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Y2 Pharmacology > Receptors > Flashcards

Receptors Flashcards

1
Q

What are class I nuclear receptors?

A

Lipophilic receptors that have to be recruited to the nuclear membrane
e.g steroid receptors

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2
Q

What are class II nuclear receptors?

A

Heterodimeric receptors already in the membrane which regulate transcription

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3
Q

Outline a GPCR response

A
  1. Agonist binding
  2. GDP detaches from the α-subunit and is replaced by GTP
  3. The α-subunit detaches from βγ and activates adenylyl cyclase which activates PKA which has downstream effects
  4. GTP is hydrolysed and βγ reattaches. This switches the signal off.
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4
Q

What type of structure has an NDMA receptor got?

A

Ionotropic glutamate type ion channel

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5
Q

What type of structure has GABAa and nAChR got?

A

Cys-loop type ion channel

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6
Q

What type of receptor is an insulin receptor?

A

Receptor tyrosine kinase

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7
Q

What class of receptor do cytokines activate?

A

Receptor tyrosine kinase

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8
Q

In myasthenia gravis, what sort of receptors do autoantibodies target?

A

Nicotinic acetylcholine receptors

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9
Q

Autoantibodies can lead to graves disease. What are the symptoms?

A

High metabolic rate
Increased skin temperature
Bulging eyes
Tachycardia (high heart rate)

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10
Q

What are overactive ligand gated ion channels in the brain associated with?

A

Epilepsy

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11
Q

Mutations in what class of receptors are usually associated with cancers?

A

Receptor tyrosine kinases

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12
Q

What are schild plots used to measure?

A

Reversible competitive antagonist affinity
Plots log[antagonist] against log[dose ratio -1]

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13
Q

What practical method is used to measure receptor affinity?

A
  1. Ligands are bound to the sample
  2. Unbound ligands are rinsed off
  3. Filter this to find percentage of bound ligands
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14
Q

When measuring ligands bound to binding sites, how are they incubated

A

Stored at low temperature and with antioxidants for stability
-ine molecules are oxidisable so must avoid air

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15
Q

What is drug efficacy?

A

How well a drug evokes a response

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16
Q

What is an intermediate efficacy?

A

If agonists occupy all receptors and cannot produce a full response. (Efficacy between 0 and 1)

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17
Q

How can cells become desensitised to drugs?

A

When a drug is given continuously,
Endocytosis of receptors and degradation. This leads to a loss of receptors.
Change in receptor e.g phosphorylation
Increased metabolic degradation

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18
Q

How many types of opiate receptor are there?

A

3

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19
Q

What type of opiate receptor do morphine and phentanol target?

A

μ-receptors

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20
Q

What are some side effects of opiate use?

A

Chronic constipation
Impaired breathing and brain functions

21
Q

Name some μ-opiate receptor agonists

A

Morphine, heroin, methadone, codeine, fentanyl, β-endorphins

22
Q

What sort of drug is naxolone?

A

μ-opiate receptor antagonist

23
Q

What is a false substrate drug?

A

Drug which produces an abnormal metabolite or prevents transporters working

24
Q

What is a prodrug?

A

Drug which binds an enzyme, releasing an active version of the drug

25
Q

How can toxicity of heavy metals be reduced with chemical antagonism?

A

Using chelating agents, e.g dimercaprol

26
Q

Outline chemical antagonism

A

Substances reacting in solution, so that effects of the active drug are lost

27
Q

Outline non-competitive antagonism

A

Blocks a step between receptor activation and response
Does not compete with the agonist
Inhibits function of a signalling molecule

28
Q

Outline pharmacokinetic antagonism?

A

Change in drug metabolism, e.g decreasing absorption in the GI tract
Warfarin thins blood, reducing a drug’s effective concentration in the bloodstream
Change in excretion of an agonist
Drugs that alter protein binding and filtration

29
Q

What is physiological antagonism?

A

Two drugs with opposing actions in the body interacting
Endogenous mediators- describe actions through separate cells or transduction-receptor systems

30
Q

Outline competitive antagonism

A

Compete with agonists for a receptor
The complex formed does not stimulate any downstream effects

31
Q

What is dose ratio?

A

How many more times an agonist is required in the presence of an antagonist

32
Q

How do irreversible competitive antagonists come about?

A

Bond created between the drug and receptor. This antagonism cannot be reversed by washing.
e.g dibenamine blocking histamine responses.

33
Q

Give the definition of a drug

A

chemical of known structure which produces a biological effect in living organisms

34
Q

Give the definition of a receptor

A

protein which recognises and binds chemical mediators

35
Q

What is a medicine

A

preparation which contains a drug to produce a theraputic effect. Often contain excipients, stabilisers and solvents

36
Q

How can the molecular nature of a signal transduction mechanism be predicted?

A

Class/structure of the receptor

37
Q

Give 3 examples of chemical mediators

A

Hormones
Neurotransmitters
Antibodies

38
Q

What are first generation biopharmaceuticals?

A

endogenous proteins produced with DNA technology

39
Q

What are second generation biopharmaceuticals?

A

engineered proteins to improve performance

40
Q

What is -mab the suffix of?

A

monoclonal antibody

41
Q

What is -asone the suffix of?

A

corticosteroid

42
Q

What is -caine the suffix of?

A

local anaestetic

43
Q

What is -statin the suffix of?

A

lipid lowering drug

44
Q

What is -artan the suffix of?

A

angiotensin receptor blocker

45
Q

What is -dipine the suffix of?

A

calcium channel blocker

46
Q

What is -barpital the suffix of?

A

barbiturate

47
Q

What is EC50?

A

Effective concentration of a drug which gives 50% of a maximal response

48
Q

What is a receptor reserve?

A

less than 100% of receptors have to be occupied to give a max response

Y2 Pharmacology (10 decks)

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