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This lecture covers the quantitative description of ligand-receptor binding, including equilibrium binding, association/dissociation kinetics, and concentration-effect relationships. It explores agonists, antagonists, and allosteric modulators, such as benzodiazepines, affecting receptor responsiveness. The lecture delves into the mechanisms of GABAA receptor modulators and the pharmacology of nicotinic acetylcholine receptors. It discusses competitive and non-competitive inhibition, binding/activation stoichiometry, and the variability of drug responses. Additionally, it explains desensitization, tachyphylaxis, and factors influencing drug response, like receptor internalization and altered drug metabolism.