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BMS 242 Core Physiology and Pharmacology > Drug Affinity > Flashcards

Drug Affinity Flashcards

1
Q

What is a constant in drug receptor theory

A

affinity of drug for receptor

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2
Q

How can affinity of a drug be determined

A

ligand binding assays

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3
Q

What is affinity

A

how tightly the drug and receptor interact

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4
Q

What is the measurement of affinity

A

KD

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5
Q

When is KD measured

A

at equilibrium

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6
Q

Describe the relationship between KD and affinity

A

inverse relationship

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7
Q

Describe the affinity if the KD value is low

A

high affinity

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8
Q

What is KD

A

Concentration of drug required to occupy 50% of receptors

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9
Q

Why is the relationship between KD and affinity inverse

A

the better the drug is at binding the lower the conc to occupy receptors

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10
Q

What is the efficacy value for agonists

A

high

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11
Q

What type of drug has no response of efficacy

A

antagonists

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12
Q

What does efficacy govern

A

activation

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13
Q

What is EC50

A

effective concentration giving 50% of maximal response

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14
Q

What is the receptor reserve

A

spare receptors

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15
Q

What can efficacy of an agonist influence

A

size of response

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16
Q

What does ACh bind to (guinea-pig ileum)

A

GPCR muscarinic receptor

17
Q

What happens when ACh binds to GPRC muscarinic receptors (guinea-pig ileum)

A

Gq proteins activate, generate a second messenger

18
Q

What does the second messengers trigger (guinea-pig ileum)

A

rise in intracellular calcium

19
Q

What does the rise in intracellular calcium trigger (guinea-pig ileum)

A

activation of contractile machinery - contraction

20
Q

What is drug concentration to response curves plotted on

A

semi logarithmic scale

21
Q

What does the sigmoidal curve hill equation fit to

A

concentration response curve

22
Q

What value does the Hill slope tend to be

A

around 1

23
Q

When would you have two agonists bind at once

A

nicotinic receptors

24
Q

What does the hill slope value tend to be when two agonists bind

A

around 2

25
Q

Describe the relationship between drug potency and EC50

A

low EC50 values are more potent

26
Q

Describe the relationship between affinity and potency

A

as affinity increases potency increases

27
Q

What factors determine potency

A

affinity, efficacy and spare receptors

28
Q

What is the efficacy of partial agonists

A

partial agonists have an efficacy less than 1

29
Q

What is KD value the same as for partial agonists

A

KD=EC50

30
Q

What is the efficacy of full agonists

A

1

31
Q

What is the efficacy a measure of

A

a single agonist receptor complex’s ability to generate a response

32
Q

What properties determine the effect of a drug in a living system

A

specificity, affinity, efficacy

33
Q

What can vary between different tissues

A

EC50

BMS 242 Core Physiology and Pharmacology (13 decks)

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