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Systems Pharmacology
Principles of Drug Action/Intro to Receptor Pharmacology
17
Biology
Graduate
11/08/2011

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Term
regulatory protein targets
Definition
-enzymes
-ion channel proteins
-receptor proteins
-transporters
Term
non-specific interactions
Definition
-pH
-osmolarity
-surfactant (decreases ST)
-protein denaturation
-alter membrane fluidity
-selective toxicity
Term
bonds usually involved in drug-receptor binding
Definition
hydrogen bonding
Term
bonds NOT usually involved in drug receptor binding
Definition
covalent
Term
receptor definition
Definition
-bind specifically
-receive/process extracellular signals
-role in intracellular communication via chemical messengers
-change activity of intracellular enzymes
Term
cell biologist classification of receptors
Definition
-enzyme ligand
-ligand-gated ion channels
-G-protein coupled
-nuclear receptors
Term
John Langley
Definition
-1900s
-isolated muscle fibers
-2 compounds competing for a third unknown substrate
Term
Paul Ehrlich
Definition
-1st to use term "receptor"
-microbiologist
-stereoselectivity
-lock and key
Term
binding properties of receptors
Definition
-Drug specificity
-Reversibility
-Stereoselectivity
-Saturability
-Tissue Specificity
Term
ligand
Definition
-chemicals that bind to receptors
Term
affinity
Definition
-how well a ligand binds to a receptor
-nothing to do with what effect the ligand has
Term
efficacy
Definition
measure of the effect produced after a ligand binds
Term
potency
Definition
a ligand is potent if it produces an effect at a low concentration
Term
determines binding in the body
Definition
ADME
Term
determines binding in a dish of cells
Definition
-specificity
-solubility
-stability
Term
purpose of radioactive saturation bind study
Definition
-determine affinity and number of receptors
Term
Kd
Definition
-dissociation constant
-measure of affinity (inversely)
-concentration of drug where 50% of receptors are complexed with drug
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