DRUG DESIGN FOR THE TREATMENT OF BLADDER INCONTINENCE

治疗膀胱失禁的药物设计

• 批准号: 3487827
• 负责人: EDWARD JAKOBOVITS
• 金额: $ 5万
• 依托单位: NEUREX CORPORATION
• 依托单位国家: 美国
• 财政年份: 1989
• 资助国家: 美国
• 起止时间: 1989-08-01 至 1990-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3487827
• 关键词: drug design /synthesis /production; immunocytochemistry; in situ hybridization; inhibitor /antagonist; ion exchange chromatography; laboratory rabbit; molecular cloning; muscarinic receptor; nervous system disorder chemotherapy; nucleic acid sequence; radioimmunoassay; receptor binding; receptor expression; stimulant /agonist; synthetic nucleic acid; tissue /cell culture; transfection; transposon /insertion element; urinary incontinence; western blottings

Bladder incontinence is a functional disorder with growing consequences for the aging population. Current therapy includes drug treatment aimed at antagonizing the cholinergic input to the bladder. There are severe drawbacks to drug therapy primarily due to the lack of specificity of the drugs which result in side effects, many of which cannot be tolerated by the elderly. We propose to design novel pharmaceutica agents which are both efficacious and highly specific. Using rDNA technologies we will design peptomementic molecules which reconstruct specific sites of receptor interaction with cellular metabolic machinery and, as a result, mimic receptor action. This will provide a new approach for the rational design of more specific drugs to address problems of the autonomic nervous system.

膀胱失禁是一种后果日益严重的功能性疾病。 为老龄化的人口服务。目前的治疗方法包括有针对性的药物治疗 拮抗胆碱能传入膀胱的作用。有严重的 药物治疗的缺点主要是由于缺乏特异性 导致副作用的药物，其中许多不能 为老年人所容忍。 我们建议设计新的药物制剂，它们都是 有效且高度特效。使用rDNA技术，我们将设计 重组受体特定部位的胃动素分子 与细胞代谢机制的相互作用，结果是模仿 受体作用。这将为Rational提供一种新的方法 设计更具针对性的药物来解决自主神经的问题 神经系统。