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Patho > Set 2 > Flashcards

Set 2 Flashcards

1
Q

binding of an agonist results in an induced fit that

A

activates the receptor

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2
Q

binding of an antagonist results in an induced fit that

A

does not activate the receptor

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3
Q

where do agonists and antagonists bind

A

at the top

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4
Q

antagonists engage __ of the receptor and bind ___ and engage ___ ____

A

more, higher, other parts

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5
Q

silent antagonists have

A

no effect

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6
Q

potency def

A

the dose of a drug required to produce a particular effect of given intensity

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7
Q

on a graph high potency

A

is to the left with the same shape

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8
Q

higher EC50 means ___ potency

A

lower

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9
Q

efficacy

A

the biological response resulting from the drug receptor interaction

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10
Q

T/F a strong agonist has high affinity and high efficacy

A

True

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11
Q

T/F Efficacy is more important than potency as a drug property

A

True

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12
Q

10^-4, 10^-5, 10^-6

A

100, 10 1 micromolar

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13
Q

10^-7, 10^-8, 10^-9

A

100, 10, 1 nanomolar

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14
Q

partial agonist

A

produced a reduced response even at full recepter occupancy

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15
Q

T/F partial agonists can sometimes close or can’t

A

True

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16
Q

what are the effects of partial agonist on binding on a binding graph

A

full agonist decrease and partial agonists increase

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17
Q

effects of a partial agonist on functional response on a response graph

A

decreases total response to the same umber that partial agonist increase to

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18
Q

inverse agonists

A

opp of agonist and inhibits production

19
Q

T/F inverse agonists require constitutive activity

A

True

20
Q

what are the three types of receptor antagonists

A

competitive, noncompetitive, irreversible

21
Q

competitive antagonism

A

reversible, competing for same site for agonist

22
Q

T/F competitive antagonism can re reversed by increasing the dose of the agonist

A

True

23
Q

on a graph competitive antagonism looks like

A

an s that increases to the right and the shape stays the same

24
Q

noncompetitive antagonist

A

produces its effect at a site of the receptor other than the site used by agonist (allosteric)

25
Q

T/F the agonist and antagonist compete for a single binding site

A

FALSE they do not compete

26
Q

T/F noncompetitive cannot be completely reversed by increasing the agonist

A

True

27
Q

on a graph noncompetitive looks like

A

smaller bmax and higher EC50 the shape shifts down

28
Q

maximal response is often still possible because of

A

spare receptors

29
Q

irreversible antagonists

A

bind to same site as agonist(orthosteric) and not readily displaced

30
Q

irreversible antagonist form what kind of bond

A

covalent

31
Q

T/F if irreversible antagonist leaves then the inhibition still happens

A

True

32
Q

once spare receptors are all occupied what happens on the graph

A

the Emax lowers

33
Q

which of the following is not true regarding spare receptors
A. it is system/tissue dependent
B. allow a noncompetitive antagonist to look like a competitive antagonist
C. spare receptors are independent of effector numbers
D. may differ between signaling pathways with the same receptor

A

C

34
Q

Which of the following is not true regarding antagonist
A. irreversible and allosteric antagonists have similar effects on the dose response curves of agonists
B. in the absence if spare receptors, a noncompetitive antagonist increases the Emax
C. irreversible antagonists typically bind the orthosteric site
D. antagonist affinity can be estimated using a Schild plot

A

B

35
Q

functional antagonism

A

two drugs influence a physiological system but in opposite direction

36
Q

chemical antagonism

A

a chemical reaction occurs between an agonist and an antagonist to form an inactive product

37
Q

what are the allosteric ligands

A

positive allosteric modulators (PAMs)
negative allosteric modulators (NAMs)

38
Q

positive allosteric modulators- ____ Emax and potency

A

increase

39
Q

NAMs on a graph looks like

A

noncom inhib so the Emax lowers

40
Q

PAMs on a graph looks like

A

com inhib the curve stays the same and moves to the left

41
Q

neutral allosteric ligands

A

bind to allosteric site and prevents PAMs and NAMs from binding

42
Q

NAMs ___ binding of GABA to own receptor

A

decrease

43
Q

which of the following statements about allosteric ligands is false
A. allosteric modulators bind at sites unique from the agonist
B. NAMs are noncom
C. PAMs are safer than orthosteric agonists
D. there are no FDA-approved allosteric modulators
E. allosteric modulators would also regulate inverse agonist

A

D

Patho (11 decks)

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