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PATHO > Lecture 3: Response, Potency and Efficacy > Flashcards

Lecture 3: Response, Potency and Efficacy Flashcards

1
Q

Agonist

A

-bind to receptor site
-enhanced cellular activity
-induced fit that activates receptor

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2
Q

Antagonist

A

-binds to and blocks receptor site
-blocks natural chemical from binding to receptor
-induced fit that does NOT activate receptor

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3
Q

Potency

A

-dose of drug required to produce particular effect of given intensity
-comparison based on doses that produce SAME effect (usually ED50)
-may be overrated

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4
Q

High potency

A

entire curve shifted left towards lower x values

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5
Q

low potency

A

entire curve shifted right to higher x values

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6
Q

Efficacy

A

-response resulting from DR interaction
-limited by toxicity
-more important than potency

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7
Q

Strong agonist

A

high affinity and high efficacy

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8
Q

Higher efficacy

A

curve reaches closer to 100%
-higher y value

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9
Q

lower efficacy

A

lower y value

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10
Q

Partial Agonist

A

-produce reduced response even at full occupancy
-cannot produce same maximal effect as full agonist
-may competitively inhibit response to full agonist
-related to drug binding. to inactive form of receptor

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11
Q

Partial agonist examples

A

-aripiprazole, D2
-buprenorphine, mu opiate
-buspirone, 5-HT1A

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12
Q

partial agonist structural basis

A

resembles a shape between agonist and antagonist

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13
Q

Partial Agonist theory

A
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14
Q

Level of response

A

full agonist > partial agonist > inactive compound > inverse agonist

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15
Q

Heroin Methadone example

A

-Buprehorphine (partial agonist) binds all receptors and provides about half effect of heroin as treatment for opiod addiction = nowhere for heroin to bind so no withdrawal
-Naloxone (antagonist) blocks all receptors but with no effect = no euphoria = withdrawal

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16
Q

Full agonist structure

A

-fits neatly
-loop c closes in

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17
Q

Partial agonist structure

A

-a bit bigger, sticks out
-loop c can close but not all the way

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18
Q

Antagonist structure

A

-bigger, sticks out of receptor
-loop c cannot close

19
Q

Inactive to active form

A

Lecture 4 recording

20
Q

As partial agonist concentration increases

A

more occupancy of receptors
-undos full agonist binding?? idk

21
Q

as full agonist concentration increases

A

less occupancy of receptors

22
Q

Increase partial concentration

A

decrease overall response

23
Q

Assumption: adding enough partial agonist or antagonist

A

displaces full agonist

24
Q
A
25
Q

Inverse agonist

A

-requires constitutive activity (otherwise it’s just an antagonist)
-opposite response of agonist
-inactivates receptor?
-full or partial
-response can be altered by agonist, partial agonist, antagonist (shared binding site)
-stabilize inactive form of receptor
-ex: rimonobant (acomplia)-CB1 receptors

26
Q

Inactive receptor + agonist

A

conformational change of receptor and interaction with G proteins

27
Q

active conformation of receptor w/o agonist + inverse agonist

A

inactive receptor
no interaction with G proteins

28
Q

Rimonobant (acomplia)

A

-inverse agonist
-binds to cannaboid (CB1)receptors
-reduced hunger, increased anxiety
-oops she never made it to the market

29
Q

activation of CB1 receptors

A

-THC bind
-decreased anxiety, hunger, relaxation

30
Q

constitutive activity

A

REQUIRED for inverse agonists
-active form of receptor

31
Q

constitutive activity absent

A

same as antagonist

32
Q

constitutive activity present

A

-inverse agonist lower than antagonist curve
-backward s curve

33
Q

Endogenous agonist present

A

silent antagonist has backward s curve

34
Q

endogenous agonist. absent

A

silent antagonist straight line

35
Q

constitiutive absent, endogenous agonist absent

A

no effect from either
-straight horizontal line on top

36
Q

constitutive activity, NO endogenous agonist

A

-silent antagonist no effect
-inverse agonist has effect

37
Q

NO constitutive activity, endogenous agonist present

A

-both have same effect

38
Q

Constitutive activity and endogenous agonist present

A

-both have effect
-inverse agonist has better effect

39
Q

Receptor Antagonism

A

-DR interaction that interfres with or prevents the development of drug response by agonist
-competitive, noncompetitive, irreversible

40
Q

Competitive Antagonism

A

-competing for active site
-reversible by increasing dose
-increase concentration shifts curve right

41
Q

Log dose-response curve of AGONIST in presence of competitive antagonist

A

-shifts right
-reduction in effective potency of agonist
-need more agonist

42
Q

Schild plot

A

-ability to calculate KD of ligand to generate P2 value

43
Q

Binding affinity generally correlates with

A

the potency of antagonists

44
Q
A

PATHO (31 decks)

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