BMS 450 Lecture Notes - Agonist, Triumph Tr5, Dissociation Constant

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15 Jul 2014
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Ed50 concentration @ which 50% of population gets effect of drug (effective dose) Congeneric drug still different api, but binds the same site. Drug with lower ed50 greater potency higher affinity. Classification as useful, toxic &c. depends on affinity/effects that predominate. Td50 toxic dose at which 50% of population experiences toxic response. Drug a ed50 = 1 mg; td50 or ld50 = 2 mg; tr = 2. Drug b ed50 = 100 mg; td50 or ld50 = 500 mg; tr = 5. Drug a is more potent than drug b. Drug b is safer larger range of doses in which it is non-toxic. If tr = 1, at the dose that 50% of the population gets the benefit, 50% is dying. Aj clark mathematical relationship between drugs and receptor. Ka (constant of dissociation) = k2 k1 or ka (constant of association; affinity constant) = k1 k2. Kd concentration at which 50% receptors are occupied.

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