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Cell Bio - Lucas > Modern Receptor Theory > Flashcards

Modern Receptor Theory Flashcards

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1
Q

Black-box Era

A

Time when the input was known and the output was observed but what happened between was unknown. Limited by technology.

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2
Q

Horace Davenport

A

An eminent gastric physiologist who wrote an essay to describe the use of the straw lever and smoked drum technique in teaching physiology to students.

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3
Q

Horace

A

Horace Davenport

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4
Q

Davenport

A

Horace Davenport

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5
Q

Straw Lever

A

Part of early technique to generate dose-response curve. (Similar to drinking straw)

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6
Q

Drum

A

Part of early technique to generate dose-response curve. (Moving drum used to record muscle contractions.)

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7
Q

Acetylcholine

A

A neurotransmitter used at neuromuscular junctions, triggering the firing of motor neurons.

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8
Q

AJ Clark

A

Demonstrated the earliest quantification of receptor action by stimulating isolated tissues in an organ bath with acetylcholine. Also created the occupancy model (quantification enters pharmacology)

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9
Q

ACh

A

Acetylcholine

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10
Q

Irving Langmuir

A

Developed the absorption isotherm while studying the absorption of gases on films. A physical chemist who got his doctorate under Nernst in Germany. Works in research labs at General Electro Co. In New York developing better electric bulbs.

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11
Q

Nernst

A

Need to figure out

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12
Q

Evaporate (Langmuir)

A

Molecules sticking to the free surface. (Double check)

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13
Q

Condensate (Langmuir)

A

Molecules being released from the free surface. (Double check)

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14
Q

Equilibrium (absorption isotherm)

A

The amount of diffusing towards the free surface is balanced by those tending to leave the surface.

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15
Q

Occupation Model

A

Can be described as empty chairs waiting. Developed by AJ Clark. The addition of quantification to pharmacology.

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16
Q

Equilibrium Law

A

Another term for the law of mass action

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17
Q

Law of Mass Action

A

[receptor] + [signalling molecule] <> [signal-receptor complex]. Rate of formation and dissociation equal.

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18
Q

Guldberg and Waage Law

A

Another name for Law of Mass Action

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19
Q

Guldberg

A

Part of name for Guldberg and Waage Law of Mass Action. Add more info about him.

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20
Q

Waage

A

Part of name for Guldberg and Waage Law of Mass Action. Add more info about him.

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21
Q

[receptor]

A

Includes both free and bound receptors.

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22
Q

Equilibrium (law of Mass action)

A

Occurs when the formation of new signal-receptor complexes equals the rate at which existing signal-receptor complexes dissociate.

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23
Q

LMA

A

Law of Mass Action

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24
Q

kON

A

the rate of formation of new signal receptor complexes. Think of as [S. R.]. An equilibrium constant - think of chemistry. The forward direction, only include products. So just [S.R.]

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25
kOFF
The rate at which molecules unbind from receptors. Think of as [S] [R]. An equilibrium constant. Think of chemistry. Reverse direction, only include products. So just [S] [R]
26
kD
The equilibrium dissociation constant: [ligand] needed to saturate half of the receptors. kOFF /kON = [S] [R] / [S.R.] You need a certain concentration of ligand to be able to saturate half of the receptors. This measures that. [R] includes bound and unbound receptors. With 50% occupied, [S.R.] will equal half of [R]. Half of the concentration of [S] will be lost to [S.R.]. Therefore 1/2*2 = 1 and kD = [S].
27
kA
The reciprocal of kD, measures the affinity of receptors for the signalling molecule. kON / kOFF = [S.R.] / [S] [R].
28
Neurotransmitters kOFF, kON, kD, kA
kOFF - fast reverse (dissociation) rate so high kON - present in huge concentrations so forward rate slower. low kD - need large concentration of ligand to achieve 50% effect so high kA - affinity is low because released in such high concentrations. Low
29
Hormones kOFF, kON, kD, kA
kOFF - bind to receptor for long time, slow dissociation (reverse), low kON - not present in large concentrations since has to travel long distances. Therefore forward rate very high. kD - not a lot of ligand needed to achieve 50% effect - low kA - affinity is high because not many ligands make it to the receptor - high
30
Affinity
A measure of molecule activity. The ability of a molecule to bind to receptors.
31
Stickability
Chari’s term for affinity.
32
Efficacy
A measure of molecule activity. The ability of a molecule to produce a response.
33
Doability
Chari’s word for efficacy
34
Concentration Response Curve
Graphically demonstrates the potency and efficacy of a drug
35
CRC
Concentration Response Curve
36
Dose Response Curve
Graphically demonstrates the potency and efficacy of a drug.
37
DRP
Dose response curve
38
Occupation Theory
Same as occupancy model
39
Stochastic
Random, non-deterministic, no pattern.
40
Agonist
A molecule that binds to a receptor and elicits a response
41
Antagonist
Binds to a receptor, does not elicit a response and prevents the agonist from functioning.
42
Pharmacological Antagonism.
Refers to antagonism on a single receptor
43
Agonism
Occupation of the receptor by an agonist that leads to a response.
44
Antagonism
Occupation by an antagonist interferes with the response of the agonist.
45
Competitive Antagonist
Causes a shift of potency (to the right.)
46
Irreversible Antagonist
Causes a shift of efficacy (shift down) Changes max output.
47
Log
Dose-response curve generally increases by these increments on the x axis (measuring dosages)
48
Competitive antagonist
Antagonist and agonist compete for the same spot on a receptor
49
Non-competitive antagonist
Antagonist binds so agonist can no longer bind and produce an effect.
50
Surmountable
Competitive antagonist
51
Nonsurmountable
Non-competitive
52
Irreversible
Non-competitive
53
Reversible
Competitive
54
Physiological antagonism
Two receptors, two different agonists
55
Partial agonism
Even with all of the receptors occupied, the full response is NOT seen. Simply due to the fact that the agonist binds to both the active and inactive conformations, although more so to the active.
56
Full Agonism
With all receptors occupied, the full response is seen. Due to the fact that the agonist binds only to the active confirmations
57
Spare Agonism
Even with a small fraction of receptors occupied; full response is seen. Possible explanation - the environment favours the active confirmation and induces this change so that even without ligand, effects are seen.
58
Signoidal
The type of curve generated by a DR curve
59
Invariantly
In a matter that is without variation; consistent
60
Tau
The transducer constant, a practical measure of efficacy. The inverse of the fraction of receptors that must be occupied by agonist to obtain the half-maximal response.
61
Fudge Factor
a term to describe how Tau solves the complexity of efficacy
62
Stickability
Affinity
63
Doability
Efficacy
64
Vexing
causing annoyance, frustration, or worry
65
Induce
bring about or give rise to
66
Conformational Induction
a change on the shape of a macromolecule, often induced by environmental factors
67
Conformations
the many potential structures of proteins
68
Constitutive Activity
even under basal conditions, some conformations are coupled to intracellular processes
69
Baseline Activity
the response of the tissue with no ligand present. Not zero but slightly above because of constitutive activity.
70
Basal
Baseline activity

Cell Bio - Lucas (5 decks)

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