Receptor pharmacology Flashcards
what are the 4 major types of intracellular signalling?
ligand gated ion channels
G-protein coupled receptors
Kinase linked receptors
Nuclear receptors
what is a partial agonist?
activates the receptor but not to its maximum capacity
what is an inverse agonist?
a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist
-makes receptor less active
what is affinity measured by?
potency
what is the law of mass action?
the more drug you add the more response you get
what do you want a high therapeutic index in a drug
so there is a therapeutic window
what is efficacy?
the ability of the agonist to produce a response
- causes conformational change
-causes cellular response
-is not linked to potency
does antagonists have efficacy?
no because they block the binding of the agonist
what are non-competitive antagonists?
bind at an allosteric modulator
can be positive or negative
why are allosteric modulators good for drugs for future medicine ?
lots of variation in allosteric sites
less severe side effects
what is pharmacological efficacy?
how good the agonist works in terms of size and response
what is clinical efficacy?
how well it works in the clinic/clinical trials
what is the difference between vaccine efficacy and effectiveness?
efficacy - refers to how the vaccine performs in ideal conditions (controlled clinical trials)
effectiveness - refers to how the vaccine performs in a wider population
what is the biggest class of receptors in the body?
GPCRs
