This exam consists of short answer questions (SAQs) for your practice. All questions are of equal value (15 marks). 本次考试包含简答题(SAQs)以供练习。所有问题价值相等(15 分)。
In this practice test, you have unlimited time and unlimited attempts up until your final exam. 在这次练习测试中,你有无限的时间和无限的机会,直到你的最终考试。
SECTION B 第一节
Answer each question in the text box. Please note in the exam you will need to answer and SAQ for Modules 1-3. For each module you will be able to choose between 2 questions that may have multiple parts; only answer one of the two questions. 在文本框中回答每个问题。请注意,在考试中,你需要为模块 1-3 回答一个 SAQ。对于每个模块,你可以在两个可能包含多个部分的问题中选择一个问题进行回答;只需回答其中一个即可。
For this practice exam, SAQs will not be marked. 本次练习考试,SAQs 将不会评分。
SAQs Module 1 Principles of Drug Action: Pharmacodynamic SAQs 模块 1 药物作用原理:药效学
Question 115 pts 题目 115 分
Module 1 (Example 1) Principles of Drug Action: Pharmacodynamics 模块 1(示例 1)药物作用原理:药效学
A. Explain the steps involved when an agonist interacts with its receptor target(s) to elicit a response. In your answer explain affinity, selectivity, intrinsic efficacy, and potency and identify at which steps these occur or can be measured. Be specific when defining the terms (12 marks). A. 解释激动剂与其受体靶点相互作用以引起反应的步骤。在您的答案中解释亲和力、选择性、内在效力和效能,并确定这些步骤发生在何处或如何测量。在定义这些术语时要具体(12 分)。
B. Provide an example of an agonist interacting with it’s target in the heart or lung and describe the response that occurs (3 marks). B. 提供一个激动剂与其靶点在心脏或肺部相互作用的例子,并描述发生的反应(3 分)。
Describe the relationship between concentration (on a linear-scale) and response. (1 mark) 描述浓度(线性尺度)与反应之间的关系。(1 分)
Describe the relationship between concentration (on a log-scale) and response. (1 mark) 描述浓度(对数尺度)与响应之间的关系。(1 分)
What effect does the Hill-slope (h)(h) have on the relationship between log-concentration and response? (1 mark) 希尔斜率 (h)(h) 对对数浓度与响应之间的关系有何影响?(1 分)
Describe three reasons why the EC_(50)\mathrm{EC}_{50} value may differ from the dissociation constant (K_(D))\left(\mathrm{K}_{\mathrm{D}}\right) for an agonist. (3 marks) 描述三种可能导致 EC_(50)\mathrm{EC}_{50} 值与激动剂的解离常数 (K_(D))\left(\mathrm{K}_{\mathrm{D}}\right) 不同的原因。(3 分)
Part B Pharmacodynamics for salbutamol and law of mass action (9 marks) B 部分:沙丁胺醇的药理学和作用量定律(9 分)
Name the receptor and the pharmacodynamic effect of salbutamol on the airways and the heart? (3 marks) 请说出沙丁胺醇对呼吸道和心脏的受体及药效动力学作用。(3 分)
What is the cytosolic signaling mechanism that causes this pharmacodynamic effect of salbutamol in the airways? Either draw or describe in words (3 marks) 沙丁胺醇在呼吸道中产生这种药效动力学作用的细胞质信号传导机制是什么?请绘制或用文字描述。(3 分)
What would be your prediction of using an antagonist such as propranolol (non-selective) on the respiratory system? (1 mark) 如果使用如普萘洛尔(非选择性)这样的拮抗剂对呼吸系统的影响,你的预测是什么?(1 分)
This receptor that salbutamol targets exhibits constitutive activity. Describe what this means and what the effect would be if this receptor was internalized through desensitization. (2 marks) 沙丁胺醇靶向的这种受体表现出构成活性。请描述这意味着什么,如果这种受体通过脱敏作用内化,会产生什么效果。(2 分)
Module 2 Molecular Pharmacology and Drug Discovery (Part A, B and C) - File Upload Question 模块 2 分子药理学与药物发现(A、B 和 C 部分) - 文件上传问题
Part A: The figure below shows the interaction between acetylcholine and muscarinic acetylcholine receptor. What kind of binding can you recognise as being important between acetylcholine and Asn617 and Asp-311? For this type of question you would need to remember what are the important properties of each type of amino acid. Keep in mind that Rob Vandenberg is a structural biologist, so his interest is in understanding the relationship between ligands and proteins. Ligands are usually small molecules such as nicotine or peptides such as oxytocin. Another exercise would be to label the interactions between the amino acids and a muscarinic antagonist. Going through such exercises will help you recognise the R groups of the 20 amino acids. You would be expected to remember what type of interactions each of the amino acids might have. Part A: 下图展示了乙酰胆碱与毒蕈碱型乙酰胆碱受体的相互作用。你能识别出乙酰胆碱与 Asn617 和 Asp-311 之间的哪种结合方式是重要的?对于这类问题,你需要记住每种氨基酸的重要性质。记住,Rob Vandenberg 是一位结构生物学家,他的兴趣在于理解配体与蛋白质之间的关系。配体通常是像尼古丁这样的小分子或像催产素这样的肽。另一个练习是标记氨基酸与毒蕈碱拮抗剂之间的相互作用。通过这样的练习,将有助于你识别 20 种氨基酸的 R 基团。你将需要记住每种氨基酸可能有什么类型的相互作用。
Asn-617- NH_(2)\mathrm{NH}_{2}
Trp-307
Asp-311
Ala-505 阿拉-505
C[14CH3]CCOC(C)=OOO
Tyr-616 泰尔-616
Ala-508 阿拉-508
CC(=O)OCC[18OH]OOO18H
Trp-613 亮氨酸-613
Part B: Name all types of reversible bond interactions with that the tyrosine (left panel) and lysine (right panel) functional groups could potentially have with different drugs. B 部分:列出酪氨酸(左侧面板)和赖氨酸(右侧面板)官能团可能与其他药物发生的所有可逆键合相互作用类型。