BIO200H5 Lecture Notes - Lecture 6: Dissociation Constant, Dynamic Equilibrium, Caffeine

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22 Sep 2017
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Drugs bind to the same target as endogenous ligands. Allosteric drug = binds to alternative pocket (~far away) allow more of the drug to bind. We never compete with ligand for allosteric drug - we could open the pocket and. We could also close the pocket and prevent binding to reduce activity. Enhances (allosteric agonist) or inhibits target activity (allosteric antagonist) Gaba = inhibitory neurotransmitter; decreases neuronal activity. Receptor = ligand-gated ion channel; opens = increased chloride influx. Valium = sleep aid; gaba receptor opens longer. Gaba binds, ion channels open and ions flow in - when allosteric agonist. When an allosteric antagonist inhibits target then the channels close and binds, it enhances the actions of the inhibitor potential effect - increase neural activity. Inverse agonist decreases activity of the ligands. Allosteric activators bind and allosteric inhibitors inhibit their designated spot. Drug occupancy of receptors + pharmacological response = coupling. Ligand = molecules that bind to other molecules.

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