You
What lowers the DRC to 0%
Inverse agonist
An Allosteric agonist is also known as what
Positive allosteric modulators (PAMs)
Which antagonist has the greatest affinity
Irreversible antagonist
What are some regulations of receptors
Synthesis and degradation
Covalent modification
Association with other regulatory proteins
Re-localization within the cell
What is the difference between the ED50 and LD50
The ED50 is the dose of the drug that gives the desired drug response to 50% of the population
The LD50 is the dose of the drug that kills 50% of the population
What has the highest affinity for the receptors in the inactive state and has negative efficacy
Inverse agonist
An allosteric antagonist is also known as what
Negative allosteric modulators (NAMs)
What can Irreversible antagonists do that is noticeable on the DRC graph
Up-regulation happens when
Chronic reduction of receptor stimulation (antagonist)
How to you calculate the Therapeutic index
LD50/ED50
What do antagonists do
Interfere with the interaction of an agonist and a receptor
Binds reversibly to the receptor
The agonist cannot overcome the antagonist which will cause asymmetrical shifts
What are the effects of spare receptors in tissues with a lot of receptors
Be more sensitive to an agonist
Be less sensitive to antagonist
Respond to a non-competitive or irreversible antagonist as if it were competitive (initially)
Down regulation happens when
Chronic exposure of receptor to a stimuli
How do you calculate the safety index
LD01/ED99
What are important about competitive antagonists
Most common in clinical practice. agonist and antagonist compete for the same receptor site
Do competitive antagonists evoke a change in the receptor
NO
What are the effects of spare receptors in tissues with few of receptors
Be less sensitive to an agonist
Be more sensitive to antagonist
Emax drops faster in response to a non-competitive
What are 4 examples of Long-term downregulation
Binding to coated pits
Recycling
Degradation
Do you want your safety index to be big or small
Big
What is important about orthosteric antagonists
Bind irreversibly and cannot be overcome by an increase concentration of agonist
What happens to the DRC of an agonist in the presence of an antagonist
If you increase the concentration of the antagonist, you will need to increase the dose of the agonist to overcome the antagonist
What are indirect antagonists
They are antagonists that inhibit the generation of a biological response by acting at some point down stream of the receptor. It can be reversible or irreversible and an example of this is cancer drugs
What is the Therapeutic index
Estimates the drug margin of safety
Ratio of therapeutic effect to toxic effect
Toxic effect is an example of undesired effect
Undesired actions of drugs are commonly called side effects
What can Myasthenia Gravis cause due to what
It is muscular weakness and it is the antibody that is directed towards nicotinic receptor at neuromuscular junction