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22 Cards in this Set
- Front
- Back
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what is the definition of receptor
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the component of a cell that interacts with a drug and initiates the chain of biochemical events leading to the drugs observed effects
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what is the function/importance of receptors
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1.)determines the relationship b/w the dose and effect
2.)is responsible for the drugs selectivity 3.) mediator b/w agonist and antagonists |
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what is pharmacodynamics?
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-"what the drug does to the body"
-the drugs mechanism of action |
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What are 3 types of surface receptors?
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Those linked to ion channels
Those lnked to enzymes Those linked to g protiens |
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How does an intracellular receptor work?
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Endogenous hormone binds to receptor in cytoplasm, then the complex moves to the nucleus to effect gene expression
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How does a receptor linked directly to ion channels work?
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Changes the membrane permeability
When bound to drug, receptor activates and opens pore |
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How do receptors linked directly to enzymes work
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There is an extracellular receptoor site and an intracellular enzymatic component. When activated the enzyme phosphorolates & can then break down something else
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How do receptors linked to regulatory protiens work?
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Receptor links to G protien to activate it. Then the G protien alters activity of an intracellular effector
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Are G protoens stimulatory ro inhibitory?
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Can be either
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What is affinity? How is it measure?
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The amount of attraction b/w drug and receptor
Measured by the amount of drug needed to bind to unoccupied receptors |
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What is an allosteric modulator?
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Something that binds to a receptor and changes the affinity of the receptor to the drug
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What does it mean for a drug to be 100% selective?
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It only goes to target tissue and has only the intended effect
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What does it mean for a drug to be non-selective?
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Drug is able to bind to other receptors and have side effects
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What is the receptors effect on dose-response?
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Response is somewhat proportional to # of receptors bound (within a given drug concentration)
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What is a full agonist?
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Binds to a receptor & causes maximal functional response
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What is a partial agonist?
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Binds to receptor but does not cause full response
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What is an antagonist?
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Binds to receptor but does not cause a response
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What is a competitive antagonist?
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Where the agonist has an equal opportunity to bind to the receptor
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What is a noncompetitive antagonist?
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Where agonist is unable to compete
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What is a mixed agonist antagonist drug
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Acts as an agonist on some receptors and antagonist on others
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What is an inverse agonist?
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Drug that binds to a receptor and has the opposite effect as agonist
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How is it dertermined which is the agonist and which is the inverse agonist?
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The agonist is more closely related to an endogenous chemical
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