lecture 1 Flashcards
(17 cards)
non specific drugs
biological effect at relatively high concentrations
specific drugs
biological effect at relatively low concentrations. chemical and biological specifity
cytoplasmic signalling
polar molecules across membranes
cytoplasmic to membrane signalling
e.g. gasses and radicals
intramembrane signalling
e.g. hydrophobic molecules, lipids
the hill-langmuir equation
allows for the determination of the proportion of total receptor bound at any given concentration of a ligand.
potency
a lower concentration is needed to reach the EC50
efficacy
amount of effect reached. 100% efficacy=100% response.
reversible competitive antagonism
adding antagonist to solution decreases potency but 100% efficacy can still be reached
non-competitive antagonism
potency doesnt change, but efficacy goes down
irreversible competitive antagonism
no dissociation of antagonist, causes a change in potency and efficacy
kinetic subtype selectivity of antagonist
the affinity of a compound can differ depending on the receptor it is bound to
inverse agonist
pushes receptor towards resting state so no response will follow if an agonist binds
multiple receptor state model
the most frequent conformations depend on the agonists present
functional antagonism
target the opposite signalling pathway to inhibit the reaction by promoting the opposing reaction
non-receptor antagonists
chemical antagonism, can be neutralizing antibodies, antacids or chelators
receptor desensitization
prevents continuous firing of neurons. in beta cells: taking away receptors which will regenerate after a period of time