allosteric activation - correct answer-the active site becomes available to the substrates
when a regulatory molecule binds to a different site on the enzyme
you get a confirmational change distal to the ligand binding site which is allosteric activation
now because it has changed its shape something within the cell can bind to it
alpha receptors bind to either IP3 or cAMP - what does this lead to? - correct answer-smooth
muscle contraction
competitive (reversible) antagonist - correct answer-the antagonist is competing with the
agonist and it is reversible - this means that they have equal affinities for the receptor
because if one had an advantage or higher Ka it would not be competitive it would just take
the receptor site
ED50 - correct answer-the dose that produces a response equal to half of the maximum
response
Efficacy - correct answer-the maximum response that a drug is capable of achieving
(this is where the drug plateaus on the curve
Enantiomers - correct answer-isomers that are mirror images of each other
Epi and NE have greater affinity for which adrenoceptors? - correct answer-epi - binds to all
four but greater affinity for beta
NE - binds to alpha 1, alpha 2, and beta 1 but greater affinity for alpha
full agonist - correct answer-Ability of a drug to produce 100% of the maximum response
regardless of the potency
Functions of the PNS - correct answer-rest and digest
-slows heart rate
-increases gastric secretions
-empties bladder and bowel
-focuses eye for near vision
-constricts pupil
-constricts bronchi
, Functions of the SNS - correct answer-fight or flight
-increases heart rate
-increases blood pressure
-shunts blood from skin and viscera to skeletal muscles
-dilated bronchi
-mobilizes energy stores
GABA - correct answer-a major inhibitory neurotransmitter
ligand gated ion channel - chloride
pulls cell further away from threshold and need more to be stimulated
Glutamate - correct answer-A major excitatory neurotransmitter; involved in memory
binds to sodium and calcium
binds to GPCR
graded response - correct answer-when we express the response on the y axis as an
absolute value
-numbers that can assume values across a scale
How can competitive antagonists be overcome? - correct answer-by increasing the dose of
the agonist
If you compare the LDR curve for the agonist alone and the agonist plus the competitive
reversible antagonist the curve is shifted to the right and is parallel which means you can still
achieve the same magnitude of effect but you need more dose
How do you calculate therapeutic index? - correct answer-TI = TD50/ED50
irreversible antagonist - correct answer-Affinity is so high that receptor is unavailable to bind
agonist. Duration of action independent of rate of elimination and more dependent on rate of
turnover of receptor molecules
binds to receptors with a covalent bond which can't be broken will be bound to that receptor
site for the life of the cell
Is it better to have a high or low therapeutic index? - correct answer-High
Ka - correct answer-Ka is the volume needed to get one mole of unbound drug when 50% of
the receptors are occupied
Kd - correct answer-Kd is the concentration of drug in the plasma when 50% of the receptors
are occupied
Muscarinic agonist - correct answer-think PNS
-peeing, wheezing, pooping, drooling
would give for muscle retention or glaucoma
Muscarinic antagonist - correct answer-atropine for example
binds to muscarinic - think PNS
indicated for bradycardia, pupil dilation, GI hypermotility
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