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any substance that causes a response by the body
Drug
scientific study of the effects of drugs on living organism
Pharmacology
means from inside of body
Endogenous
means from outside of body
Exogenous
molecules that bind to receptors
Ligand
drug that activates the receptor
Agonist
drug that inhibits or prevents receptor activation
Antagonist
receptors exist in a reversible equilibrium between inactive and active states
Active/inactive Receptor
concentration dependent toxic effects of drugs
Averse Effect
use of drugs in medicine
Pharmacotherapy
refers to drug receptor’s ability to bind to one target or molecule with greater affinity over another
Drug selectivity
way drug works on our bodies and tells us how a drug influences its target to elicit a biological response
mechanism of action
the magnitude of response is proportional to the number of drug-receptor complexes formed
Drug receptor complex and response
biochemical change in a cell produced when a drug interacts with a receptor; described as the receptor handling the signal to downstream parts of a cascade that produce the biological response
Signal transduction
where the alphas subunits bind GTP subunits dissociate and signal downstream effectors
G-protein coupled receptor
channels normally closes; ligand binding causes a conformational change that opens the channel and allows ions to flow, mediating rapid signaling
Ligand Gated Ion Channels
channels regulated by membrane potential; they permit ion flow in response to voltage changes
Voltage Gated Ion Channels
receptors located inside the cell; ligand must be membrane-permeable. Once activated they act on DNA to alter gene/protein expression’ effects are typically slow
Intracellular Receptor
receptor that when activated increase intracellular enzyme activity
Enzyme Linked Receptors
repeated or continuous agonist exposure leads to receptor modification
Desensitization
this exact term is not explicitly defined, refers to functional loss of receptor/channel activity
Inactivation
repeated agonist exposure leads to internalization or destruction of receptors, reducing receptor number on surface
Down regulation
repeated exposure to antagonist increases receptor number making cells more sensitive to agonist
Upregulation
one ligand-receptor interaction leads to multiple downstream signals
Signal amplification
systems where maximal response can be achieved without occupying all receptors (consequence of signal amplification)
spare receptors