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Cell Bio - Lucas > Modern Receptor Theory > Flashcards

Modern Receptor Theory Flashcards

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
Q

kOFF

A

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]

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26
Q

kD

A

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].

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27
Q

kA

A

The reciprocal of kD, measures the affinity of receptors for the signalling molecule. kON / kOFF = [S.R.] / [S] [R].

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28
Q

Neurotransmitters kOFF, kON, kD, kA

A

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

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29
Q

Hormones kOFF, kON, kD, kA

A

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
Q

Affinity

A

A measure of molecule activity. The ability of a molecule to bind to receptors.

31
Q

Stickability

A

Chari’s term for affinity.

32
Q

Efficacy

A

A measure of molecule activity. The ability of a molecule to produce a response.

33
Q

Doability

A

Chari’s word for efficacy

34
Q

Concentration Response Curve

A

Graphically demonstrates the potency and efficacy of a drug

35
Q

CRC

A

Concentration Response Curve

36
Q

Dose Response Curve

A

Graphically demonstrates the potency and efficacy of a drug.

37
Q

DRP

A

Dose response curve

38
Q

Occupation Theory

A

Same as occupancy model

39
Q

Stochastic

A

Random, non-deterministic, no pattern.

40
Q

Agonist

A

A molecule that binds to a receptor and elicits a response

41
Q

Antagonist

A

Binds to a receptor, does not elicit a response and prevents the agonist from functioning.

42
Q

Pharmacological Antagonism.

A

Refers to antagonism on a single receptor

43
Q

Agonism

A

Occupation of the receptor by an agonist that leads to a response.

44
Q

Antagonism

A

Occupation by an antagonist interferes with the response of the agonist.

45
Q

Competitive Antagonist

A

Causes a shift of potency (to the right.)

46
Q

Irreversible Antagonist

A

Causes a shift of efficacy (shift down) Changes max output.

47
Q

Log

A

Dose-response curve generally increases by these increments on the x axis (measuring dosages)

48
Q

Competitive antagonist

A

Antagonist and agonist compete for the same spot on a receptor

49
Q

Non-competitive antagonist

A

Antagonist binds so agonist can no longer bind and produce an effect.

50
Q

Surmountable

A

Competitive antagonist

51
Q

Nonsurmountable

A

Non-competitive

52
Q

Irreversible

A

Non-competitive

53
Q

Reversible

A

Competitive

54
Q

Physiological antagonism

A

Two receptors, two different agonists

55
Q

Partial agonism

A

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
Q

Full Agonism

A

With all receptors occupied, the full response is seen. Due to the fact that the agonist binds only to the active confirmations

57
Q

Spare Agonism

A

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
Q

Signoidal

A

The type of curve generated by a DR curve

59
Q

Invariantly

A

In a matter that is without variation; consistent

60
Q

Tau

A

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
Q

Fudge Factor

A

a term to describe how Tau solves the complexity of efficacy

62
Q

Stickability

63
Q

Doability

64
Q

Vexing

A

causing annoyance, frustration, or worry

65
Q

Induce

A

bring about or give rise to

66
Q

Conformational Induction

A

a change on the shape of a macromolecule, often induced by environmental factors

67
Q

Conformations

A

the many potential structures of proteins

68
Q

Constitutive Activity

A

even under basal conditions, some conformations are coupled to intracellular processes

69
Q

Baseline Activity

A

the response of the tissue with no ligand present. Not zero but slightly above because of constitutive activity.

70
Q

Basal

A

Baseline activity

Cell Bio - Lucas (5 decks)

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