W8 - Efficacy and partial agonists Flashcards

1
Q

What is efficacy

A

ability of a drug to activate a receptor and cause a response

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2
Q

what is the measurement of binding

A

affinity

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3
Q

what is the measurement of effect

A

efficacy

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4
Q

what is emax

A

maximum response that an agonist can achieve

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5
Q

what is ec50

A

concentration of agonist required to produce 50% of the emax potency

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6
Q

what is the equation for fractional occupancy

A

ligand/ligand + kd

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7
Q

what is kd

A

dissociation constant and is a measure of affinity

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8
Q

how can we tell the difference between a full agonist and a partial agonist on a crc

A

full agonist will have a fractional response of one

partial agonist has fractional response of <1

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9
Q

how do we order efficacy

A

we use emax

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10
Q

how do we order potency

A

we use ec50

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11
Q

in cases where partial agonists provide the maximal response what has this meant

A

stimulus from drug receptor must be amplified to give the response

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12
Q

what does the stimulus in amplification rely upon

A

occupancy of receptors by drug

intrinsic efficacy of drug

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13
Q

is the statement that the response is not directly proportional true or false

A

true

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14
Q

what are reserve receptors

A

a proportion of receptors in a tissue are never used, these are reserve receptors

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15
Q

what doe the existence of reserve receptors mean

A

Signal amplification must occur i.e. The tissue contributes to the effect and begins to explain tissue specificity

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16
Q

what does the response generated during signal amplification in reserve receptors rely upon

A

transduction
receptor number

affinity
intrinsic efficacy

17
Q

what is an inverse agonist

A

it is an agonist that produces opposite response to the agonist

18
Q

What happens when agonist added to equilibrium

A

shifts to right

19
Q

what happens when inverse agonist added

A

shifts to left

20
Q

describe the two state receptor theory

A

receptor have different state inthe state of equillibrium

receptors have intrinsi activity