receptor pharmacology Flashcards

1
Q

what is the law of mass action

A

the more drug you add the more response you get

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2
Q

what underpins the ability of the drug to be attracted to the receptor

A

affinity

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3
Q

what does an agonist cause

A

a change in the receptor to give a response (efficacy)

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4
Q

what does potency mean

A

a measure of the concept of affinity

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5
Q

is there multiple receptors for the same endogenous agonist

A

yes

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6
Q

what receptors does histamine have

A

H1 and H2

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7
Q

what adrenoceptors are there

A

A1 and A2
B1, B2 and B3

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8
Q

what muscarinic receptors are there

A

M1-5

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9
Q

do receptors of the same family have any differences

A

yes they have structural differences in the site where the agonist binds

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10
Q

what does alpha adrenoceptors control

A
  • vasoconstriction
  • dilation of pupil
  • contraction of uterus and ureters
  • relaxation of intestinal movements
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11
Q

effects of beta adrenoceptors

A
  • vasodilation
  • stimulation of heart
  • relaxation of uterus
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12
Q

is efficacy linked to potency

A

no

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13
Q

what is efficacy based on

A

the ability of the agonist to produce a conformational change in the receptor

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14
Q

what is a full agonist

A

an agonist with good efficacy

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15
Q

what is a partial agonist

A

an agonist that doesn’t reach the same levels as a full agonist

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16
Q

what do antagonists do

A

block binding of the agonist to the receptor

17
Q

what do allosteric modulators do

A

they bind to the allosteric site, can be negative (NAM) or positive (PAM)

18
Q

why would allosteric modulators be good drugs for future medicines

A
  • lots of variation in allosteric sites (easier to make a selective modulator)
  • modulators don’t tend to block receptor completely (less severe side effects)
19
Q

what is inverse agonism

A

when a drug binds to the receptor and makes it less active