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ESA2 > Membranes and Receptors > Flashcards

Membranes and Receptors Flashcards

0
Q

3 types of protein mobility.

A

Conformational change
Rotational
Lateral

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1
Q

4 types of phospholipid motion.

A

Flexion/Conformation
Rotation
Lateral Diffusion
Flip Flop

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2
Q

Restraints of protein mobility

A

Separate to fluid/cholesterol poor region
Association between proteins in membrane
Peripheral protein association (Aggregation, Tethering, Interaction with cells)

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3
Q

What is Black Film?

A

A container with a divide containing a small section of lipid bilayer.

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4
Q

Difference in Passive and Active transport in terms of ΔG.

A

Passive has -ΔG

Active has +ΔG

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5
Q

Define co transport.

A

1< type of ion or molecule transported on membrane transporter.

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6
Q

Define antiport.

A

2 or more ions transported in opposite directions across membrane.

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7
Q

Define Symport.

A

2 or more ions/molecules transported in same direction across membrane.

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8
Q

Average Na concentrations.

A 
Extra = 145 mM
Intra = 12mM
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9
Q

Average K concentration

A

Extra 4 mM

Intra 155 mM

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10
Q

Average Ca concentration.

A

Extra 1.5 mM

Intra 0.1μM

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11
Q

Average Cl concentration

A

Extra 123 mM

Intra 4.2 mM

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12
Q

Define membrane potential

A

Potential difference across a membrane in a cell

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13
Q

What is Nernst equation used for?

A

Finding Equilibrium Potential

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14
Q

What is conductance (g)?

A

Increases by increase in number of channels for that ion.

Increase in g moves membrane potential (Vm) toward equilibrium potential for that ion.

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15
Q

What is a voltage clamp?

A

Prevents change in membrane voltage in response to membrane current.

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16
Q

Define ARP

A

Absolute Refractory Period

All Na channels inactivated

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17
Q

Define RRP

A

Recovery of Na channels from inactivation.

Excitability returns to normal.

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18
Q

Give an example of a Complete Blocker of nAChR

A

Tubocurarine

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19
Q

Give an example of a Depolarisation Blocker of nAChR

A

Succinylcholine

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20
Q

What is capacitance in terms of current?

A

Ability to store charge

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21
Q

How is conductance calculated?

A

1/Resistance

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22
Q

Define paracrine cell signalling

A

Signalling between cells via local mediator

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23
Q

Define endocrine cell signalling

A

Signalling via hormone in the blood

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24
Q

Define synaptic signalling

A

Signalling by neurotransmitter

25
Q

Define receptor

A

Molecule that recognises a specific ligand or family of ligands and which brings about regulation of a cellular process

26
Q

Define ligand

A

Molecule which binds specifically to a receptor site

27
Q

What is the difference between agonist and antagonist?

A

Agonist activates receptor

Antagonist combines with receptor but with no activation

28
Q

Define phagocytosis

A

Internalisation of particulate matter.

29
Q

Define pinocytosis

A

Invagination of membrane to produce a vesicle

30
Q

Define endocytosis

A

Selective internalisation by specific cell surface receptors

31
Q

3 principles of signal transduction.

A

Diversity Specificity Amplification

32
Q

Define affinity

A

Ability of ligand to bind to target receptor

33
Q

Define intrinsic efficacy

A

Ability of ligand to activate cellular response

34
Q

Define Bmax

A

Maximum binding capacity (receptor number)

35
Q

Define Kd

A

Concentration of ligand needed for 50% receptor occupancy.

36
Q

Define EC50

A

Effective concentration needed to give 50% maximal response.

37
Q

Define Emax

A

Maximum cellular response

38
Q

What is potency?

A

Combination of both affinity, intrinsic efficacy and efficacy.

39
Q

What is the difference between intrinsic efficacy and efficacy?

A

Intrinsic efficacy is how well the ligand activates the receptor.
Efficacy is how well the activated receptor generates a cellular response.

40
Q

What is meant by spare receptors?

A

EC50<Kd.

Less than half the receptors must be occupied to generate 50% response.

41
Q

How do spare receptors affect potency?

A

Increased sensitivity at low concentrations therefore increased potency. Allows for variation in sensitivity.

42
Q

Define IC50

A

Concentration of antagonist giving 50% inhibition.

43
Q

What is KB?

A

Kd when antagonist is derived pharmacologically.

44
Q

Define pharmacokinetics

A

What the body does to the drug.

45
Q

Define oral bioavailability

A

Proportion of dose given orally that reaches systemic circulation unchanged.

46
Q

How is bioavailability expressed?

A

Amount or Rate

47
Q

Explain how bioavailability is measured by amount

A

Area under curve of blood drug level vs time.

48
Q

How is bioavailability measured by rate?

A

Measured by peak height and rate of rise of drug level in blood.

49
Q

What is the therapeutic ratio?

A

Maximum Tolerated Dose/Minimum Effective Dose

50
Q

How is therapeutic ratio calculated?

A

Lethal Dose 50% of people/Effective Dose 50% of people

51
Q

Define first pass metabolism

A

Occurs when drug absorbed in ileum and enters venous system. Through hepatic portal vein to liver. Extensively metabolised here.

52
Q

How can first pass effect be avoided?

A

Parenteral, Sublingual or Rectal administration.

53
Q

Define drug distribution

A

Theoretical volume that a drug is distributed into assuming this is instantaneous.

54
Q

How is dug distribution calculated?

A

Amount given/Plasma Concentration at Time 0

55
Q

Define Class 1 drug

A

Dose < number of albumin binding sites

56
Q

Define Class II drug

A

Dose is greater than number of albumin binding sites

57
Q

What is first order kinetics?

A

Metabolism is proportional to drug concentration

58
Q

What is the calculation for first order rate of metabolism?

A

Rate = Vmax x [C]/Km

59
Q

What is zero order kinetics?

A

Rate of metabolism is constant

60
Q

After how many half lives is the steady state reached?

A

5

ESA2 (4 decks)

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