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Block 4 Handbook > Autonomic neuronal receptor pharmacology > Flashcards

Autonomic neuronal receptor pharmacology Flashcards

(68 cards)

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1
Q

Noradrenaline is a potent agonist at?

A

1- and a 2- adrenoceptors, and b1-adrenoceptors

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2
Q

Noradrenaline has little effect at?

A

B2-adrenoceptors

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3
Q

Adrenaline is a potent agonist at?

A

All adrenoceptors

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4
Q

Acetylcholine activates all?

A

All muscarinic receptor subtypes (M1, M2, M3) and both nicotinic receptor subtypes (neuronal, skeletal muscle)

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5
Q

Adrenoceptors are all coupled to?

A

Coupled to G-proteins

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6
Q

G-proteins interact with?

A

A variety of intracellular mechanisms

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7
Q

Activation of A1-adrenoceptors results in?

A

Results in activation of phospholipase C

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8
Q

Activation of phospholipase C increases?

A

Increases levels of the intracellular second messengers inositol triphosphate and diacylglycerol

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9
Q

A2-adrenoceptor activation results in?

A

Results in an inhibition of adenylyl cyclase

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10
Q

Inhibition of adenylyl cyclase results in?

A

A decrease in intracellular cAMP

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11
Q

Activation of B1- and B2-adrenoceptors activates?

A

Adenylyl cyclase

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12
Q

Activated adenylyl cyclase results in?

A

elevated intracellular cAMP

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13
Q

Agonist drugs which mimic noradrenaline and adrenaline at adrenoceptors include?

A
  • Phenylephrine
  • Clonidine
  • Isoprenaline
  • Dobutamine
  • Salbutamol
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14
Q

Phenylephrine is selective for?

A

A1-adrenoceptor

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15
Q

Clonidine is selective for?

A

A2-adrenoceptor

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16
Q

Isoprenaline is selective for?

A

B1- and B2-adrenoceptors

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17
Q

Dobutamine is selective for?

A

B1-adrenoceptors

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18
Q

Salbutamol is selective for?

A

B2-adrenoceptors

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19
Q

Drugs which act as competitive antagonists at adrenoceptors include?

A
  • Labetalol
  • Phentolamine
  • Prazosin
  • Propranolol
  • Metoprolol
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20
Q

Labetalol is selective for?

A

Non-selective

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21
Q

Pentolamine is selective for?

A

A1- and A2-adrenoceptors

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22
Q

Prazosin is selective for?

A

A1-adrenoceptors

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23
Q

Propranolol is selective for?

A

B1- and B2-adrenoceptors

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24
Q

Metoprolol is selective for?

