Autonomic neuronal receptor pharmacology Flashcards

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
Q

Principal effector cell actions mediated by A1-adrenoceptors include?

A
  • 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
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26
Q

Main actions mediated by A2-adrenoceptors are?

A
  • Prejunctional inhibition of nordarenaline release from sympathetic postganglionic nerve terminals (autoinhibition) and platelet aggregation
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27
Q

Effector cell actions resulting from B1-adrenoceptor activation include?

A
  • Increases in heart rate and force of contraction
  • Relaxation of gastrointestinal non-sphincter smooth muscle
  • Amylase-rich saliva secretion and lipolysis
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28
Q

Main actions mediated by B2-adrenoceptors are?

A
  • Smooth muscle relaxation (vascular, bronchial, bladder detrusor, uterine)
  • Glycogenolysis
  • Inhibition of mast cell inflammatory mediator release
29
Q

Muscarinic receptors are all coupled to?

A

G-proteins

30
Q

Activation of muscarinic M1 and M3 receptors results in?

A

Activation of phospholipase C

31
Q

Activation of muscarinic M2 receptors inhibits?

A

Inhibits adenylyl cyclase

32
Q

Activation of muscarinic M2 receptors enhances?

A

K+ conductance

33
Q

Agonist drugs which mimic the actions of acetylcholine at muscarinic receptors include?

A
  • Carbachol

- Pilocarpine

34
Q

Carbachol is selective for?

A

Non-selective, also a nicotinic receptor agonist

35
Q

Pilocarpine is selective for?

A

Non-selective

36
Q

Drugs with competitive antagonist properties at muscarinic receptors include?

A
  • Atropine
  • Pirenzepine
  • Gallamine
37
Q

Atropine is selective for?

A

Non-selective

38
Q

Pirenzepine is selective for?

A

M1 selective

39
Q

Gallamine is selective for?

A

M2-selective; also a nicotinic skeletal muscle receptor antagonist

40
Q

Principal effector cell actions mediated by muscarinic M1 receptors include?

A

Gastric acid secretion

41
Q

M1 receptors are also present on sympathetic postganglionic neuronal cell bodies and contribute to?

A

Acetylcholine-induced excitation in sympathetic ganglia

42
Q

Principal effects of M2 receptor activation are a?

A
  • Decrease in heart rate

- Prejunctional inhibition of acetylcholine release from parasympathetic preganglionic nerve terminals (autoinhibition)

43
Q

Main actions mediated by M3 receptors are?

A
  • 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
Q

Nicotinic receptor activation results in?

A
  • Ligand-gated sodium/potassium channels

- Fast excitation (depolarization) of skeletal muscle and neuronal cells

45
Q

Agonist drugs which mimic the actions of acetylcholine at nicotinic receptors include?

A
  • Carbachol
  • Nicotine
  • Suxamethonium
46
Q

Carbachol is selective for?

A

Non-selective; also a muscarinic receptor agonist

47
Q

Nicotine is selective for?

A

Non-selective

48
Q

Suxamethonium is selective for?

A

Skeletal muscle-selective

49
Q

Initial excitation for skeletal muscle receptors is rapidly followed by?

A

Densensitization blockade, i.e. “Depolarizing neuromuscular blockade”

50
Q

Tubocurarine and gallamine act as _____ at skeletal muscle nicotinic receptors

A

Competitive antagonists, results in “non-depolarizing neuromuscular blockade”

51
Q

Mecamylamine is a ?

A

Selective neuronal nicotinic receptor antagonist

52
Q

The only nicotinic receptors in the autonomic nervous system are the?

A

Neuronal subtype on postganglionic neuronal cell bodies and adrenal medulla cells

53
Q

Nicotinic receptor activation results in?

A

Sympathetic and parasympathetic postganglionic neuronal excitation and adrenaline release

54
Q

Reserpine function?

A

Decreases storage of norepinephrine

55
Q

Methyltyrosine function?

A

Inhibits noradrenaline and adrenaline synthesis

56
Q

Amphetamine and ephedrine function?

A

Enhances release of noradrenaline and adrenaline

57
Q

Guanethidine function?

A

Inhibits release of noradrenaline and adrenaline

58
Q

Cocaine and tricyclic antidepressants (e.g. amitriptyline) function?

A

Blocks neuronal uptake transporter

59
Q

Hydrocortisone function?

A

Blocks the extraneuronal uptake transporter

60
Q

Monoamine oxidase inhibitors such as tranylcypromine and moclobemide function?

A

Inhibits degradation of adrenaline and noradrenaline

61
Q

Cholinergic neurotransmission is affected by drugs which are able to inhibit?

A

Inhibit acetylcholine synthesis and inhibits its release and inhibits its degradation

62
Q

Hemicholinium function?

A

Inhibits acetylcholine synthesis

63
Q

Botulinum toxin function?

A

Inhibits release of acetylcholine

64
Q

Anticholinesterases function?

A

Inhibits degradation of acetylcholine

65
Q

Physostigmine function?

A

Inhibits degradation of acetylcholine

66
Q

Neostigmine function?

A

Inhibits degradation of acetylcholine

67
Q

Malathion function

A

Inhibits degradation of acetylcholine

68
Q

Anticholinesterases include which drugs?

A
  • Physostigmine
  • Neostigmine
  • Malathion