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This lecture covers the mechanisms of action of drugs targeting ligand-gated ion channels and kinase-linked receptors, focusing on modulators of the GABAA receptor, benzodiazepines, and clinical uses. It also discusses the subunit composition of the GABAA receptor, subtype-specific roles, and testing drug-induced sedation, amnesia, and anticonvulsant activity. Furthermore, it explores the insulin receptor, physiological context of insulin, and therapeutic strategies for diabetes mellitus type 2, including insulin sensitizers and GLP-1-based therapies.