Essential Pharmacology Flashcards

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1
Q

How is receptor specificity maintained?

A

Chemical messengers (e.g. NT/hormones) only fit certain receptors and so will only produce a response in specific cells with that receptor.

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2
Q

Can receptors be coupled?

A

The same receptor can be coupled to trigger a different response in different cells- one cell can have many of the same or different receptors.

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3
Q

What are intracellular receptors?

A

Intracellular receptors are lipid-soluble (e.g. steroid hormones)- they can cross the cell membrane therefor act on receptors in the cell, including on the nucleus (transcription factors etc).

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4
Q

What is an example of an intracellular receptor?

A

Nitrogen oxide.

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5
Q

Why can intracellular receptors have direct action on nucleic processes?

A

Can permeate the cell membrane as they are lipid-soluble.

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6
Q

What are cell surface (plasma membrane) receptors?

A

Receptors on the cell surface.

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7
Q

What are the 4 types of cell surface receptors?

A
Ionotropic receptors (act as ion channels)
Receptors with intrinsic enzyme activity
Receptors interacting with JAK kinases
G-protein coupled receptors
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8
Q

What do ionotropic cell surface receptors do?

A

Act as ion channels.

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9
Q

What do receptors with intrinsic enzyme activity do?

A

Directly initiate enzyme activity.

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10
Q

What do receptors interacting with JAK kinases do?

A

Bind to JAK kinases which allows phosphorylation and subsequent activation of response.

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11
Q

What do G-protein coupled receptors do?

A

Messenger binds to receptor which is coupled with a G-protein- the G-protein initiates enzyme regulation.

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12
Q

What are two common enzymes that G-protein coupled receptors can be attached to?

A

Adenylyl cyclase

Phospholipase C

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13
Q

What does adenylyl cyclase do?

A

Produces cAMP to regulate PKA.

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14
Q

What does phospholipase C do?

A

Produces DAG to regulate PKC and IP3 to regulate calcium.

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15
Q

What do PKA and PKC do?

A

Used to phosphorylate therefore have a host of functions.

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16
Q

What is the largest class of cell surface receptors?

A

G-protein coupled receptors.

17
Q

Are there different types of G-protein coupled receptor?

A

Yes, there are many- Gs, Gi, Go, Gq etc.

18
Q

What is a drug?

A

A drug is a chemical agent that affects a biological system.

19
Q

What are the 4 sources of drugs?

A

Natural products
Synthetic products
Gene therapy
Biotechnology

20
Q

How do drugs act?

A

Act by binding on receptor binding sites and have characteristic responses.

21
Q

What do agonists do?

A

Mimic receptor function.

22
Q

What do antagonists do?

A

Block receptor function.

23
Q

What is the EC50?

A

EC50 is the concentration of the drug that gives a 1/2 maximal response.

24
Q

What is affinity?

A

Affinity is determined by the strength of chemical attraction between a drug and its receptor.

25
Q

What is efficacy?

A

Efficacy is determined by a drugs ability at actually activating the receptor.

26
Q

What characterises a full agonist in terms of affinity and efficacy?

A

Increased affinity, increased efficacy.

27
Q

What characterises a partial agonist in terms of affinity and efficacy?

A

Increased affinity, reduced efficacy.

28
Q

What characterises an antagonist in terms of affinity and efficacy?

A

Increased affinity, NO efficacy (blocks).

29
Q

Does one transmitter always act on one receptor?

A

No- one transmitter may act on several receptor subtypes.

30
Q

What do selective agonists do?

A

Only activate some receptors.

31
Q

Give an example of a selective agonist.

A

Salbutamol.

32
Q

What do selective antagonists do?

A

Only block some receptors.

33
Q

Give an example of a selective antagonist.

A

Propanolol.

34
Q

How is EC50 affected by affinity?

A

Higher affinity = lower EC50

Lower affinity = higher EC50