Module Title Molecular Pharmacology, PHARG003 Core module, 15

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Module Title Molecular Pharmacology, PHARG003

Core module, 15 credits

Module code

Module leader

Short description

Module aims

Module objectives

PHARG003

Dr Alasdair Gibb and Dr Guy Moss

Molecular Pharmacology is a 0.5 unit (15 credits) course designed to provide core material on the structure and function of receptors and the quantitative aspects of the action of drugs at receptors.

The course aims to teach students about the structure and function of neurotransmitter and hormone receptors and about the quantitative aspects of the action of drugs at receptors.

On completion of the course, students should have a detailed knowledge of the following topics

1) Use of the Law of Mass Action to quantify the interaction of drugs and receptors

2) The action of agonists and antagonists and the concept of efficacy

3) Ion channel receptors and their activation and block

4) The structure of transporters, ion channel receptors and G protein-coupled receptors

5) Radioligand binding

Module assessment

(percentage)

Written examination

(percentage)

List of possible lectures/seminars

Dates of schedule

25% ; Coursework: Radioligand binding data analysis exercise (12.5%) and bioinformatics exercise (12.5%)

75% ; Three hour exam with one data analysis question (30%) and one essay

(45%).

Receptors; early ideas, concentration-response curves

Competitive antagonism I

Irreversible and non-competitive antagonism

Competitive antagonism II

Sodium channel block data analysis exercise

Efficacy, partial agonists

Agonist efficacy; meaning and measurement

Structure and assembly of ligand-gated ion channel receptors

Structure-function relations among ligand-gated ion channel receptors

Receptor structure: G protein coupled receptors

Radioligand binding; theory

Radioligand binding; practical aspects.

Radioligand binding data analysis exercise

Non-linear curve fitting

Algebra revision - optional tutorial

Radioligand binding data analysis: optional tutorial

Structure and function of neurotransmitter transporters

Principles of in vivo drug binding: PET and SPECT

Tutorial (Problem sheets)

Agonist efficacy; single receptor molecule concepts

Agonist efficacy; constitutively active receptors

Structure-function of CFTR and ABC transporters

Molecular mechanism of CFTR and ABC transporters

Principles of the rates of drug action: the rate at which equilibrium is approached

Rates of antagonist action: ion channel block

Tutorial (Problem sheets)

Classical pharmacology in modern drug development

Radioligand binding data analysis: optional tutorial

Term 1: Monday 11:00-1:00 and 2:00-5:00; Wednesday 9:00-11:00

1st Lecture: Wednesday 30th September, 9.00am, Roberts 106,

Lecture Theatre Course material, Lecture Notes and Problem Sheets can

be downloaded from Moodle.

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