大鼠脑匀浆中去甲肾上腺素能和多巴胺能神经元突触小体摄取儿茶酚胺抑制作用的构效关系。
Structure-activity relations for the inhibition of catecholamine uptake into synaptosomes from noradrenaline and dopaminergic neurones in rat brain homogenates.
作者信息
Horn A S
出版信息
Br J Pharmacol. 1973 Feb;47(2):332-8. doi: 10.1111/j.1476-5381.1973.tb08331.x.
Abstract
- The effects of various phenylethylamine analogues on the inhibition of (3)H-noradrenaline and (3)H-dopamine uptake into homogenates of rat hypothalamus and corpus striatum respectively, were examined.2. Phenolic hydroxyl groups and alpha-methylation of the side chain were both found to enhance the affinity for the neuronal uptake sites.3. Methoxylation, beta-hydroxylation and N-methylation were all found to reduce the ability of a compound to inhibit catecholamine transport.4. The noradrenaline and dopamine transport systems responded in a quantitatively different manner to the various phenylethylamine analogues. It was found that, in general, the noradrenaline uptake process was more sensitive to structural changes, both positive and negative, than the dopamine system.
摘要
研究了各种苯乙胺类似物分别对大鼠下丘脑和纹状体匀浆中(3)H-去甲肾上腺素和(3)H-多巴胺摄取的抑制作用。
发现酚羟基和侧链的α-甲基化均增强了对神经元摄取位点的亲和力。
发现甲氧基化、β-羟基化和N-甲基化均降低了化合物抑制儿茶酚胺转运的能力。
去甲肾上腺素和多巴胺转运系统对各种苯乙胺类似物的反应在数量上有所不同。结果发现，一般来说，去甲肾上腺素摄取过程比多巴胺系统对结构变化（无论是正向还是负向）更敏感。
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Regional differences in H3-norepinephrine and H3-dopamine uptake into rat brain homogenates.大鼠脑匀浆中H3-去甲肾上腺素和H3-多巴胺摄取的区域差异。
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Quantum mechanical study of the conformational properties of phenethylamines of biochemical and medicinal interest.对具有生化和医学意义的苯乙胺构象性质的量子力学研究。
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