1、分 子药理学晏为力教学大纲中文名称 分子药理学英文名称 Molecular Pharmacology 课 内总学时 ： 32 教学方式：讲授 撰写人 ：晏 为力 考核方式：考试 +论文报告 开课学期： 学分数 : 2 内容偏重 ：理 论 教学要求及目的 使学生了解分子药理学的基础知识和各系统分子药理学的进展，为从事药学基础研究工作和新药开发奠定理论基础。课程内容 内容 授 课人 日期 1绪论 : 分子药理学研究内容 , 药物作用的机制 晏 为力 9/11 2受体药理及信号传导 9/18 3细胞内第二信使蛋白激酶及有关药物进展 9/25 4炎症介质与抗炎药物 10/9 5抗糖尿病药物 谭 睿 1
2、0/16 6缺血再灌注性损伤的分子机制 10/23 7抗体及生物技术药物分子药理学基础 喻 凯 10/30 8离子通道和抗心律失常药理 11/6 9高血压药的分子药理学 11/13 10细胞色素 p450及调控 11/20 11神经药理的分子药理学基础 黄新河 11/27 12学习、记忆药理及老年痴呆的药物干预 12/4 13细胞凋亡机理及抗癌药物研究进展 12/11 14氧自由基与抗氧化剂及一氧化氮 12/18 考核方式： 上课情况 15%， 学期论文 25%，考试 60%分子药理学（ Molecular Pharmacology) 分子药理学属于一门新兴学科，其与传统 药理学 的最大区别就
3、在于，它是从分子水平和 基因表达 的角度去阐释药物作用及其机制。 The use of techniques of molecular biology to enhance the understanding of the mechanism of action of existing drugs, and with the help of molecular graphics to predict the structure of novel drugs, especially compounds that might bind to proteins of known structure.
4、 近代药理学的进展，主要表现在 受体 理论、 离子通道 、 信息传递 、 细胞因子 等分子水平上的研究突破。分子药理学是指其学科层次、水平上的科学性和先进性达到 “ 分子水平 ” ，且又属于 “ 药理学 ” 范畴， 分子生物学 等相关学科的基础知识贯穿其中。药物的作用机制 Receptors Drug/receptors and biological responses Second-messenger systems The chemistry of drug-receptor binding Dynamics of drug-receptor binding Dose response r
5、elationship Potency and intrinsic activity Drug antagonismReceptor A fundamental concept of pharmacology: to initiate an effect in a cell, most drugs combine with some molecular structure on the surface of or within the cell. This molecular structure is called a receptor. Receptor + Drug ? Complex ?
6、 ? ?ResponsesDRUG RECEPTORS AND BIOLOGICALRESPONSES Receptor: molecular substances or macromolecules in tissues that combine chemically with the drug. Ach receptor Na influx action potential increased free Ca contraction Specific receptive substances serve as triggers of cellular reactions.Agonist v
7、s Antagonist Chemicals that interact with a receptor to initiate a cellular reaction are termed agonists. Antagonist interacts with the receptor and prevents the interaction of agonist with its receptor.SECOND-MESSENGER SYSTEMS Many receptors are capable of initiating a chain of events involving sec
8、ond messengers. G proteins, short for guanine nucleotidebinding proteins. G proteins have the capacity to bind guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). Receptor activation, G protein, adenylyl cyclase, ATP-cAMP, kinases activation, protein phosphorylation. Which
9、G protein couples with the receptor Which kinase is activated Which proteins are accessible for the kinase to phosphorylateThe specific binding sites for agonists occur at the extracellular surface, while the interaction with G proteins occurs with the intracellular portionsof the receptor. The general term for any chain of events initiated by receptor activation is signal transduction.
