Pharmacology lecture 3 0.0 / 5 ? BiologyDrug interactionsUniversityNone Created by: willmiddlehamCreated on: 27-03-15 13:05 What does a graded dose response relationship show? A response of a particular system 1 of 14 What does a quantal dose response relationship show? The drug dose required to produce a specified response determined in each member of a population 2 of 14 What does a dose-response curve allow you to estimate? 1) Emax 2) Concentration or dose required to produce 50% of maximal response - EC50 3 of 14 What does a dose-response curve allow you to determine? And define them. 1) Efficacy - ability to produce a desired response 2) Potency - amount required to produce a max effect 4 of 14 Kd = (definition) concentration of ligand at which 50% of available receptors are occupied(equilibrium dissociation constant) 5 of 14 Kd = (formula) Kd = K-1/K1 6 of 14 Affinity = (formula) Affinity = K1/K-1 7 of 14 A LOWER Kd indicates.... a tighter ligand-receptor interaction (HIGHER AFFINITY) 8 of 14 A LOWER EC50 value.... the GREATER the POTENCY 9 of 14 FULL agonist High efficacy - produce MAX response while occupy small % of receptors 10 of 14 PARTIAL agonist Low efficacy - unable to produce a max response even when occupying all available receptors 11 of 14 Tachyphylaxis Desensitisation of receptors 12 of 14 What do positive allosteric modulators do? Not active alone but INCREASE affinity and/or efficacy of endogenous agonist 13 of 14 What do negative allosteric modulators do? Not active alone but DECREASE affinity and/or efficacy of endogenous agonists 14 of 14
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