How do drugs work through receptors
1
2
3
Quantitation
Drug interaction with site
Activation
Antagonism
Comp
non-comp
Binding
Affinity
Agonism
efficacy
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Shape
Alprenolol-B2-adrenoceptor antagonist
Attractive forces
1/d
balance strength and range
Mass Action
The rate of a chemical reaction is proportional to the concentrations of the reactants
drug (A) >>>>>>>>#receptor (R)
rate = product * constant
Fractional receptor occupancy
[AR]/[R}t
=0.5 when A= KA
Occupancy ~= response
EC50
Potency
Structure-activity relationships
Efficacy
Drug-dependent
high affinity
high efficacy
Tissue-dependent
Lots of receptors
Efficient S-R coupling
Antagonism
Chemical
Competition
Surmountable
Dose-related
Competitive
non-competitive
receptor
Allosteric
not receptor
Pathway inhibitors
functional (physiological) antagonists
Partial agonism
Buprenorphine
initial treatment for opiate dependency
Salbutamol
B2-adrenoceptor selective partial agonist
Pindolol
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