CHARACTERIZATION OF HEART ATRIAL MUSCARINIC RECEPTOR

心房毒蕈碱受体的表征

• 批准号: 3337343
• 负责人: Michael Schimerlik
• 金额: $ 11.64万
• 依托单位: OREGON STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1980
• 资助国家: 美国
• 起止时间: 1980-07-01 至 1986-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3337343
• 关键词: acetylcholine; affinity chromatography; antibody; anticholinergic agent; atrium; chemical reaction; cholinergic agents; density gradient ultracentrifugation; fluorescent dye /probe; gel filtration chromatography; guanine nucleotides; guanylate cyclase; heart pharmacology; ligands; molecular weight; radiotracer; thermodynamics

Parasympathetic innervation of the heart, mediated in the atria by the muscarinic acetylcholine receptor; is known to be involved in the genesis and facilitation of a number of cardiac arrhythmias. In order to gain insight in to the molecular mechanism and composition of the muscarinic receptor, the purification of this protein is proposed using techniques such as affinity chromatography. Hydrodynamic studies are proposed in order to gain information on the apparent molecular weight and shape of the solubilized protein. Thermodynamic studies of the effects of putative regulatory agents such as guanine nucleotides are proposed in order to determine the mechanism by which these compounds affect receptor interactions with muscarinic agonists and antagonists. Information obtained as a result of these studies will increase our level of understanding of neural control of the heart and may lead to the development of more effective antiarrhythmic agents.

心脏的副交感神经支配，由心房介导 毒蕈碱乙酰胆碱受体；已知参与创世 并促进一些心律失常。 为了获得 深入了解毒蕈碱的分子机制和组成 受体，建议使用技术纯化该蛋白质 如亲和层析。 流体动力学研究提出于 为了获得有关表观分子量和形状的信息 溶解的蛋白质。 假定影响的热力学研究 建议使用鸟嘌呤核苷酸等调节剂来 确定这些化合物影响受体的机制 与毒蕈碱激动剂和拮抗剂的相互作用。 信息 这些研究的结果将提高我们的水平 了解心脏的神经控制并可能导致 开发更有效的抗心律失常药物。