Drug Receptor Theory Flashcards
Drug receptor theory
Out of the internet
Receptor theory is essential to understanding drug action and states that drugs act as agonists, antagonists, or inverse agonists of physiologic receptors and thus can only mimic, intensify, inhibit, or block normal physiologic responses.
Physiological receptors
Receptors that serve for the endogenous ligands for physiological functions
Drug affinity measure
Dissociation constant [strength of the reversible interaction between a range it’s receptor. ]
Agonists mimic physiological ligands
Primary agonist- primary r orthosteric site/ allosteric - different region/ block or reduce the action of agonist are antagonists [ allosteric, chemical,functional], partial agonists regard less of the concentration, inverse agonist.
Inverse agonists
- Regulates the receptors that exhibit action despite the absenceof a ligand
Receptor occupancy theory
Laws of mass action is the basis for the law of mass action
Efficacy
The ability of a drug to activated receptor generate a cellular response is a reflection of its efficacy
Historical quantification of efficacy
A proportionality constant that quantifies the extent of functional change impacted to a receptor-mediated response system on binding a drug
Relative apparent dissociation constant
Kapp- a macroscopic equilibrium constant that reflects the ligand binding equilibrium and the subsequent equilibrium results formats in the on of the active receptor LR
In viva (0) drug life-cycle
O- distribute to specific targets o receptor, 1-bind to receptor, 12. Promote/block- activation of receptor-mediated physiological effects. 4. Termination of effect.
Receptors - functional mediators