Flashcards in Affinity, Agonist/Antagonists and Potency Deck (25):
What bonds allow for irreversible reactions?
What are the three non-covalent bonds?
Ionic bonds, hydrogen bonds and van der waals forces.
What % of targets do low affinity drugs target?
What % of targets do high affinity drugs target?
How can you increase the affinity of a low affinity drug?
By increasing the concentration.
Give the three methods of measuring concentration?
Radio ligand binding assay, competition binding and enzymes.
Define the term Kd?
The concentration of the drug which is required to occupy 50% of the receptors.
What does Bmax stand for?
Define the term agonist?
A drug which causes a biological response upon binding to its target.
Define the term antagonist?
A drug that causes no effect and can be used to block and agonist.
In terms of enzymes define an agonists and an antagonist?
Substrate and inhibitor.
In the somatic NS what are the agonists and antagonists for a nicotinic receptor?
Acetylcholine and neostigmine
In the sympathetic NS what are the receptors used for noradrenaline?
Nicotinic acetylcholine and a and ß receptors
What is antagonist that can not be overcome?
An insurmountable antagonist.
What can partial agonists act as to full agonists?
What % maximum response do full agonists have?
What is a competitive surmountable antagonist?
An antagonist which can be overcome with the use of more agonist (reversible).
In the parasympathetic NS what receptor is used for acetylcholine and hexamethonum?
Muscat ionic acetylcholine
What does EC50 tell you?
About the potency. It is the concentration that produces 50% maximum binding.
Does a lower or higher concentration give a lower potency?
Give an examples of an alpha receptor?
What isoprenaline potency do alpha receptors have?
Give an example of ß receptors?
Heart and lungs
What are the two ways to measure response?
Signalling assays and isolated tissue.