Lecture 15- Pharmacodynamic receptor theory Flashcards
drug targets include
- Mainly GPCR
- Ion channels
- Kinases
- Few nuclear receptors
- Enzymes
drugs are
ligands for a receptor
how many GOCRs in man
800
- 400 olfactory receptors e.g. sigh and smell
- non-olfactory receptors
olfactory receptors are regulated by
light, odorants, hormones, NT and ions
what is critical in determining drug action
the concentration of drug moelcule around receptors
uM
10-6M
nM
10-9M
pM
10-12M
how many moles in a uM
100,000
most drugs bind to receptors in an
irreversible manner
drugs either act
as antagonists
as agonists
antagonists
block the binding of endogenous agonists
agonists
activate the receptor
to bind to a receptor (as an antagonist or agonist)
drug must have affinity
higher affinity= stronger binding
mode of action: antagonists
- goverened by affinity
- no intrinisc efficacy
intrinsic efficacy and antagonists
wont switch the receptor to active state