receptor theory and class of drug acion Flashcards
4 main regulatory proteins
receptors
enzymes
carrier molecules
ion channels
main receptor classes
intreacell receptor
enzyme-linked receptors
G-protein coupled receptors
ligand-gated ion channel
how many attachement is need of a drug to a receptor site is required
3
3 different binding studies
- kinetic
- saturation
- competiton/modulation
radioreceptor assay:
measure binding of drugs to receptors
agonist
interact with specific cell constituents
ED50
effective dose to make 50% max response
partial agonists
act on same receptor as agonists but can not produce same biological response
inverse agonists
act on same receptors as agonist but inverse effect
spare receptor
max responses are elicited at less than max receptor occupancy
intrinsic activity
ability of agonist to activate receptor as compared to maximally active compound in series being studied
antagonist
inhibits effect of agonist but 0 biological activity of its own may compete on the same receptor site that agonist occupies or may act on allosteric site
different antagonists
competitive
noncomp
allosteric
physiological
what does occupation theory say
drugs act on independent binding site and activate to make a biological response
Rate theory:
response proportional to rate of drug-receptor complex formation
heteroreceptor
regulates the release of chemical mediators other than its own ligand
autoreceptor
found in nerve ending that regulates synth and release of own ligand
receptor down regulation
agonist induces a decrease in number of receptors available for binding
receptor up regulation
agonist induces increases in number f these receptors available for binding
affinity is propertional to
Kd
macromolecular perturbation theory
- aseptic conformational perubation leads to biological response
- nonspec conformational pertubation leads to 0 biological response
activation-aggregation theory
suggests drug receptor still exists in equilibrium between activated state and in activated state
2 state receptor models are developed on basis of
competitive and allosteric inhibition
agonists have high affinity for
R* state
class of drugs
chemotherapeutic agents
pharmacodynamic agents
miscellaneuos agents
drug action mechanism
physcial
chemical
ligands are
endogenous
agonists can produce
chain reaction