L6- Receptor Pharmacology Flashcards
(16 cards)
Agonist
Have affinity and efficacy
Antagonist
Affinity no efficacy
Can receptor activation have an inhibitory response
Yes
Full agonist
100% response
Partial agonist
50% response
Neutral antagonist
0% response
Inverse agonist
-50% response
Chemical antagonism
One drug antagonises the action of another by chemically combining with it
Pharmacological antagonism
When drugs counteract each other by acting on the same receptor type
Physiological antagonism
When 2 drugs counteract each other by producing opposing effects on different receptors
Effect of Increased agonist conc on response in regards to competitive antagonism
Restore response
Cause of irreversible competitive antagonism
Covalent bonding
Can agonists and antagonist have the same effect
Yes - depending on receptor location
What does physiological response depend on
Ion permeability- GABA causes hyper polarisation (cl- ion)
G protein coupled receptors
A signalling pathway which is activated depending on G protein coupling. Has 7 transmembrane domains
Importance of GPCRs and examples of drugs
Involved in numerous physiological responses and a target for over half of all prescribed medicines. Eg hyoscine- Mach receptor antagonist
Promethasine-H1 receptor antagonist