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局部麻醉药跨色素细胞膜的转运。

Transport of local anaesthetics across chromatophore membranes.

作者信息

Packham N K, Jackson J B

出版信息

Biochim Biophys Acta. 1979 Apr 11;546(1):142-56. doi: 10.1016/0005-2728(79)90176-2.

DOI:10.1016/0005-2728(79)90176-2
PMID:312654
Abstract
  1. Both simple amines and tertiary amino local anaesthetics give rise to an accelerated decay of the absorption change of added pH indicator dyes and a decelerated decay of the endogenous carotenoid absorption band shift, following short flash excitation of Rhodopseudomonas sphaeroides chromatophores. 2. With increasing medium pH, lower concentrations of amine or local anaesthetics are effective. 3. The order of potency of the local anaesthetics concurs with their reported membrane/buffer partition coefficients and concentrations required for action potential blockade in nerve fibres. 4. The data are taken as evidence for rapid transport of the free base across the chromatophore membrane and relatively slow penetration of the protonated local anaesthetic. Protolytic reactions complete the effective dissipation of the trans-membrane pH gradient. 5. Benzocaine, with its unusually low pKa and the quaternary derivative, chloropromazine methiodide do not display this type of behaviour. 6. In the presence of membrane potential-collapsing agents, such as valinomycin/K+ or thiocyanate ions, local anaesthetics decelerate the decay of the cresol red change but have no effect on the carotenoid shift decay. It appears that transport of the unprotonated local anaesthetic although electrically neutral, requires the presence of a membrane potential. 7. In contrast, the non-anaesthetic amines act independently of the membrane potential. 8. Ca2+ interferes with the mechanism of local anaesthetic deceleration of the cresol red change decay in the presence of valinomycin/K+ or thiocyanate but not with other anaesthetic or amine reactions.
摘要
  1. 对球形红假单胞菌的载色体进行短闪光激发后,简单胺类和叔氨基局部麻醉剂都会使添加的pH指示剂染料的吸收变化衰减加速,使内源性类胡萝卜素吸收带位移的衰减减速。2. 随着介质pH值升高,较低浓度的胺或局部麻醉剂即可产生效果。3. 局部麻醉剂的效能顺序与其报道的膜/缓冲液分配系数以及神经纤维动作电位阻断所需浓度相符。4. 这些数据被视为游离碱快速穿过载色体膜以及质子化局部麻醉剂穿透相对缓慢的证据。质子转移反应完成了跨膜pH梯度的有效消散。5. 苯佐卡因具有异常低的pKa值,其四元衍生物氯丙嗪甲碘化物不表现出这种行为。6. 在存在膜电位塌陷剂(如缬氨霉素/K⁺或硫氰酸根离子)的情况下,局部麻醉剂会使甲酚红变化的衰减减速,但对类胡萝卜素位移衰减没有影响。看来未质子化的局部麻醉剂的转运虽然呈电中性,但需要膜电位的存在。7. 相比之下,非麻醉性胺类的作用与膜电位无关。8. 在存在缬氨霉素/K⁺或硫氰酸盐的情况下,Ca²⁺会干扰局部麻醉剂使甲酚红变化衰减减速的机制,但不会干扰其他麻醉剂或胺类的反应。

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1
Transport of local anaesthetics across chromatophore membranes.局部麻醉药跨色素细胞膜的转运。
Biochim Biophys Acta. 1979 Apr 11;546(1):142-56. doi: 10.1016/0005-2728(79)90176-2.
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The effect of diaminodurene on the delayed light and the carotenoid band shift in Rhodopseudomonas spheroides.二氨基杜烯对球形红假单胞菌延迟发光和类胡萝卜素谱带位移的影响。
Biochim Biophys Acta. 1972;283(1):67-78. doi: 10.1016/0005-2728(72)90099-0.
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Biochim Biophys Acta. 1973 Oct 19;325(1):102-13. doi: 10.1016/0005-2728(73)90155-2.

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