How do drugs work through receptors

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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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