NEU 365D Lecture Notes - Lecture 10: Reaction Rate Constant, Dissociation Constant, Drug Action
Document Summary
Efficacy - the ability to produce its desired effect. Drug action - binding to specific receptors on target cells. Receptors - identified 1960"s - binding assays w/ radioactively-labeled. Specific - if leads to an effect on the cell or organism. Most receptors are proteins: bind mostly endogenous ligands (i. e. neurotransmitters) Nonspecific binding site - any body component that a drug binds to without leading to an effect. Interact with different proteins, lipids, carbs, other chemicals few elicit an effect. No control to what the radioactive substrate would bind to. Determine specific binding to receptors vs other things. Concentration required to go from a threshold saturating effect: ~ 100x. Most drugs bind reversibly to their receptor. Electrostatic forces, hydrogen bonds and van der waals forces. Drug and receptor must show complementarity in their binding groups (small changes can markedly affect its ability to bind to its receptor) Stereoselective - preference for one optical isomer of a drug.
