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阿片样物质在大鼠组织中的分布。

Distribution of opiate-like substances in rat tissues.

作者信息

Neidle A, Manigault I, Wajda I J

出版信息

Neurochem Res. 1979 Jun;4(3):399-410. doi: 10.1007/BF00963809.

Abstract

Rat tissues were tested for their ability to inhibit the binding of [3H]dihydromorphine or [3H]naloxone to membrane-bound opiate receptors. By this criterion, morphine-like substances were found in lung, heart, liver, and kidney as well as in brain. The relative activity of the extracts, based on initial tissue weight, differed with the radioactive lignand employed. With dihydromorphine, the order was as above. With naloxone, lung was most active, followed by heart, brain, liver, and kidney. The ability of all tissue extracts to inhibit opiate binding was reduced by 100 mM NaC1 and slightly reduced by 1 mM MnC1(2). Gel filtration using Sephadex G-25 indicated that the inhibitory substances were heterogeneous in molecular weight. Only with brain and kidney extracts was there significant activity at the elution volume where enkephalins would be expected. Fractionation using Amberlite XAD-2, a resin which selectively absorbs hydrophobic materials, again indicated that the major protion of activity in all tissue extracts was due to substances other than enkephalins.

摘要

对大鼠组织抑制[3H]二氢吗啡或[3H]纳洛酮与膜结合阿片受体结合的能力进行了检测。根据这一标准,在肺、心脏、肝脏、肾脏以及大脑中均发现了类吗啡物质。基于初始组织重量,提取物的相对活性因所使用的放射性配体而异。使用二氢吗啡时,顺序如上所述。使用纳洛酮时,肺的活性最高,其次是心脏、大脑、肝脏和肾脏。所有组织提取物抑制阿片结合的能力在100 mM氯化钠存在时降低,在1 mM氯化锰存在时略有降低。使用葡聚糖凝胶G-25进行的凝胶过滤表明,抑制物质的分子量具有异质性。只有大脑和肾脏提取物在预期脑啡肽洗脱体积处有显著活性。使用选择性吸收疏水性物质的树脂Amberlite XAD-2进行分级分离,再次表明所有组织提取物中的主要活性部分是由脑啡肽以外的物质引起的。

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