Receptor Theory Flashcards
What are examples of some drug targets?
Receptors
Enzymes
Carrier molecules
Ion channels
What is a receptor?
Target molecule through which soluble physiological mediators produce their effect
What is required for drug receptor interactions?
Specific chemical structure required
What are kinetic experiments in binding studies?
Where the binding of one or more concs of radioligand is measured at an incrementing series of time points
What are saturation experiments in binding studies?
Where binding of an increasing series of concs of radioligand L
What are competition/modulation experiments in binding studies?
Where the binding of one or more fixed concs of a radioligand is measured at eqm in presence of an incrementing series of cons of a non-labelled compound
What is an agonist?
A substance that interacts with the receptor, + elicits observable biological response. Can be endogenous or exogenous substance
What happens as agonist conc increases?
Response increases
What is ED50?
Effective dose = indicates how much drug is required
What is a partial agonist?
Acts on same receptor as agonists, BUT, regardless of the dose it cannot produce same max biological response as full agonist
What happens to partial agonist as drug conc increases?
Response of agonist increases
What are inverse (negative) agonists?
Acts on same receptor of agonist yet produces an inverse effect
What happens to inverse agonist as drug conc increases?
Response decreases
What is a spare receptor?
Max responses elicited at less than max response occupancy. Receptors which exist in less of those required to produce full effect
What is intrinsic activity?
Value that refers to the ability of complex to produce a response
What is an antagonist?
Inhibits the effect of an agonist BUT has no effect of its own. May compete on the same receptor site that the agonist couples, or may act on allosteric site
What are the different type of antagonists?
Competitive
Non-competitive
Allosteric
Physiological
What is a competitive antagonist?
Binds to same site as agonist in reversible manner
What is a non-competitive antagonist?
Binds to same site as agonist irreversibly
What is an allosteric antagonist?
Antagonist + agonist bind to different site on same receptor
What is a physiological antagonist?
2 drugs have opposite effects through different mechanisms
What does a competitive antagonist do to the curve?
Shift to right
What does a non-competitive antagonist do to the curve?
Shift to right + down
What does a allosteric antagonist do to the curve?
Shift to right
What is a heteroreceptor?
Receptor that regulates synthesis + release of chemical mediators other than its own ligand
What is an auto receptor?
Macromolecule typically found in nerve ending that regulates synthesis + release of own ligand
What is receptor-down regulation?
Agonist, induces a decrease in no. of receptors available for binding
What is receptor-up regulation?
Agonist, induces an increase in no. of receptors available for binding