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BI316 > Drug receptor Interactions - lecture 6 > Flashcards

Drug receptor Interactions - lecture 6 Flashcards

1
Q

Name the 5 main models to explain the effects of partial agonists, full agonists and antagonsists.

A

Occupancy Model, Rate Model, Induction Model, Perturbation Model and Cooperativity Model.

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2
Q

Occupancy Model

A

The intensity of pharmacological effect is directly proportional to the number of receptor binding sites occupied by the drug.

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3
Q

Rate Model

A

The intensity of pharmacological effect is directly proportional to the total number of encounters of the drug with its receptor binding sites per unit time.

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4
Q

Induction Model

A

The pharmacological effect is induced by the drug through specific conformational changes in the active binding site of the receptor complex.

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5
Q

Perturbation Model

A

Pharmacological substances induce macromolecular perturbations, agonist trigger relatively specific conformational changes as compared to antagonists.

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6
Q

Cooperativity Model

A

If pharmacological receptors exist in a dynamic equilibrium between activated and inactive states, agonists may shift the equilibrium to an active state and antagonists to an inactive state.

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7
Q

How many receptor super-families are there and what do they provide?

A
  • 4 receptors
  • Provides a useful framework for interpreting most drug-receptor interactions.
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8
Q

What are the type 1 receptors and give an example.

A

Ionotropic receptor
- Ligand-gated ion channel receptor
- example: nAChR

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9
Q

Describe the components of the Ligand-gated ion channel

A
  • Ligand binding domain
  • Ion channel lining domain
  • Membrane-spanning domain
    > Hydrophobic a-helical region
    > approx. 20 AAs long
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10
Q

How many subunits are formed together to result in a ion channel complex?

A

five

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11
Q

Characteristics of type 1 receptors?

A
  • Extremely fast response (milliseconds)
  • Membrane-bound
  • Direct coupling to ion channel
  • Oligomeric assembly of subunits surrounding central ion pore.
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12
Q

What are the type 2 receptors and give an example.

A

Metabotropic receptor
- G-protein coupled receptor
- example: mAChR

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13
Q

Describe the components of the type 2 receptors

A
  • Ligand binding domains
  • G-protein coupling domain
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14
Q

Characteristics of type 2 receptors?

A
  • fast response (seconds)
  • membrane-bound
  • indirect coupling via G-protein to effector (enzyme or ion channel)
  • monomeric assembly comprising of seven trans-membrane helices.
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15
Q

What are the type 3 receptors and give an example.

A

Kinase-linked receptor
- Cytokine receptor
-example: Insulin-R

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16
Q

Describe the components of the type 3 receptors

A
  • Extracellular Ligand binding domain
  • Intracellular, Catalytic domain, Kinase activity
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17
Q

Characteristics of type 3 receptors?

A
  • slow response (hours)
    -membrane-bound
  • direct coupling to enzyme
  • single trans-membrane helix
  • direct linkage between receptor and kinase enzyme.
18
Q

What are the type 4 receptors and give an example.

A

Nuclear receptor
- example: Steroid-R

19
Q

Describe the components of the type 4 receptors

A
  • Receptor binding domain
  • ‘Zinc-fingers’ DNA-binding domain
20
Q

Characteristics of type 4 receptors?

A
  • slow response (hours)
  • intracellular
  • coupling via DNA
  • effect on gene transcription
  • monomeric structure with separate receptor and DNA binding domains
21
Q

What are the types of nuclear receptors?

A

Class I, Hybrid Class and Class II

22
Q

Class 1 of nuclear receptors characteristics and examples?

A
  • present in cytoplasm
  • operate as homodimers
  • mainly endocrine ligands
  • high affinity
    examples: GR, MR, ER and PR
23
Q

Hybrid Class characteristics and examples?

A
  • mainly endocrine
  • operates as RXR heterodimers
    examples: TR, VDR
24
Q

Class II characteristics and examples?

A
  • present in nucleus
  • operate as heterodimers (except RXR)
  • mainly lipid ligands
  • low affinity
    examples: PPAR, LXR, FXR and RXR
25
Q

What is the agonist for the nAChR receptor?

A

Nicotine

26
Q

Nicotine

A
  • alkaloid from tobacco plants
  • Agonist of nicotinic acetylcholine receptor
  • stimulating drug (Parasympathomimetic)
  • potential toxic side effects
27
Q

What is the agonist for the beta-adrenoreceptor receptor?

A

Isoprenaline

28
Q

Isoprenaline

A
  • B-adrenergic agonist
  • structural similarity to adrenaline
  • treatment of slow heart rate (Bradycardia)
29
Q

What is the modulator for the ion channel: Voltage-dep. Na+ - channel?

A

Lidocaine

30
Q

Lidocaine

A
  • local anaesthetic
  • common usage: injected for dental anesthesia and minor surgery, topical form relieves skin inflammation.
31
Q

What is the agonist for the Voltage-dep. Ca2+ - channel?

A

Nifedipine

32
Q

Nifedipine

A
  • Dihydropyridine
  • L-type calcium channel blocker
  • Usage:
    > anti-anginal drug
    > antihypertensive agent
33
Q

What is the inhibitor for the enzyme: Acetylcholinesterase?

A

Neostigmine

34
Q

Neostigmine

A
  • Reversible inhibitor of acetylcholinesterase
  • Interference with the breakdown of physiological ligand
  • Indirect stimulation of nicotine and muscarinic receptors
  • usage:
    > Reversal of the effected of non-depolarising muscle relxants following anaesthesia
    > Treatment of myasthenia gravis to increase NMJ stimulation.
35
Q

What is the inhibitor for the enzyme Cyclooxygenase?

A

Aspirin

36
Q

Aspirin

A
  • Non-steroidal anti-inflammatory drug (NSAID)
  • Inhibitor of the enzyme cyclooxygenase (COX-1>COX-2)
  • Usage:
    > Analgesic
    > Anti-platelet drug
37
Q

What is the inhibitor for the choline carrier?

A

Hemicholinium

38
Q

Hemicholinium

A
  • blocks choline uptake
  • not used clinically
  • neuromuscular blocking drug
39
Q

What is the inhibitor for the Na+/K+- pump?

A

Ouabain

40
Q

Ouabain

A
  • Cardiac glycoside
  • Blocker of Na+/K+ - ATPase
  • Increases (Ca2+)i due to decreased NCX
  • Therapeutic usage in heart failure
  • Potential toxicity

BI316 (2 decks)

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