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PDA > Receptors 3 > Flashcards

Receptors 3 Flashcards

1
Q

affinity

A

tells us how well the drug interacts with the receptor

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2
Q

Specificity

A

how selective is a drug binding to one type of receptor but not to other types of receptors?

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3
Q

efficacy

A

tells us how effective a drug is at producing a particular receptor response

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4
Q

Potency

A

tells us how much of the drug is required to produce an effect

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5
Q

agonist

A

drug that activates receptor

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6
Q

Antagonist

A

a drug that blocks a neurotransmitter to bind to receptor

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7
Q

how can affinity be measured?

A

can be measured using a binding assay. This is a direct measure of the physical interaction between a drug and a receptor

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8
Q

A drug may bind to many biological targets, those with high affinity is called?

A

specific binding

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9
Q

A drug may bind to many biological targets, those with lower affinity is called?

A

nonspecific binding.

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10
Q

How does nonspecific binding increase?

A

it will increase with high concentration of radioligand

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11
Q

How do you find specific binding?

A

subtract non-specific binding from total binding to find specific binding

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12
Q

what is Kd?

A

equilibrium dissociation constant

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13
Q

How do you find Kd? (equation)

A

tendency of RD complex to dissociate / tendency of R & D to form RD complex

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14
Q

What is the releation between Kd and RD?

A

the smaller Kd the less likely RD to dissociate, the higher the affinity of D for R

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15
Q

Kd on a curve means what?

A

drug concentration when 50% of receptors bound with the drug

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16
Q

the smaller the Kd value = ?

A

higher affinity for receptor

17
Q

what is EC50 ?

A

the concentration of a drug that produces 50% of maximal response

18
Q

Efficacy reflects what?

A

the upper limit (maximal response) achieved by a drug on the dose response curve

19
Q

Potency is inversely correlated to what?

A

EC50

20
Q

in regards to potency and EC50 relationship, Higher Potency =?

A

smaller EC50 concentrations

21
Q

when agonist binds to a receptor and activates signaling, how does that shift equilibrium?

A

it shifts equilibrium towards the active state

22
Q

When antagonist binds to the receptors but does not activate signaling, how does that change the equilibrium?

A

does not change the equilibrium between active and inactive states of receptor, but it can prevent agonist binding.

23
Q

Inverse agonist

A

produces a response opposite of that induces by full agonists

24
Q

How does inverse agonist effect equilibrium when bound to receptor?

A

shifts equilibrium towards the inactive state

25
Q

Partial agonist

A

produces a lower response (even at full receptor occupancy), than do full agonists which produce maximal response

26
Q

What is chantix?

A

a nicotinic ACh receptor partial agonist

27
Q

nicotine

A

a full agonist on nicotinic ACh receptors

28
Q

For smoke cessation we do what?

A

replace a full agonist with a partial agonist

29
Q

Narcan is a what?

A

pure opioid receptor atntagonist

30
Q

What is Narcan used for?

A

treating opioid overdoese induced respiratory inhibition, CNS depression

31
Q

Forms of Narcan?

A

IM or intranasal.

32
Q

How fast is narcan active?

A

2-5 minutes

33
Q

How does Naloxone block drug effects?

A

Naloxone has a higher affinity for opioid receptors

34
Q

What type of antagonist is naloxone?

A

competitive antagonist

35
Q

noncompetitive inhibitor works how?

A

noncompetitive antagonist will bind to allosteric site making it more difficult for agonist to bind to active site. Or the binding of antagonist modifies receptor activity.

36
Q

Competetive antagonist increase _______ but do not change _________

A

increase EC50; max response not changed

37
Q

in noncompetitive antagonist ______ will be reduced and _________ may or may not be changed

A

max response; EC50

PDA (6 decks)

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