PHPY 304 Chapter Notes - Chapter 1: Receptor Antagonist, Partial Agonist, Van Der Waals Force
18 Nov 2016
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Pharmacodynamics: define receptor, agonist, antagonist, partial agonist, affinity, intrinsic activity, efficacy, therapeutic index, therapeutic window, ec50, kd. Receptor: a macromolecule whose biological function changes when a drug binds to it. Most drugs produce their pharmacological effects by binding to specific receptors in target tissues. Drug-receptor binding triggers a cascade of events known as signal transduction, through which the target tissue responds. Antacids and laxatives are examples, because they are just causing acid-base reactions. Types of bonds between drug and receptor: van der waals force: weak, short-range electrostatic attractive forces between uncharged molecules, arising from the interaction of permanent or transient electric dipole moments. Ionic interactions: chemical bonds formed between two ions with opposite charges. Bonds form when one ion gives one or more protons to the other. This leads to toxicity: stereospecific interactions: >50% of drugs exist as stereoisomers and interact stereospecifically with receptors. Multiple bonds are involved in the stereospecific interaction between a receptor and its ligand.
