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毒蕈碱型乙酰胆碱受体在火鸡心脏各腔室中的表达。

Expression of muscarinic acetylcholine receptors in turkey cardiac chambers.

机构信息

Institute of Pharmacology, Pharmacy and Toxicology, Faculty of Veterinary Medicine, University of Leipzig, An den Tierkliniken 15, D-04103 Leipzig, Germany.

Rudolf-Boehm-Institute of Pharmacology and Toxicology, Clinical Pharmacology, Faculty of Medicine, University of Leipzig, Härtelstr. 16 -18, D-04107 Leipzig, Germany.

出版信息

Res Vet Sci. 2021 May;136:602-608. doi: 10.1016/j.rvsc.2021.04.016. Epub 2021 Apr 16.

Abstract

The aim of the present study was to characterize the specific binding sites for [N-methyl-H]-scopolamine ([H]-NMS), a radioligand for labeling muscarinic acetylcholine receptors (mAChRs), in membranes of four heart chambers obtained from adult male British United Turkey (BUT) Big 6 ("meat-type") and Cröllwitzer ("wild-type") turkeys. MAChR subtypes were examined by inhibiting [H]-NMS binding with subtype selective non-labelled receptor antagonists. In all left and right atria as well as left and right ventricles of both turkey breeds, the specific [H]-NMS binding was saturable, reversible and of high affinity (K range: 0.5-1.0 nM). The maximum receptor density (B) was not significantly different between the four cardiac chambers of BUT Big 6 turkeys, but a significant difference was found between atria and ventricles of Cröllwitzer turkeys. Moreover, significant lower B was found in the atria of Cröllwitzer turkeys than in the atria of BUT Big 6, while the ventricular B was significantly higher. In all cardiac chambers, unlabeled mAChR antagonists competed for specific [H]-NMS binding sites in a concentration-dependent manner, suggesting the presence of the M and M receptor subtypes, whereby the latter was the predominant subtype. The presence of the M subtype could not be excluded. In conclusion, there was a difference between BUT Big 6 ("meat-type") and Cröllwitzer ("wild-type") turkeys with regard to receptor density in heart chambers with dominant M and M receptor subtypes.

摘要

本研究的目的是描述从成年雄性英国联合火鸡(BUT)Big 6(“肉用型”)和 Cröllwitzer(“野生型”)火鸡的四个心腔室获得的膜中用于标记毒蕈碱乙酰胆碱受体(mAChR)的 [N-甲基-H]-东莨菪碱([H]-NMS)的特异性结合位点。mAChR 亚型通过用亚型选择性非标记受体拮抗剂抑制 [H]-NMS 结合来检查。在 BUT Big 6 火鸡的所有左右心房以及左右心室中,特异性 [H]-NMS 结合是可饱和的、可逆转的且具有高亲和力(K 范围:0.5-1.0 nM)。BUT Big 6 火鸡的四个心腔室之间的最大受体密度(B)没有显着差异,但在 Cröllwitzer 火鸡的心房和心室之间发现了显着差异。此外,在 Cröllwitzer 火鸡的心房中发现 B 显着低于 BUT Big 6 的心房,而心室 B 显着更高。在所有心腔室中,非标记的 mAChR 拮抗剂以浓度依赖性方式竞争特异性 [H]-NMS 结合位点,表明存在 M 和 M 受体亚型,其中后者是主要亚型。不能排除 M 亚型的存在。总之,BUT Big 6(“肉用型”)和 Cröllwitzer(“野生型”)火鸡在心腔室中存在受体密度的差异,主要存在 M 和 M 受体亚型。

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