Drug receptor interactions Flashcards
How many of the top drugs on the market target G-protein coupled receptors?
34 of top 100
What is an agonist drug?
drug that binds to a receptor and elicits a biological process
What is an antagonist drug?
Drug that blocks the action of an agonist compound: commonly binding to a receptor without eliciting a biological response
What is a partial agonist drug?
An agonist drug that produces a biological effect but never the maximal of which the tissue is capable-posses antagonist properties
What is an inverse agonist drug?
Agonist that produces an opposing biological response to that observed by a full agonist
What is affinity?
Ability of a drug molecule to bind to a receptor site
What is efficacy?
Ability of a drug to elicit a biological response from a drug receptor interaction
What is occupation governed by?
Affinity
What is activation governed by?
Efficacy
How do most agonists bind to receptors?
Reversibly
Why do most agonist bind reversibly?
Relatively weak attractions such as Hydrogen bonding, ionic bonding and van der waal’s forces between the receptor and agonist, therefore easy dissociation
How do some agonist bind to receptors in rare cases?
Irreversibly
Why do agonist rarely bind irreversibly?
Interactions between receptor and agonist are by stable strong bonds such as covalent bonds. These are relatively strong therefore have poor dissociation
What is the B-max?
Maximum amount of receptors the drug can bind to
What is the Kd?
Amount of drug needed to occupy half the number of maximum receptor