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2a- Pharmacology > Drugs and receptors > Flashcards

Drugs and receptors Flashcards

1
Q

What are targets of drugs?

A

● Receptors
● Enzymes
● Transporters
● Ion channels

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2
Q

What is a receptor?

A

A component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to the ligands observed effects

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3
Q

What are the 2 types of ligand?

A

exogenous (drugs) or endogenous (hormones, neurotransmitter, etc)

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4
Q

Which classes of chemicals communicate using receptors?

A
  • Neurotransmitters → acetylcholine, serotonin
  • Autacoids → cytokines, histamine
  • Hormones → testosterone, hydrocortisone
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5
Q

What causes allergy?

A

Increased histamine

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6
Q

What causes Parkinson’s?

A

Reduced dopamine

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7
Q

What causes Myasthenia gravis?

A

Loss of Ach receptors

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8
Q

What causes mastocytosis (mast cells)?

A

Increased c-kit receptor

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9
Q

What are the 4 types of receptor?

A
  • Ligand-gated ion channels
  • G protein coupled receptors
  • Kinase-linked receptors
  • Cytosolic/nuclear receptors
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10
Q

What are ligand-gated ion channels receptors?

A

nicotinic ACh receptor

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11
Q

What are G protein coupled receptors?

A

beta-adrenoceptors

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12
Q

What are Kinase-linked receptors for?

A

receptors for growth factors

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13
Q

What are Cytosolic/nuclear receptors?

A

steroid receptors

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14
Q

What is the GPCR M3R’s G protein?

A

Gg

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15
Q

What is the GPCR M3R coupled with?

A

PLC

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16
Q

What are the 2nd messengers for the GPCR M3R?

A

IP3/DAG

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17
Q

What is the GPCR β2-AR’s G protein?

A

Gs

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18
Q

What is the GPCR β2-AR coupled with?

A

Adenylyl cyclase (AC)

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19
Q

What is the 2nd messenger for the GPCR β2-AR?

A

Cyclic-AMP

20
Q

How do kinase-linked receptors work?

A
  1. Kinasesare enzyme that catalyse the transfer of phosphate groups between proteins - process is known as phosphorylation
  2. The substrate gains a phosphate group ”donated” by ATP
  3. Transmembrane receptors activated when the binding of an extracellular ligand causes enzymatic activity on the intracellular side
  4. Interaction with ligand on surface causes change of catalytic energy of enzyme → signalling
21
Q

How do ligand gated ion channels work?

A
  • Ion channelsare pore-formingmembrane proteinsthat allowionsto pass through the channel pore so that the cell undergoes a shift inelectric chargedistribution
  • The change in charge can be mediated by an influx of any kind ofcation(+ve) or efflux of any kind ofanion (-ve)
  • Causes conformational change
22
Q

How do G protein coupled receptors work?

A
  • act as molecular switches (GDP (guanosine diphosphate) = on, GTP (guanosine triphosphate) = off)
  • Targeted by >30% of drugs
  • Ligands include light energy, peptides, lipids, sugars and proteins
23
Q

How do nuclear receptors work?

A

Work by modifying gene transcription

24
Q

What is tamoxifen?

A
  • acts as aselective oestrogen receptor modulator(SERM), or as apartial agonistof theoestrogen receptors
  • Used in ER+ (oestrogen receptor positive) cancers
25
Q

What is an agonist?

A

a compound that binds to a receptor and activates it

26
Q

What is an antagonist?

A

a compound that reduces the effect of an agonist

27
Q

What is intrinsic activity (IA) or efficacy?

A

ability of a drug-receptor complex to produce a maximum functional response

28
Q

What are the 2 category’s of cholinergic receptors?

A

nicotinic and muscarinic

29
Q

What is the agonist for mAChR?

A

Muscarine

30
Q

What is the antagonist for mAChR?

A

Atropine

31
Q

What is the agonist for nAChR?

A

Nicotine

32
Q

What is the antagonist for nAChR?

A

Curare

33
Q

Do agonists have efficacy or affinity?

A

Have both

34
Q

Do antagonists have efficacy or affinity?

A

Have affinity but NO efficacy

35
Q

What is competitive antagonism?

A

Binds to the same site

36
Q

What is non-competitive antagonism?

A

Binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor

37
Q

What factors govern drug action?

A
  • Receptor-related
    • affinity
    • efficacy
  • Tissue-related
    • receptor number
    • signal amplification
38
Q

What is a receptor reserve?

A

Spare receptors basically

39
Q

What is affinity?

A

Describes how well a ligand binds to the receptor

40
Q

What is efficacy?

A

Describes how well a ligand activates the receptor

41
Q

Are receptor reserves for full or partial agonists?

A
  • This holds for a full agonist in a given tissue
    • reserve can be large or small, depends on tissue
  • No receptor reserve for a partial agonist
42
Q

What is signal transduction?

A

a basic process involving the conversion of a signal from outside the cell to a functional change within the cell

43
Q

What is signal amplification?

A

to increase the strength of a signal

44
Q

What is allosteric modulation?

A

When an allosteric ligand binds to a different site on the molecule and prevents the signal from being transmitted

45
Q

What is inverse agonism?

A

When adrug that binds to the same receptor as anagonistbut induces a pharmacological response opposite to that of theagonist

46
Q

What is tolerance?

A

(slow)
- reduction in agonist effect over time
- continuously, repeatedly, high concentrations
- eg. Continuously having
steroid in asthma

47
Q

What is desentisation?

A
  • (rapid)
  • uncoupled
  • internalized
  • degraded

2a- Pharmacology (10 decks)

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