USMLE (Fach) / Pharmacology (Lektion)
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Receptor binding
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Competitive antagonist: Shifts curve right (↓ potency), no change in efficacy. Can be overcome by ↑ the concentration of agonist substrate.- Example: Diazepam (agonist) + flumazenil (competitive antagonist) on GABA receptor.
Noncompetitive antagonist: Shifts curve down (↓ efficacy). Cannot be overcome by ↑ agonist substrate concentration.- Example: Norepinephrine (agonist) + phenoxybenzamine (noncompetitive antagonist) on α-receptors.
Partial agonist: Acts at same site as full agonist, but with lower maximal effect (↓ efficacy). Potency is an independent variable.- Example: Morphine (full agonist) vs buprenorphine (partial agonist) at opioid μ-receptors.
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