Receptors are the most common drug target
Ionotropic receptors (ligand gated ion channels) v quick
G protein coupled receptors quick
Kinase liked receptors medium
Nuclear receptions (steroids and hormonal) long as well
Drug binding and reception
Occupation vs activation
Occupation is defined by the affinity of a drug
Activation is defined by efficacy of a drug
Agonism
Bring a response in tissue, can be full or partial, the full terminology is being phased out for high agonist
Inverse agonism
They negatively affect action of a receptor
Antagonism
These bind and do nothing but block other
Noncompetitive and competitive
Competitive bind to the same site as a the agonist and the noncompetitive binds to another site and allosterically affects the binding site
Reversible and irreversible
Reversible competitor doesnt covalently bond to the active site and can therefore be reversed
Irreversible takes enzymes out of the equation
Specificity
We want drugs that dont cause massive side effects and are quite specific to the intended receptor
Also most fda approved drugs have nanomolar affinities and high potency
Long exposure to drugs can bring about tolerance and resistance