receptor theory and class of drug acion Flashcards

1
Q

4 main regulatory proteins

A

receptors
enzymes
carrier molecules
ion channels

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2
Q

main receptor classes

A

intreacell receptor
enzyme-linked receptors
G-protein coupled receptors
ligand-gated ion channel

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3
Q

how many attachement is need of a drug to a receptor site is required

A

3

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4
Q

3 different binding studies

A
  • kinetic
  • saturation
  • competiton/modulation
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5
Q

radioreceptor assay:

A

measure binding of drugs to receptors

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6
Q

agonist

A

interact with specific cell constituents

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7
Q

ED50

A

effective dose to make 50% max response

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8
Q

partial agonists

A

act on same receptor as agonists but can not produce same biological response

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9
Q

inverse agonists

A

act on same receptors as agonist but inverse effect

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10
Q

spare receptor

A

max responses are elicited at less than max receptor occupancy

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11
Q

intrinsic activity

A

ability of agonist to activate receptor as compared to maximally active compound in series being studied

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12
Q

antagonist

A

inhibits effect of agonist but 0 biological activity of its own may compete on the same receptor site that agonist occupies or may act on allosteric site

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13
Q

different antagonists

A

competitive
noncomp
allosteric
physiological

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14
Q

what does occupation theory say

A

drugs act on independent binding site and activate to make a biological response

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15
Q

Rate theory:

A

response proportional to rate of drug-receptor complex formation

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16
Q

heteroreceptor

A

regulates the release of chemical mediators other than its own ligand

17
Q

autoreceptor

A

found in nerve ending that regulates synth and release of own ligand

18
Q

receptor down regulation

A

agonist induces a decrease in number of receptors available for binding

19
Q

receptor up regulation

A

agonist induces increases in number f these receptors available for binding

20
Q

affinity is propertional to

A

Kd

21
Q

macromolecular perturbation theory

A
  • aseptic conformational perubation leads to biological response
  • nonspec conformational pertubation leads to 0 biological response
22
Q

activation-aggregation theory

A

suggests drug receptor still exists in equilibrium between activated state and in activated state

23
Q

2 state receptor models are developed on basis of

A

competitive and allosteric inhibition

24
Q

agonists have high affinity for

A

R* state

25
Q

class of drugs

A

chemotherapeutic agents
pharmacodynamic agents
miscellaneuos agents

26
Q

drug action mechanism

A

physcial

chemical

27
Q

ligands are

A

endogenous

28
Q

agonists can produce

A

chain reaction