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Phys, pharm > Receptors > Flashcards

Receptors Flashcards

1
Q

What are the 4 classes of proteins targeted by drugs?

A

Enzymes
Transporters
Ion channels
Receptors

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2
Q

Define Receptors

A

Proteins that serve as recognition sites and allow binding of chemical mediators

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3
Q

What is the function of receptors ?

A

Regulation of cellular processes
Chemical recognition and binding
Intracellular signal generation

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4
Q

Name 2 drugs which interfere with ion channels

A

Lignocaine (voltage gated sodium channel blocker)
Gabapentin (voltage gated calcium channel blocker)

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5
Q

How many aa segments do transmembrane receptors span?

A

20-25 hydrophobic amino acids

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6
Q

What is a type 1 receptor?

A

Ligand gated ion channel

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7
Q

Is a type 1 receptor ionotropic or metabotropic?

A

Ionotropic

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8
Q

How do drugs interact with membrane receptors ?

A

Via the extracellular ligand binding domain, travels through the transmembrane segments, into the cytoplasm via the cytoplasmic domain

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9
Q

What is the type 2 receptor?

A

G-protein coupled receptor

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10
Q

Is the type 2 receptor ionotropic or metabotropic?

A

Metabotropic

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11
Q

What is the effector for a type 1 ?

A

An ion channel

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12
Q

What is the effector for type 2?

A

Channel or enzyme

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13
Q

What is the type 3 receptor?

A

Receptor kinase

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14
Q

What is the type 4 receptor?

A

Nuclear receptor

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15
Q

How does a type 4 receptor couple?

A

Via DNA

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16
Q

How is a type 4 different to type 1,2&3?

A

Type 4 is an intracellular receptor whereas the others are all membrane receptors

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17
Q

Define ligand

A

Any molecule that binds to a receptor

18
Q

Define an agonist

A

An agonist produces a response in the cell after binding to a receptor

19
Q

Define an antagonist

A

An antagonist inhibits or prevents a response after a possible receptor binding

20
Q

How does a type 4 receptor work?

A

Soluble receptors that sense lipid and hormone signals and modulate gene transcription. The binding ligand must be able to cross the plasma membrane

21
Q

Give an example of an agonist

A

Pilocarpine
Nicotine
Acetylcholine
Morphine

22
Q

Give an example of an antagonist

A

Atropine
Curare

23
Q

How does type 1 transduce a signal ?

A

Hyperpolarisation or depolarisation

24
Q

How does type 2 transduce a signal?

A

Change in excitability or
Second messengers (protein phosphorylation, Ca2+ release/other) which produces a cellular effect

25
Q

How do type 3 transduce a signal?

A

Protein phosphorylation ->
Gene transcription ->
Protein synthesis ->
Cellular effects

26
Q

How does type 4 transduce a signal?

A

Ligand binds to receptor in the nucleus ->
Gene transcription ->
Leaves nucleus and protein synthesis occurs ->
Cellular effects

27
Q

Example of type 1

A

Nicotinic ACh receptor

28
Q

Example of type 2

A

Muscarinic ACh receptor

29
Q

Example of type 3

A

Cytokine receptor

30
Q

Example of type 4

A

Oestrogen receptor

31
Q

What is an ionotropic receptor?

A

Receptors that are ion channels

32
Q

What is an endogenous agonist?

A

Fast/classical neurotransmitters stored in synaptic vesicles, composed of 3-5 subunits with a central aqueous pore.

33
Q

When does a channel close?

A

When an agonist is removed or
When a receptor enters a desensitised state

34
Q

What does activation of ionotropic receptors by excitatory neurotransmitters cause? Give an example and its antagonist

A

Membrane depolarization
Action potential firing
Example: Nicotinic Acetylcholine Receptor, antagonist = tubocurarine

35
Q

What does activation of ionotropic receptors by inhibitory neurotransmitters cause? Give an example

A

Inhibits membrane depolarisation
Reduces action potential firing
Example: GABAaRs

36
Q

Structure of type 1

A

Pentameric assembly
Cys-loop type

37
Q

Structure of type 2

A

Tetrameric assembly
ionotropic glutamate type

38
Q

Structure of type 3

A

Trimeric assembly
P2X type

39
Q

Structure of type 4

A

Tetrameric assembly
Calcium release type

40
Q

Why may cells express different receptors?

A

To coordinate their responses to changes in external environments and maintain homeostasis

41
Q

What does the physiological consequence of a drug rely on?

A

Specificity

Phys, pharm (31 decks)

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