Dinner

In this introductory session we will discuss the principle of how drugs interact with receptors, ion channels and enzymes and then discuss major reasons why drugs fail in clinical trials and why this highlights the importance of ’thorough ‘ pharmacology.

Close

Introduction to day 1 - What Data is collected in Equilibrium Assays and what does it miss?

What is a Ki and Kd - What do they mean, what is the Value of such Data in Drug Discovery Programmes

Breakout Session: Ligand Binding in Agonist v. Antagonist Programmes

Coffee Break

Types and Antagonism, Assay used, Interpretation of Data

Breakout: Types of Inhibition/Antagonism; Ligand Binding v. Function; Allosterism

Lunch

How can you predict if your Antagonist/inhibitor is likely to have Efficacy in vivo

Breakout: can you explain why one Antagonist/inhibitor has worked but one hasn’t

Coffee Break

Drug Case History Angiotensin 1 receptor antagonists for hypertension

Round up of Day 1

Introduction to Day 2

Defining Agonist Action: Assays used to assess Potency and Efficacy at GPCRs and Ion Channels

Breakout Session: Assessing Potency and Selectivity of Agonists in vitro

Coffee Break

The importance of defining Agonist Action in terms of Affinity driven and Efficacy

Breakout Session: why doesn’t your Agonist work in Natural Receptor Systems?

Lunch

Breakout session: What do these PK-PD Profiles indicate about Drug Receptor Interactions?

Coffee Break

Drug Case History – The Transformation of Adrenaline into inhaled beta 2 Agonists to treat Asthma

Round Up of Day 2

Introduction

Principles of Receptor Kinetics and Assays

Coffee Break

What do these Kinetic Profiles indicate?

Feedback from Breakout Session

Summary

Lunch and depart