BBH 451 Pharmacodynamics Review Questions and Correct Answers

Pharmacodynamics The study of what the drug does to the body -drug receptor interactions After drugs bind to receptor sites they can... induce or block alterations of shape Agonism the drug mimics the effects of neurotransmitter Antagonism the drug prevents action that would normally be carried out when a drug binds to a receptor inverse agonism binds to the inactive form of a receptor and shifts the equilibrium so that the opposite response to an agonist is produced (from baseline) GPCRs metabotropic receptors that activate G-proteins which have a variety of actions -often activate second messengers Which two Amercian scientists shared this year's Nobel Prize for deciphering the communication system that the human body uses to send messages to the cells? Robert Lefkowitz and Brain Kobilka psychoactive drugs chemicals that affect the central nervous system and alter activity in the brain -mimic or block actions of basic neurotransmitters AG1 (DRUG) competitive agonism -because it works to get to the same sight as the endogenous ligand -fit into same space so have same activity and consequence between drug and ligand AG2 non competitive it fits into the slot so it induces the same change as the neurotransmitter (ligand) What is the initial action of a drug (ligand) binding to a receptor? the receptor changes shape -cannot get any signaling unless the shape is changed which is same with endogenous Norephinephrine (NE) Receptor Schematic GPCR threads through the membrane 7 times -length and sequence of actual extracellular parts and different amount of amino acid -each sphere is an amino acid Old prediction of NE receptor in 3D if pull transmembrane domains would not be able to see beta 2 adrenergic receptors Primary role is to expands and increase -future work includes better structure-function analysis and rational drug design by understanding drug receptor interactions -fats do not crystalize, if you know structure you can use a rational design of thinking new drugs What is the goal for Receptor structure? If you understand structure, perhaps you can design a different chemical that will fit into that pocket but interact in a different way and create a different type of agonist or antagonist (rational thinking) NE receptor with ASP highlighted aspartate interacts with NE where they interact will help us develop better drugs as well