TRITIUM LABELLING OF SEROTONIN ANALOG: GASTROINTESTINAL DISORDER & ULCERS

血清素类似物的氚标记：胃肠道疾病

• 批准号: 6220433
• 负责人: HIROMI MORIMOTO
• 金额: $ 0.61万
• 依托单位: UNIVERSITY OF CALIF-LAWRENC BERKELEY LAB
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-08-01 至 2000-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6220433
• 关键词: biomedical resource; female; human subject; male

Muscarinic receptors mediate the cellular actions of acetylcholine at the parasympathetic neuroeffector junction. In addition, these receptors mediate cholinergically mediated effects in the central nervous system (CNS), particularly in cortical and subcortical regions of the brain. Five muscarinic genes, m1 to m5 have been cloned, where m1, m2 and m3 appear to correspond to the pharmacological subtypes M1, M2 and M3 respectively. Muscarinic M3 antagonist are potentially useful as spasmolytics for the treatment of patients with various conditions involving smooth muscle spasms such as gastrointestinal motility disorders, functional diarrhea, irritable bowel syndrome, gastric and duodenal ulcers, spasms of the urinary tract and urinary incontinence. Scientists at Pfizer, Inc. have designed and synthesized Darifenacin for the treatment of urinary incontinence and irritable bowel disease. Tritium-labelled Darifenacin with high specific activity is required for receptor binding studies. The tritiated precursor from this labelling project will be converted to Darifenacin, which is a standard used to investigate the muscarinic receptor antagonist pharmacology. User Details: Experiment Details: User Number: 1616 Tritiation City, State: Palo Alto, CA NMR Funding Source: Industry Tritides Charge: $1752.52 1 day Program Income: $1505.70 1 compound

M受体介导乙酰胆碱的细胞作用 在副交感神经效应器交界处。此外，这些 受体介导中枢胆碱介导的效应 神经系统(CNS)，特别是皮质和皮质下区域 大脑的一部分。已经克隆了5个毒扁豆碱基因M1至M5，其中 M1、M2和M3似乎对应于药理亚型M1， M2和M3。毒鼠强M3拮抗剂具有潜在的 可作为解痉剂用于治疗各种不同类型的 涉及胃肠道等平滑肌痉挛的情况 运动障碍，功能性腹泻，肠易激综合征， 胃和十二指肠溃疡、尿路痉挛和尿路痉挛 大小便失禁。辉瑞公司的科学家们设计了一种 合成达利芬治疗尿失禁和尿失禁 肠易激疾病。高纯度氚标记达菲他汀类药物 受体结合研究需要特定的活性。这个 来自该标签项目的氚前体将被转换为 达菲他汀，这是一种用来研究毒鼠强的标准 受体拮抗剂药理学。用户详情：实验详情： 用户编号：1616 Tritiation City，State：Palo Alto，CA NMR Funding 来源：行业三重奏收费：1752.52美元一天计划收入： $1505.70 1化合物