A

B1-adrenoceptors

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25
Principal effector cell actions mediated by A1-adrenoceptors include?
- Smooth muscle contraction (vascular, gastrointestinal sphincters, bladder trigone, urethral internal sphincter, iris radial). - Relaxation of gastrointestinal non-sphincter smooth muscle - K+ rich saliva secretion - Glycogenolysis
26
Main actions mediated by A2-adrenoceptors are?
- Prejunctional inhibition of nordarenaline release from sympathetic postganglionic nerve terminals (autoinhibition) and platelet aggregation
27
Effector cell actions resulting from B1-adrenoceptor activation include?
- Increases in heart rate and force of contraction - Relaxation of gastrointestinal non-sphincter smooth muscle - Amylase-rich saliva secretion and lipolysis
28
Main actions mediated by B2-adrenoceptors are?
- Smooth muscle relaxation (vascular, bronchial, bladder detrusor, uterine) - Glycogenolysis - Inhibition of mast cell inflammatory mediator release
29
Muscarinic receptors are all coupled to?
G-proteins
30
Activation of muscarinic M1 and M3 receptors results in?
Activation of phospholipase C
31
Activation of muscarinic M2 receptors inhibits?
Inhibits adenylyl cyclase
32
Activation of muscarinic M2 receptors enhances?
K+ conductance
33
Agonist drugs which mimic the actions of acetylcholine at muscarinic receptors include?
- Carbachol | - Pilocarpine
34
Carbachol is selective for?
Non-selective, also a nicotinic receptor agonist
35
Pilocarpine is selective for?
Non-selective
36
Drugs with competitive antagonist properties at muscarinic receptors include?
- Atropine - Pirenzepine - Gallamine
37
Atropine is selective for?
Non-selective
38
Pirenzepine is selective for?
M1 selective
39
Gallamine is selective for?
M2-selective; also a nicotinic skeletal muscle receptor antagonist
40
Principal effector cell actions mediated by muscarinic M1 receptors include?
Gastric acid secretion
41
M1 receptors are also present on sympathetic postganglionic neuronal cell bodies and contribute to?
Acetylcholine-induced excitation in sympathetic ganglia
42
Principal effects of M2 receptor activation are a?
- Decrease in heart rate | - Prejunctional inhibition of acetylcholine release from parasympathetic preganglionic nerve terminals (autoinhibition)
43
Main actions mediated by M3 receptors are?
- Relaxation of vascular smooth muscle (via release of endothelial nitric oxide) - Smooth muscle contraction (GI, bronchial, bladder detrusor, iris and ciliary circular) - Exocrine gland secretion (potassium-rich salivary, sweat, gastrointestinal, bronchial)
44
Nicotinic receptor activation results in?
- Ligand-gated sodium/potassium channels | - Fast excitation (depolarization) of skeletal muscle and neuronal cells
45
Agonist drugs which mimic the actions of acetylcholine at nicotinic receptors include?
- Carbachol - Nicotine - Suxamethonium
46
Carbachol is selective for?
Non-selective; also a muscarinic receptor agonist
47
Nicotine is selective for?
Non-selective
48
Suxamethonium is selective for?
Skeletal muscle-selective
49
Initial excitation for skeletal muscle receptors is rapidly followed by?
Densensitization blockade, i.e. "Depolarizing neuromuscular blockade"
50
Tubocurarine and gallamine act as _____ at skeletal muscle nicotinic receptors
Competitive antagonists, results in "non-depolarizing neuromuscular blockade"
51
Mecamylamine is a ?
Selective neuronal nicotinic receptor antagonist
52
The only nicotinic receptors in the autonomic nervous system are the?
Neuronal subtype on postganglionic neuronal cell bodies and adrenal medulla cells
53
Nicotinic receptor activation results in?
Sympathetic and parasympathetic postganglionic neuronal excitation and adrenaline release
54
Reserpine function?
Decreases storage of norepinephrine
55
Methyltyrosine function?
Inhibits noradrenaline and adrenaline synthesis
56
Amphetamine and ephedrine function?
Enhances release of noradrenaline and adrenaline
57
Guanethidine function?
Inhibits release of noradrenaline and adrenaline
58
Cocaine and tricyclic antidepressants (e.g. amitriptyline) function?
Blocks neuronal uptake transporter
59
Hydrocortisone function?
Blocks the extraneuronal uptake transporter
60
Monoamine oxidase inhibitors such as tranylcypromine and moclobemide function?
Inhibits degradation of adrenaline and noradrenaline
61
Cholinergic neurotransmission is affected by drugs which are able to inhibit?
Inhibit acetylcholine synthesis and inhibits its release and inhibits its degradation
62
Hemicholinium function?
Inhibits acetylcholine synthesis
63
Botulinum toxin function?
Inhibits release of acetylcholine
64
Anticholinesterases function?
Inhibits degradation of acetylcholine
65
Physostigmine function?
Inhibits degradation of acetylcholine
66
Neostigmine function?
Inhibits degradation of acetylcholine
67
Malathion function
Inhibits degradation of acetylcholine
68
Anticholinesterases include which drugs?
- Physostigmine - Neostigmine - Malathion

Block 4 Handbook (3 decks)

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