PSYC 3030 Lecture Notes - Lecture 3: G Protein–Coupled Receptor, Competitive Inhibition, Hypoventilation

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3: drug binding: silent receptors (depot binding) Albumin (natural carrier of free fatty acids in plasma) Drugs cannot reach active sites or be metabolized. Reversible, drug can be released by the receptor at a later time. Ex) neurotransmitter, hormone, drugs are ligands: receptors. First site of action of a biologically active agent. Cell surface receptor, signal is transduced in a different way, nothing physically moves across the cell) receptors. In the cytoplasm (such as glucocorticoids) or in the nucleus (such as sex hormones) Ionotropic (ion channel coupled with receptor) and metabotropic (g protein coupled. Drugs here have to be lipid soluble (like hormones) Down-regulation due to an increase in a substance. A competitive inhibitor can fit the receptor site, but will have no action or effect. Ligand affinity: how well it fits to the site of the receptor. Ligand efficacy: the ability of the ligand to alter the 3d structure of the receptor and initiate intracellular changes (agonist vs. antagonist)

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