Ligands Flashcards
Agonist
Has affinity and intrinsic activity
Mimic actions of endogenous compounds
Antagonists
Have affinity
No intrinsic activity
Block effect of agonist
Produces all of the effects of receptor
Maximal response
Full agonist
Full Agonist
Morphine
Isoproterenol
Produces some of the effects of the receptor; has a mixed agonist
and antagonist action
Partial Agonist
Full agonist + Partial Agonist
Partial Agonist becomes Antagonist
Ex. Morphine + Nalbuphine
Morphine is a full agonist to mu receptors while Nalbuphine is a partial agonist for same receptor, when taken together, result is reduction of analgesia
Partial Agonists
Nalbuphine
Tamoxifen
Buprenorphine
Varenecline
Partial Agonists
Nalbuphine
Tamoxifen
Buprenorphine
Varenicline
Ligand which produces an effect opposite to that of an agonist occupying the same receptor
Inverse Agonist
Inverse Agonist
Block constitutive activity
Ex. Beta-Carboline
Inhibit the actions of agonist
Antagonist
Produces opposite effects by binding to same or similar receptors
Pharmacologic or Receptor Antagonism
Act by interfering w/ binding of the endogenous ligand to the receptor as the agonist; Ionic Bond
Reversible, Competitive Antagonist
Atropine + Ach
Zafirlukast + Zileuton
Reversible, Competitive Antagonist
Acts by interacting w/ the non-ligand binding site of the receptor
Non-Competitive Antagonist