Receptors I Flashcards
What drug type creates a response in the cell
agonist
What is occupation of a drug-receptor governed by?
Affinity
What is activation of a drug-receptor governed by?
efficacy
What part of a drug receptor reaction is reversible
occupation forming a complex
What is the ratio of reversibility of a drug receptor reaction governed by?
affinity of the drug
Describe the reversibility of drugs with high affinities
slow reversibility
Describe occupancy
proportion of receptors occupied will vary with the drug concentration
What does occupancy vary between
0 and 1
How much drug is present at 0 occupancy
none
How can we measure occupancy
by measuring response
Describe the relationship between occupancy and response
high occupancy means there is a large response
Can you measure antagonists activity using occupancy
NO
Examples of ligands
neurotransmitters, hormones, growth factors, cytokines, drugs, toxins
Examples of protein targets
receptors, ion channels, enzymes, transporters
Describe a ligand binding practical
tissue prep with radio-ligand, incubation, filtration, rinse, count, data analysis
True or False - most ligands bind non-specifically to tissue, filter paper, glass
TRUE
How can non-specific ligand binding be reduced
reduced by anti-absorbants
What are some examples of anti-absorbants
albumin, collagen, o-catechol
What is the function of rinsing in a ligand binding practical
remove unbound radioligand from incubation medium
What is a key measurement in receptor ligand assays
specific and non specific binding