感觉刺激受体室特性。等效蒸气浓度与饱和蒸气浓度、辛醇-水和辛醇-气分配系数有关。

Acta pharmaceutica Nordica Pub Date : 1990-01-01
G D Nielsen, E S Thomsen, Y Alarie
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引用次数: 0

摘要

受体室可以是亲水的也可以是疏水的。从辛醇-水分配系数(Po/w)与水室中测得的等效平衡浓度(Cw)之间的对数关系可以揭示其疏水特性(Franke: Theoretical Drug Design Methods)。爱思唯尔,阿姆斯特丹1984)。为了在暴露于空气中的化学物质期间激活感觉刺激受体,平衡时的Cw值可以从气体或蒸气浓度[(A] A)和水气分配系数(Pw/g)中获得。但是,如果使用辛醇-气体分配系数(Po/g),则可以直接从气体或蒸气浓度进行分析。热力学活度也可以用来揭示受体的环境是否疏水。我们已经将弗兰克的理论应用于一系列空气中的感官刺激物。我们的结果表明,感觉刺激受体的环境可能是神经膜极性部分的疏水部位。扩展理论是一般的,因此建议它适用于与疏水受体处于平衡状态的其他空气暴露浓度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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Sensory irritant receptor compartment properties. Equipotent vapour concentrations related to saturated vapour concentrations, octanol-water, and octanol-gas partition coefficients.

Receptor compartments can be hydrophilic or hydrophobic. The hydrophobic character can be revealed from the logarithmic relationship between the octanol-water partition coefficient (Po/w) and the equipotent equilibrium concentration (Cw) measured in the water compartment (Franke: Theoretical Drug Design Methods. Elsevier, Amsterdam 1984). For activation of the sensory irritant receptor during exposure to airborne chemicals the Cw values at equilibrium can be obtained from the gas or vapour concentrations [( A]a) and the water-gas partition coefficients (Pw/g). However, if the octanol-gas partition coefficients (Po/g) are used, the analysis can be carried out directly from the gas or vapour concentrations. The thermodynamic activity can also be used to reveal whether the environment of the receptor is hydrophobic or not. We have adapted Franke's theory to a series of homologous airborne sensory irritants. Our results suggest that the environment of the sensory irritant receptor is likely to be a hydrophobic site within the polar part of the nerve membrane. The extended theory is general and it is therefore suggested that it applies to other airborne exposure concentrations which are in equilibrium with a hydrophobic receptor.

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