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Receptor Theory Flashcards

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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
What is a heteroreceptor?
Receptor that regulates synthesis + release of chemical mediators other than its own ligand
26
What is an auto receptor?
Macromolecule typically found in nerve ending that regulates synthesis + release of own ligand
27
What is receptor-down regulation?
Agonist, induces a decrease in no. of receptors available for binding
28
What is receptor-up regulation?
Agonist, induces an increase in no. of receptors available for binding
29
What is affinity?
The ability of drug to bind to receptor
30
What happens if a ligand has low affinity?
High conc needed for biological response
31
What is efficacy?
Measure of max physiological response
32
What is potency?
Refers to dose of drug required to produce specific effect of given magnitude
33
What is potency dependent on?
Affinity + efficacy
34
What happens if it is more potent?
Effect at lower conc
35
What happens if less potent?
Effect at higher conc
36
What is the occupation theory? | Receptor theory
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
What is rate theory?
Pharmacological activity directly proportional to rate of dissociation + association, NOT no. of receptors occupied
38
What is the dissociation + association of an agonist?
BOTH fast
39
What is the dissociation + association of an antagonist?
Fast association | Slow dissociation
40
What is the dissociation + association of a partial agonist?
Intermediate association | Intermediate dissociation
41
What is the induced-fit theory?
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
How many types of macromolecular perturbation theory is there?
2
43
What is the first type of macromolecular perturbation theory?
Specific conformational perturbation = biological response (agonist)
44
What is the second type of macromolecular perturbation theory?
Non-specific conformational perturbation = biological response (antagonist)
45
What is activation aggregation theory?
Drug receptor exists in eqm between activated state (bioactive) + inactive state (bio-inactive); agonist bind to activated state + antagonist to inactivated state
46
What is 2-state receptor model?
Receptor exists in resting + active state, presence of drug shifts eqm either way
47
What are chemotherapeutic drugs?
Used to cure diseases + cancer
48
What are examples of chemotherapeutic drugs?
Sulfa drugs + antibiotics
49
What are pharmacodynamic drugs?
Used in non-infectious diseases
50
What are examples of pharmacodynamic drugs?
Sedatives + hallucinogenic
51
What are examples of miscellaneous agents?
Narcotic analgesics + local anaesthetics
52
What are the different types of drug mechanisms?
``` Physical Chemical Drug-receptor interactions Drug-enzyme interactions Drug-channel interactions Miscellaneous ```
53
What is a physical mechanism?
Drug does NOT produce chemical reaction or change in cells of body
54
What is a chemical mechanism?
Drug acts by producing chemical reaction
55
What is drug-receptor interaction mechanism?
Act on cell membrane + builds complex
56
What is a ligand?
Substances that bind to receptors
57
What is an example of a ligand?
Acetyl choline
58
What is an agonist?
Drugs that bind to receptors = activate receptors
59
What happens after response increases till peak?
Response decreases even though agonist still bound
60
What happens once response decreases after peak is met?
Produces relaxation of skeletal muscles by: Activation of nicotine receptors Desensitization of receptors in neuromuscular junction
61
What are drug-enzyme interaction mechanisms?
Same as drug-receptor just enzymes instead | Competitive + non-competitive
62
What are drug-channel interaction mechanisms?
Same as drug-receptor just involves channels | eg. Na+, K+, Ca2+ + Cl- channels
63
What are miscellaneous mechanisms?
Drugs don't act through any mechanism already mentioned
64
Describe non-specific interactions
Drugs act by physical means outside cell External surfaces of skin + GI tract Outside of cell = chemical interactions
65
What is primary effect?
Desired therapeutic effect
66
What is secondary effect?
All other effects beside therapeutic - beneficial or harmful
67
What is local effect?
When drug effect occurs immediate vicinity of application
68
What is systemic effect?
When drug effect occurs away from site of administration
69
What are the two modes of action?
Killing foreign organisms | Stimulation + depression
70
What is killing foreign organisms? | Mode of action
Chemotherapeutic agents kill bacteria, worms + viruses
71
What is stimulation + depression? | Mode of action
Drugs act stimulating or depressing normal physiological functions Stimulation = increases rate of activity Depression = decreases
72
What is the action of drugs?
Biochemical physiological mechanisms by which the chemical produces a response in living organisms

Pharmacology (40 decks)

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