Receptor Theory Flashcards
What is a receptor
How do drugs interact with receptors
What’s a perfect drug
-small protein molecule on cell membranes that serve as targets for ligands
/they mimic , modify or block action of endogenous receptors
-binds to one receptor and consistently produces the desirable effect
List types of receptors
1 intracellular
2 seven transmembrane receptor
3 enzyme linked transmembrane receptor
4 transmembrane ion channel
Describe ligand gated ion channel and g-protein coupled receptor and what they do
- will produces or cease uptake of ions when bound to ligand to change membrane potential or ionic content within cell
- will phosphorylate proteins to produce secondary messengers
Describe enzyme linked receptors and intracellular and what they do
- protein and receptor phosphorylation
- found within cell and will phosphorylation of proteins and gene expression
Basis of naming receptors
1 principal endogenous agonist that activated
2 1st exogenous agonist found to activate receptor
What is SAR in receptor theory
/structure activity relationship
-structure of drug corresponds to structure to receptor
3 components needed for action by drugs
1 drugs reach receptor in optimal amounts to pass threshold
2 drug specific to matching receptors
3 specificity based on chemical nature of drug
What is affinity and Intrinsic activity
- ability of drug to form and subsequently maintain a complex with a receptor
- ability of drug to evoke response on combing with receptor
Types of drugs
1 agonist ( evoke response ) 2 anatagonist ( inhibit response )
List properties of drug action
1 selectivity
2 efficacy
3 potency
4 dose-response relationship
Describe drug dose relationship
draw the graph both
-as drug conc increases response increases but eventually levels out at high concentrations
Explain selectivity of drugs ( draw compare and contrast graphs )
-higher affinity drugs for certain receptors will aquire higher binding percentages at lower conc
What is potency
Describe high potency and explain dangers
-dose required to achieve required effect of given intensity as compared to standard reference
- low conc needed to achieve specific response
- can easily poison someone at lower conc changes
What is efficacy
- max response a drug can produce
- how much effect is needed