), limiting anisotropy $(r_{\infty})$, and order parameter (S) of DPH in the inner monolayer were 0.031, 0.025, 0.033, and 0.070, respectively, greater than calculated for the outer monolayer of SPMVTL. Selective quenching of DPH by trinitrophenyl groups was also utilized to examine the effects of n-alkanols on the individual monolayer structure of SPMVTL. n-Alkanols fluidized the hydrocarbon region of bulk SPMVTL, and the potencies of n-alkanols up to 1-nonanol increased with carbon chain length. It appears that the potencies in bilayer fluidization increase by 1 order of magnitude as the carbon chain length increases by two carbon atoms. The cut-off phenomenon was reached at 1-decanol, where further increase in hydrocarbon length resulted in a decrease in pharmacological activity. The n-alkanols had greater fluidizing effects on the outer monolayer as compared to the inner monolayer of SPMVTL, even though these selective effects tended to become weaker as carbon chain length increased. Thus, it has been proven that n-alkanols exhibit selective rather than nonselective fluidizing effects within transbilayer domains of SPMVTL.

• The Korean Journal of Pharmacology
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• v.29 no.1
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• pp.157-163
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• 1993

Intramolecular excimer formation with the fluorescent probe 1,3-di(1-pyrenyl)propane (Py-3-Py) was used to investigate the effects of methanol, ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, 1-heptanol, 1-octanol, 1-nonanol and 1-decanol on the lateral diffusion of synaptosomal plasma membrane vesicles isolated from bovine cerebral cortex (SPMV). The n-alkanols increased the excimer to monomer fluorescence intensity ratio (I'/I) of Py-3-Py in the SPMV. In a dose-dependent manner, n-alkanols increased lateral diffusion of hydrocarbon region of bulk (inner+outer monolayers) SPMV lipid bilayers, and the potencies of n-alkanols up to l-nonanol increased with carbon chain length. It appears that the potencies in bilayer fluidization due to the lateral diffusion increase by 1 order of magnitude as the carbon chain length increases by two carbon atoms. The cut-off phenomenon was reached at 1-decanol, where further increase in hydrocarbon length resulted in a decrease in pharmacological activity.

• Archives of Pharmacal Research
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• v.16 no.3
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• pp.191-195
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• 1993

We investigated the effects of n-alkanols on the range and rate of the lateral diffusion of 1, 3-di(1-pyrenyl)propane in the model membranes of total phospholipid fraction extracted from synaptosomal plasma membrane vesicles. n-Akanols increased the range and rate of the lateral diffusion of 1, 3-di(1-pyrenyl)propane in the bulk model membrane structures (inner + outer monolayers) and the potencies of n-alknols up to 1-nonanol increased by 1 order of magnitude as the carbon chain length increases by two carbon atoms. The cut-off phenomenon was reached at 1-decanol, where further icnrease in hydrocarbon length resulted in a decrease in the lateral diffusion. However, significant changes in the 1'/1 value were not observed by methanol (from 100 to 2500 mM), ethanol (from 25 to 800 mM), and 1-propanol (from 10 to 250 mM) over entire concentration.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.192-197
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• 1990

The microviscosites of the lipid bilayers of liposomal membranes of phospholipids were measured by the intermolecular excimer, formation method employing pyrene as a fluorescence probe, and the effects of n-alkanols and other local anesthetics on the microviscosity were investigated. The results showed that the n-alkanols and the ohter local anesthetics effectively lowered the microviscosity of the lipid bilayer of the dipalmitoyl phosphatidycholine liposomal membrane in proportion to the concentration of the additives. Moreover, there was a fairly good correlation between the ocal anesthetic activities and the microviscosity-lowering activities of these drugs. This results suggests that the nerve blocking activity of local anesthetics might have some relation with their activity fluidizing the lipid bilayer of biomembrane.

