NOVEL ANTIHYPERTENSIVES: RATIONAL DESIGN AND EVALUATION

新型抗高血压药：合理设计和评估

• 批准号: 3339576
• 负责人: SHELDON W MAY
• 金额: $ 24.86万
• 依托单位: GEORGIA INSTITUTE OF TECHNOLOGY
• 依托单位国家: 美国
• 财政年份: 1982
• 资助国家: 美国
• 起止时间: 1982-01-01 至 1994-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3339576
• 关键词: antihypertensive agents; cardiovascular pharmacology; dopamine beta monooxygenase; dopamine hydroxylase inhibitor; drug design /synthesis /production; drug metabolism; drug screening /evaluation; enzyme mechanism; heart rate; laboratory rat; peripheral nervous system; prodrugs; selenium; spontaneous hypertensive rat; sulfur compounds; tissue /cell culture; tyrosine analog

Hypertension is a causative factor in the genesis of many cardiovascular diseases, and is thus the focus of much current research. We are investigating and evaluating -- at the cellular, molecular enzymological and whole animal levels -- novel but structurally simple compounds of our own design which have the potential of acting as antihypertensive agents. Our compounds are designed so that in many cases they can act as pro-drugs or suicide substrates which we expect to affect principally the peripheral nervous system, although in some cases central effects may also be present. A variety of experimental approaches, ranging from bioassays to subcellular fraction experiments to enzymatic studies, are being employed. It is hoped that our results will establish the basis for design of new classes of clinically useful compounds.

高血压是多种心血管疾病的致病因素 疾病，因此是当前许多研究的焦点。 我们是 研究和评估——细胞、分子酶学 和整个动物水平——我们的化合物新颖但结构简单 自己的设计，具有作为抗高血压药物的潜力。 我们的化合物经过精心设计，在许多情况下可以充当前药 或自杀底物，我们预计主要影响外周 神经系统，尽管在某些情况下中枢效应也可能是 展示。 多种实验方法，从生物测定到 正在采用亚细胞级分实验和酶学研究。 希望我们的结果能够为新的设计奠定基础 临床上有用的化合物的类别。