Drug targets Flashcards
occupation
is governed by affinity
activation
is governed efficacy
Drug a (agonist) >
Response
drug b ( antagonist)
no response
at equilibrium
the ratio is constant and KD is constant
potency
indicates the dilution at which the drug will cause an effect
how to calculate potency
1/EC50
specificity/selectivity
action at the desired site vs action at an off-target site (propranolol vs atenolol)
how to calculate selectivity
potency @ site a (desired) / potency @ site b (undesired)
Drug targets ( mediators of normal functions)
receptors
ion channels
enzymes
carrier molecules
re-uptake inhibitors
inhibit uptake of neurotransmitters from the synaptic cleft- build up of monoamines- dopamine/serotonin/noradrenalin