2- Flashcards
(28 cards)
what is the drug action ?
molecular changes produced by a drug when t bind its target
what are the two aspects of drug action ?
Potency and efficacy
site the six mechanism of drug action
receptor, enzyme, ion chnnel, transport system trans factor, nucleid acid
what are receptors
proteins prticipate in intracellular comm via chemical signal
can receptors be found in cytoplasm ?
yep
which properties of receptors ?
saturability , reversibilityy (weak intermolar forces, vnderwalls)
stereoselectivity (recpgnize only one isomers)
agonist specificity related drug brind well and dissimilar compounds should bind poorly
tw0 phases of receptor propeties ?
Recognition, tranduction (functionnal response).
subpart of receptor
ligand binding domain, effector domain ssecond messenger
how is called receptor PLUS CELLULAR TARGET PLUS INTERMEDIARY MOLECULE ?
RECEPTOR EFFECTRS SYSTEM OR SIGNAL TRANSDUCTION PATHWAY
What are cell surfae receptor ?
ion gated or metabotropic (g coupled or tyrosine kinase linked receptor)
what are nuclar receptor ?
hormone
what trigers ions channel ?
change in membrane potential or ionic concentration
what triggers protein phosphorilation ?
cellular effect
What triggrs g protein ?
2nd messenger CAMP and cellular effect
what type are nAchR, NMDA r, GABAA ?
ionotropoc
what are ownstream effect of tirosine kinase linked receptor ?
for receptor dimer and activate tyrosine linase that results in phosporilation of downstream target.
WHat receptors are NGF, PDGF, insulin ?
tyrsine linked receptrs
what is transcripton facotr ?
lingand binding domainDNA binding domain that mediates binding to specific sites on the genome for activate or inhibit transcritpion of the nearby gene.
hw to measure basic radioligand binding/affinity ?
{L} plus {R} egal LR plus LFREE(ligand qui accroche pas au recepteur)
how is measured LR
radioligand binding
how to discriminate bewteen specific and nonspecific binding ?
using radilabelled ligands: radiolabelled ligand has nochance to compete with the unlabelled ligand added in excess : bound activity = non specific + specific binding
or bound radioactivity 1st set of tubes - br 2d set of tubes = bound activity due to specific binding
whats pccupancy theory ?
effect of a drug is proportionnal to nbr of receptor that is occupied by th edrug and has its basis in the law of mass action. Max response occurs whrn all receptors anre bound.
diff type of agonist ?
full agonist, partial, inverse agonist, super agonist, endogenous agonist
what is intrinsic activity ?
drug ability to bind a receptor and elicit a functional responde ?