Receptor Theory Flashcards

1
Q

What are examples of some drug targets?

A

Receptors
Enzymes
Carrier molecules
Ion channels

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2
Q

What is a receptor?

A

Target molecule through which soluble physiological mediators produce their effect

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3
Q

What is required for drug receptor interactions?

A

Specific chemical structure required

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4
Q

What are kinetic experiments in binding studies?

A

Where the binding of one or more concs of radioligand is measured at an incrementing series of time points

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5
Q

What are saturation experiments in binding studies?

A

Where binding of an increasing series of concs of radioligand L

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6
Q

What are competition/modulation experiments in binding studies?

A

Where the binding of one or more fixed concs of a radioligand is measured at eqm in presence of an incrementing series of cons of a non-labelled compound

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7
Q

What is an agonist?

A

A substance that interacts with the receptor, + elicits observable biological response. Can be endogenous or exogenous substance

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8
Q

What happens as agonist conc increases?

A

Response increases

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9
Q

What is ED50?

A

Effective dose = indicates how much drug is required

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10
Q

What is a partial agonist?

A

Acts on same receptor as agonists, BUT, regardless of the dose it cannot produce same max biological response as full agonist

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11
Q

What happens to partial agonist as drug conc increases?

A

Response of agonist increases

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12
Q

What are inverse (negative) agonists?

A

Acts on same receptor of agonist yet produces an inverse effect

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13
Q

What happens to inverse agonist as drug conc increases?

A

Response decreases

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14
Q

What is a spare receptor?

A

Max responses elicited at less than max response occupancy. Receptors which exist in less of those required to produce full effect

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15
Q

What is intrinsic activity?

A

Value that refers to the ability of complex to produce a response

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16
Q

What is an antagonist?

A

Inhibits the effect of an agonist BUT has no effect of its own. May compete on the same receptor site that the agonist couples, or may act on allosteric site

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17
Q

What are the different type of antagonists?

A

Competitive
Non-competitive
Allosteric
Physiological

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18
Q

What is a competitive antagonist?

A

Binds to same site as agonist in reversible manner

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19
Q

What is a non-competitive antagonist?

A

Binds to same site as agonist irreversibly

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20
Q

What is an allosteric antagonist?

A

Antagonist + agonist bind to different site on same receptor

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21
Q

What is a physiological antagonist?

A

2 drugs have opposite effects through different mechanisms

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22
Q

What does a competitive antagonist do to the curve?

A

Shift to right

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23
Q

What does a non-competitive antagonist do to the curve?

A

Shift to right + down

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24
Q

What does a allosteric antagonist do to the curve?

A

Shift to right

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25
Q

What is a heteroreceptor?

A

Receptor that regulates synthesis + release of chemical mediators other than its own ligand

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26
Q

What is an auto receptor?

A

Macromolecule typically found in nerve ending that regulates synthesis + release of own ligand

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27
Q

What is receptor-down regulation?

A

Agonist, induces a decrease in no. of receptors available for binding

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28
Q

What is receptor-up regulation?

A

Agonist, induces an increase in no. of receptors available for binding

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29
Q

What is affinity?

A

The ability of drug to bind to receptor

30
Q

What happens if a ligand has low affinity?

A

High conc needed for biological response

31
Q

What is efficacy?

A

Measure of max physiological response

32
Q

What is potency?

A

Refers to dose of drug required to produce specific effect of given magnitude

33
Q

What is potency dependent on?

A

Affinity + efficacy

34
Q

What happens if it is more potent?

A

Effect at lower conc

35
Q

What happens if less potent?

A

Effect at higher conc

36
Q

What is the occupation theory?

Receptor theory

A

Drugs act on independent binding sites + activate them = biological response proportional to amount of drug-receptor complex formed
Response stops = complex dissociation
Drug effect directly proportional to no. of receptors occupied

37
Q

What is rate theory?

