cellular receptors and drug action Flashcards
if a receptor is inside the cell, what kind of endogenous ligand is it going to have
it means that the endogenous liagnd is fat soluble, this is because the fat soluble can pass the inside of the cell
intracellular receptor
inside the cell, the endogenous ligand is very small and fat soluble
intracellular receptors directly effect what
our DNA
spanning enzymes
insulin - the receptor is located inside the membrane
receptor located on a ion channel
binds to receptor, ion channel opens, causing an influx of molecules
g-protien coupled receptors
they stimulate effectors to produce intracellular changes
what g-protiens subgroups exist
gs, gi, gq
what receptors interact with g protiens
light, odorants, hormones, neurotransmitters, and prostaglandins
what effectors are associated with the cAMP signal transduction pathway
adenylyl cyclase
what are gs and gi always affecting
adenylyl cyclase
what happens when adenylyl cyclase is activated
it turns ATP into AMP then CAMP
phospholipase C
only associated with gq
phospholipase C is associated with what signal transduction pathway
phsophatidylinositol
PIP yields how many messangers?
2 - IP3 and DAG
what is IP3 and DAG - what changes do they lead to
these are secondary messangers in the cell that lead to physiological changes
what 2nd messengers come from the cAMP signal transduction pathway
cAMP
what is the endogenous ligand for the muscarinic receptor
potassium
how does heart rate slow down through the signal transduction pathway
acetylcholine binds to muscarinic receptor, g protien is stimulated, potassium channel opens slowing heart rate
gs protien and activation of protien kinases
gs stimulates adenylyl cyclase, coverts to atp,Camp activates protien kinases
how do protien kinases activate enzymes
by adding a phosphate group
what effector is associated with gs
adenylyl cyclase
what does gi protien do
inhibits adenylyl cyclase, leads to a decrease in cAMP
albuterol and gs protien
adenylyl cyclase - increase in cAMP - activation of enzymes, Ca+2, inactivate MLCK, decreased levels of these cause the bronchial relaxation
what decreases levels of ca and MLCK
increase in cAMP
what process is this? adenylyl cyclase - increase in cAMP - activation of enzymes, Ca+2, inactivate MLCK, decreased levels of these cause the bronchial relaxation
albuterol (bronchiodialator)
adenylyl cyclase increases what levels
cyclic AMP
name for ventalin
salbutamol/albutterol
misprosol is linked with what receptor
gi
gi and misoprostal peptic ulcers
Gi binds, inhibit acetylyl cyclase, cAMP production decreases, protien kinases are not activated, enzyme pumps that help produce sotmach acid are blocked, stomach acid decreased
what drug also causes uterine contraction
misprostoal
GQ linked to phospholipase C
PLC links to PIP, PIP yields two messangers (IP3 and DAG) IP3 binds to the SR, binding of CA, DAG binds to calcium channels on cell membrane, calcium into cell
what process is this? PLC links to PIP, PIP yields two messangers (IP3 and DAG) IP3 binds to the SR, binding of CA, DAG binds to calcium channels on cell membrane, calcium into cell
gq and phospholipase c
DAG binds to what?
binds to calcium channels on the cell membrane facilitating the movement of extracellular calcium into the cell
what does IP3 bind to?
binds to the SR, stimulating the release of Ca+2 into the cytoplasm
ergonovine and Gq protien
binds to gq protiens, stimualtes IP3 DAG, release of Ca, induces contraction of the uterus and blood vessels
what can ergonovine and gq protiens help with
can help to terminate postpartum hemorrhage
