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血清素能配体与猪脉络丛的结合:一种新型5-羟色胺识别位点的特性

The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site.

作者信息

Pazos A, Hoyer D, Palacios J M

出版信息

Eur J Pharmacol. 1984 Nov 27;106(3):539-46. doi: 10.1016/0014-2999(84)90057-8.

Abstract

The kinetic and pharmacological characteristics of the binding of [3H]5-HT (serotonin), [3H]8-OH-DPAT (8-OH-2-di-n-propylaminotetraline), [3H]LSD, [3H]ketanserin and [3H]mesulergine to membranes from frontal cortex, hippocampus and choroid plexus of pig brain were studied. The binding of these ligands to frontal cortex and hippocampus demonstrated the presence of 5-HT1 and 5-HT2 sites in both tissues, although hippocampus was richer in 5-HT1 (subtype 5-HT1A) sites. [3H]5-HT, [3H]mesulergine and [3H]LSD labeled the pig choroid plexus with high affinity. The pharmacological profiles of [3H]5-HT and [3H]mesulergine binding to this tissue were closely comparable. Ligands reported as selective for 5-HT1A, 5-HT1B or 5-HT2 subtypes did not show high affinity for these binding sites. Therefore, these 5-HT binding sites in pig choroid plexus could be named 5-HT1C. Other drugs with a high affinity for these sites were methysergide and mianserine. In pig frontal cortex, [3H]5-HT labeled the different subtypes of 5-HT1 sites. In contrast, [3H]mesulergine bound in pig frontal cortex to a small population of sites with pharmacological properties similar to those of the choroid plexus 5-HT1C sites. Possible physiological functions in which these sites might be involved are discussed.

摘要

研究了[3H]5-羟色胺(血清素)、[3H]8-羟基-2-二正丙基氨基四氢萘(8-OH-DPAT)、[3H]麦角酸二乙胺(LSD)、[3H]酮色林和[3H]美舒麦角与猪脑额叶皮质、海马和脉络丛膜的结合动力学及药理学特性。这些配体与额叶皮质和海马的结合表明,两种组织中均存在5-HT1和5-HT2位点,尽管海马中5-HT1(5-HT1A亚型)位点更为丰富。[3H]5-羟色胺、[3H]美舒麦角和[3H]LSD以高亲和力标记猪脉络丛。[3H]5-羟色胺和[3H]美舒麦角与该组织结合的药理学特征密切可比。据报道对5-HT1A、5-HT1B或5-HT2亚型具有选择性的配体对这些结合位点没有高亲和力。因此,猪脉络丛中的这些5-羟色胺结合位点可命名为5-HT1C。对这些位点具有高亲和力的其他药物有甲基麦角新碱和米安色林。在猪额叶皮质中,[3H]5-羟色胺标记了5-HT1位点的不同亚型。相比之下,[3H]美舒麦角在猪额叶皮质中与一小部分位点结合,这些位点的药理学特性与脉络丛5-HT1C位点相似。讨论了这些位点可能参与的潜在生理功能。

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