Pharmacology 2A

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What units is Kd given in?
Molar
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What shape is the shape of the graph for fractional occupancy against concentration?
Rectangular hyperbola
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What is Kd a measure of?
Affinity
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What is the symbol for the rate constant from the inactive to the active drug receptor complex
β
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What is intrinsic efficacy?
The number the drug displays to switch the drug molecule from inactive to active
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Which will always be bigger, Kd or EC50?
Kd
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Kd/EC50 gives a rough estimate for what?
Receptor reserve
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Propranolol is a....
Antihypertensive drug
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Adrenaline acts on....
β 1 receptors
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Haloperidol is a ....
Antipsychotic
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Haloperidol works on....
D2 receptors
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Ranitidine works on which receptor?
H2
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Which drug acts at alpha 1 receptors on the pupil to cause dilation?
Noradrenaline
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Acetylcholine causes constriction of the pupil by acting on which receptors?
Muscarinic
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What is the name for when a receptor cycles between inactive and active even without anything bound to it?
Constitutive activity
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How long roughly does a receptor last on the membrane?
4 hours
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What is the symbol for the hill coefficient
n
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What does L* indicate
The radioactivity of the ligand
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What does the Cheng Prusoff method allow you to estimate?
Ki
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What structure does the nicotinic acetylcholine receptor have?
Pentameric
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Which subunit does the acetylcholine bind to in the muscle nicotinic acetylcholine receptor?
Alpha
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Which ion flows the most through the muscle nicotinic acetylcholine receptor?
Sodium
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Which ion flows the most through the neuronal nicotinic acetylcholine receptor?
calcium
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What structure is the P2X receptor?
Trimeric
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Where do allosteric ligands bind on the GABAa receptor?
between the alpha and gamma sites
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What is neostigmine?
A cholinesterase inhibitor
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NO711 blocks the take of which transmitter?
GABA
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D-tubocurarine is a competitive antagonist at which receptor in the periphery?
nAChR
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How is choline generated?
Consumed in the diet
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Are the Muscarinic or the nicotinic AChR important in rest and digest?
Muscarinic
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Toxins from food poisoning can cause what as a result of binding presynaptically at the NMJ?
Tetanus
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Botulin toxin is used medically to relieve spasticity and to...
Decrease saliva production
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What is the name of the molecule that is required to take up acetate and choline presynaptically?
Hemicholium
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Other cards in this set

Card 2

Front

What shape is the shape of the graph for fractional occupancy against concentration?

Back

Rectangular hyperbola

Card 3

Front

What is Kd a measure of?

Back

Preview of the front of card 3

Card 4

Front

What is the symbol for the rate constant from the inactive to the active drug receptor complex

Back

Preview of the front of card 4

Card 5

Front

What is intrinsic efficacy?

Back

Preview of the front of card 5
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