TRITIUM LABELLING OF SEROTONIN ANALOG: GASTROINTESTINAL DISORDER & ULCERS

毒蕈碱受体介导乙酰胆碱的细胞作用 在副交感神经效应器连接处 另外这些 受体介导中枢胆碱能介导的作用 神经系统（CNS），特别是皮质和皮质下区域 的大脑。 已经克隆了五个毒蕈碱基因，m1到m5，其中 m1、m2和m3似乎对应于药理学亚型M1， M2和M3。 毒蕈碱M3拮抗剂可能 可用作治疗患有各种 涉及平滑肌痉挛的病症，如胃肠 动力障碍，功能性腹泻，肠易激综合征， 胃溃疡和十二指肠溃疡、尿路痉挛和泌尿系统疾病 失禁 辉瑞公司的科学家们设计并 用于治疗尿失禁的合成达非那新， 肠易激综合征 氚标记达非那新， 受体结合研究需要比活性。 的 这项标签计划所产生的氚化前体， 达非那新，这是一个标准，用于研究毒蕈碱 受体拮抗剂药理学 用户详细信息：实验详细信息： 用户编号：1616 Triation市，州：Palo Alto，CA NMR资金 来源：Industry Tritides费用：$1752.52 1天计划收入： $1505.70 1化合物

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