• The Korean Journal of Pain
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• v.6 no.1
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• pp.74-82
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• 1993

신선한 소의 대뇌피질로부터 synaptosomal plasma membrane vesicles(SPMV)를 분리하고 이 SPMV로부터 추출한 총지질(cholesterol과 각종 인지질 함유)로서 제제한 인공세포막(SPMVTL)에서의 n-alkanols 침투 정도를 형광 probe를 이용한 형광 소광법을 통하여 검색하였다. n-alkanols는 SPMVTL 외부 단층(outer monolayer)의 표면에 주로 분포하되 그 탄소수에 비례하여 소수성 부위에 분포되는 양이 증가되는 경향을 나타내었다(1-decanol은 예외). Methanol, ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, 1-hepatnol, 1-cotanol, 1-nonanol 및 1-decanol은 SPMVTL 외부 단층 표면(친수성 부위)에 분포되는 것이 소수성 부위에 분포되는 것에 비하여 각각 650, 288, 151.6, 69.5, 36.8, 11.9, 4.8, 1.6, 0.74, 2.1배가 된다는 것을 확인하였다. 1-decanol은 $C_{10}$인데도 불구하고 $C_8$인 1-octanol에 비하여 적은 양이 소수성 부위에 침투 분포되는 것이 확인되었다. 또한 n-alkanols는 저자등이 이미 보고한 SPMV에서의 경우보다도 본 연구에서의 SPMVTL의 경우가 현저하게 많은 양이 소수성 부위로 침투 분포된다는 것이 확인되었다.

• The Korean Journal of Pain
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• v.6 no.1
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• pp.67-73
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• 1993

소의 신선한 대뇌피질로부터 synaptosomal plasma membrane vesicles(SPMV)를 분리한 후 이 SPMV로부터 추출한 모든 인지질들로서 제제한 인공세포막(SPMVPL)에서의 n-alkanols 침투 정도를 형광 probe를 이용한 형광 소광법을 통하여 검색하였다. n-alkanols는 SPMVPL 외부 단층(outer monolayer)의 표면에 주로 분포하되 그 탄소수에 비례하여 소수성 부위에 분포되는 양이 증가되는 경향을 나타내었다. methanol, ethanol, 1-propano, 1-butanol, 1-pentanol, 1-hexanol, 1-heptanol, 1-octanol, 1-nonanol 및 1-decanol은 SPMVPL 외부 단층의 표면(친수성 부위)에 분포되는 것이 소수성 부위에 분포되는 것에 비하여 각각 432.4, 208.9. 125.6, 88.2, 19.3, 7.9, 2.6, 1.0, 0.42, 1.36배가 되었다. 1-decanol은 $C_{10}$인데도 불구하고 $C_8$인 1-octanol에 비하여 적은 양이 소수성 부위에 침투 분포된다는 것이 확인되었다. n-alkanols의 침투에 대하여 저자등이 이미 보고한 바 있는 SPMV 및 SPMVTL(cholesterol+phospholipids)의 경우보다도 본 연구에서의 SPMVPL의 경우가 현저하게 많은 양이 소수성 부위로 침투 분포된다는 것도 확인되었다.

• Journal of the Korean Chemical Society
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• v.38 no.3
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• pp.194-199
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• 1994

The solubilization sites of some phenyl alkanols such as phenol, benzyl alcohol, phenethyl alcohol, 3-phenyl-1-propanol solubilized in 0.2 M aqueous sodium dodecylsulfate micelle solution was studied by two dimensional heteronuclear correlation spectroscopy (2D C-H COSY). The results show more quantitative and clear solubilization sites in the SDS micelle than previous results using $^1H$-NMR spectrum integration. We found that most of the phenyl alkanols penetrate into the core of SDS micelle, and the insertion depth was 6.5∼7.0 methylene units from ${\alpha}$-methylene.

• The Korean Journal of Pain
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• v.6 no.2
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• pp.237-246
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• 1993

세포막에서 마취제의 작용점을 규명하기 위하여, 마취제의 많은 부분을 차지하는 n-Alkanol을 이용하여, 소의 synaptosomal plasma membrane vesicles(SPMV)에서 n-Alkanol의 침투 정도를 형광 probe를 이용한 형광소광법을 통하여 검색하였다. n-Alkanols는 SPMV 외부 단층(outer monolayer)의 표면에 주로 분포하되 그 탄소수에 비례하여 소수성 부위에 분포되는 양이 증가되는 경향을 나타내었다(1-decanol은 제외). Methanol, Ethanol, 1-propanol, 1-butanol, 1-pentano, 1-hexanol, 1-heptanol, 1-octanol, 1-nonanol 및 1-decanil은 SPMV 외부 단층의 표면(친수성 부위)에 분포되는 것에 비하여 각각 949, 416.8, 214.8, 90.3, 53.7, 15.20, 6.80, 2.00, 1.03 및 2.40 배가 된다는 것을 확인하였다. 1-decanol은 $C_{10}$인데도 불구하고 $C_8$인 1-octanol에 비하여 적은 양이 소수성 부위에 침투 분포한다는 것이 확인되었다.