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咪唑啉识别位点与胃功能。

Imidazoline recognition sites and stomach function.

作者信息

Molderings G J, Burian M, Menzel S, Donecker K, Homann J, Nilius M, Göthert M

机构信息

Institute of Pharmacology and Toxicology, University of Bonn, Germany.

出版信息

Ann N Y Acad Sci. 1999 Jun 21;881:332-43. doi: 10.1111/j.1749-6632.1999.tb09377.x.

Abstract

Radioligand binding experiments carried out in cell membranes from rat and human stomach revealed the existence of non-adrenoceptor [3H]clonidine and [3H]idazoxan binding sites and of [3H]DTG (1,2-di-(2-tolyl)guanidine) binding sites. In rat stomach, specific binding was inhibited by imidazolines and guanidines and by non-imidazoline sigma-site ligands, respectively, at different rank orders of affinity, suggesting the existence of non-I1/non-I2 [3H]clonidine binding sites, I2-imidazoline binding sites as well as sigma 2-like-sites. These sites are not directly related to a postsynaptic contractile effect on rat gastric smooth muscle or to acid release from isolated gastric glands. Finally, we demonstrated that the gastric pathogen Helicobacter pylori is able to form and to release the endogenous imidazoline receptor ligand agmatine and that considerable amounts of agmatine are present in human gastric juice. The quantities of agmatine were higher in gastric juice from H. pylori-positive than H. pylori-negative patients.

摘要

在大鼠和人胃的细胞膜上进行的放射性配体结合实验揭示了非肾上腺素能受体[3H]可乐定和[3H]咪唑克生结合位点以及[3H]DTG(1,2 - 二 - (2 - 甲苯基)胍)结合位点的存在。在大鼠胃中,特异性结合分别被咪唑啉和胍以及非咪唑啉σ位点配体以不同的亲和力等级顺序抑制,这表明存在非I1/非I2 [3H]可乐定结合位点、I2 - 咪唑啉结合位点以及σ2样位点。这些位点与大鼠胃平滑肌的突触后收缩效应或离体胃腺的酸释放没有直接关系。最后,我们证明了胃病原体幽门螺杆菌能够合成并释放内源性咪唑啉受体配体胍丁胺,并且人胃液中存在大量的胍丁胺。幽门螺杆菌阳性患者胃液中胍丁胺的含量高于幽门螺杆菌阴性患者。

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