A

Pharmacological activity directly proportional to rate of dissociation + association, NOT no. of receptors occupied

38
Q

What is the dissociation + association of an agonist?

A

BOTH fast

39
Q

What is the dissociation + association of an antagonist?

A

Fast association

Slow dissociation

40
Q

What is the dissociation + association of a partial agonist?

A

Intermediate association

Intermediate dissociation

41
Q

What is the induced-fit theory?

A

As drug approaches receptor, receptor alters conformation of its binding site to produce drug-receptor complex. Binding produce mutual plastic moulding of both ligand + receptor

42
Q

How many types of macromolecular perturbation theory is there?

A

2

43
Q

What is the first type of macromolecular perturbation theory?

A

Specific conformational perturbation = biological response (agonist)

44
Q

What is the second type of macromolecular perturbation theory?

A

Non-specific conformational perturbation = biological response (antagonist)

45
Q

What is activation aggregation theory?

A

Drug receptor exists in eqm between activated state (bioactive) + inactive state (bio-inactive); agonist bind to activated state + antagonist to inactivated state

46
Q

What is 2-state receptor model?

A

Receptor exists in resting + active state, presence of drug shifts eqm either way

47
Q

What are chemotherapeutic drugs?

A

Used to cure diseases + cancer

48
Q

What are examples of chemotherapeutic drugs?

A

Sulfa drugs + antibiotics

49
Q

What are pharmacodynamic drugs?

A

Used in non-infectious diseases

50
Q

What are examples of pharmacodynamic drugs?

A

Sedatives + hallucinogenic

51
Q

What are examples of miscellaneous agents?

A

Narcotic analgesics + local anaesthetics

52
Q

What are the different types of drug mechanisms?

A
Physical
Chemical 
Drug-receptor interactions
Drug-enzyme interactions
Drug-channel interactions
Miscellaneous
53
Q

What is a physical mechanism?

A

Drug does NOT produce chemical reaction or change in cells of body

54
Q

What is a chemical mechanism?

A

Drug acts by producing chemical reaction

55
Q

What is drug-receptor interaction mechanism?

A

Act on cell membrane + builds complex

56
Q

What is a ligand?

A

Substances that bind to receptors

57
Q

What is an example of a ligand?

A

Acetyl choline

58
Q

What is an agonist?

A

Drugs that bind to receptors = activate receptors

59
Q

What happens after response increases till peak?

A

Response decreases even though agonist still bound

60
Q

What happens once response decreases after peak is met?

A

Produces relaxation of skeletal muscles by:
Activation of nicotine receptors
Desensitization of receptors in neuromuscular junction

61
Q

What are drug-enzyme interaction mechanisms?

A

Same as drug-receptor just enzymes instead

Competitive + non-competitive

62
Q

What are drug-channel interaction mechanisms?

A

Same as drug-receptor just involves channels

eg. Na+, K+, Ca2+ + Cl- channels

63
Q

What are miscellaneous mechanisms?

A

Drugs don’t act through any mechanism already mentioned

64
Q

Describe non-specific interactions

A

Drugs act by physical means outside cell
External surfaces of skin + GI tract
Outside of cell = chemical interactions

65
Q

What is primary effect?

A

Desired therapeutic effect

66
Q

What is secondary effect?

A

All other effects beside therapeutic - beneficial or harmful

67
Q

What is local effect?

A

When drug effect occurs immediate vicinity of application

68
Q

What is systemic effect?

A

When drug effect occurs away from site of administration

69
Q

What are the two modes of action?

A

Killing foreign organisms

Stimulation + depression

70
Q

What is killing foreign organisms?

Mode of action

A

Chemotherapeutic agents kill bacteria, worms + viruses

71
Q

What is stimulation + depression?

Mode of action

A

Drugs act stimulating or depressing normal physiological functions
Stimulation = increases rate of activity
Depression = decreases

72
Q

What is the action of drugs?

A

Biochemical physiological mechanisms by which the chemical produces a response in living organisms