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Lecture 2B - Pharmacodynamics.docx

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PSYC 3403
Tarry Ahuja

Lecture 2B - Pharmacodynamics Pharmacodynamics: How Drugs Act Chapter 2 Lecture 2B – January 15, 2014 Overview • receptor as a site of drug action • dose-response curves • drug safety • effectiveness Pharmacodynamics is the study of the biochemical and physiological effects of drugs and the mechanisms of drug action and the relationship between drug concentration and effect L + R L•R - L refers to anything that interacts with a neurotransmitor (Ligan) - R (receptor) R is the keyhole in the process (accepting) - Double sided arrow because it is in constant flux Receptors (characteristics) • membrane-spanning protein • binding sites for endogenous NTs and drug molecules (Drugs are exdrogenous) Lecture 2B - Pharmacodynamics Receptors (characteristics) • composed of 7 or 12 alpha helical coils • NT’s and drugs binds within TM coils held by ionic forces Nterminus and Cterminus Drug/NT Binding Lecture 2B - Pharmacodynamics Receptors (characteristics) • reversible binding activates receptor causing conformational change • intensity of signal determined by number of percentage of drug-receptor interaction • NT’s and drugs interact with binding site on receptor or to a nearby site Lecture 2B - Pharmacodynamics Receptors (binding) • initiate cellular response similar or identical to that of NT (AGONIST) Lecture 2B - Pharmacodynamics • binding to a nearby site which facilitates NT binding (AGONIST) • blocks normal NT binding site (ANTAGONIST) Receptor Proteins (types) • ion channel receptors • carrier proteins • G protein-coupled receptor • enzymes Ion Channel • central channel forms a “pore” • NT/drug causes opening of pore Ion Channel (GABAA receptor) Cl- Lecture 2B - Pharmacodynamics C Carrier Protein • transports small organic molecules (i.e. NTs) • active process • terminates NT actionl Carrier Protein (DA transporter) Carrier / Transport Protein Lecture 2B - Pharmacodynamics Carrier Protein (DA transporter) Lecture 2B - Pharmacodynamics G Protein-Coupled Receptor • found on the post-synaptic side • once activated induces the release of intracellular (G protein) • controls enzymatic activity on postsynaptic side Enzymes • regulate breakdown of NT’s • drug interaction may increase/decrease their activity • acetylcholine esterase: ACh (synaptic cleft) Lecture 2B - Pharmacodynamics • monoamine oxidase: NE/DA (presynaptic) AchE inhibitors block activity Lecture 2B - Pharmacodynamics Enzymes (cont’d) • AChE inhibitors prevent breakdown of NT • found in insecticides, “nerve gas” Lecture 2B - Pharm
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