Lecture 15- Pharmacodynamic receptor theory Flashcards
(43 cards)
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

mode of action of agonists
have both affinity and intrinsic efficacy

ligands bind tor eceptor due to
affinity
- both antagonists and agonists
intrinsic efficacy means that
ligand activates rthe recpetor and causes a response inside the cell
pharmacology efficacy
if drug causes blood vessel to dilate
clinical efficacy
if the drug actually lowes BP
lock and key analogy of antaognists and agonists
both bind due to affinity
Agonists- cause activation of receptor and repsosne inside cell (intrinsic efficacy)
Antagonists- have affinity but do not have intirnsic efficacy (block response of effector)
two ways the effect of drug concnenreation can be looked at
1) binding to the receptor
2) functional response




