Adrenergic Receptors Flashcards

1
Q

α1 means of action

A

Primarily coupled to PLC with increase in IP3 and DAG

- release K+ liver

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2
Q

Which G protein is coupled to α1 receptors?

A

Gq

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3
Q

What are the effects of α1 stimulation?

A
  1. Vasoconstriction (in smooth muscle)
  2. Medriasis in pupil
  3. Bowel continence, urinary retention
  4. Glycogenolysis in liver
  5. Kidney inhibits renin release
    => sympathetic response
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4
Q

α2 means of action

A

Acts on pre-sympathetic nerve endings. Decreases intracellular cAMP which decreases NA -> - feedback control
(Negatively coupled to adenylate cyclase)

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5
Q

Which G protein is coupled to α2 receptors?

A

Gi

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6
Q

What are the effects of α2 stimulation?

A

Pancreatic islets decrease insulin production

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7
Q

How did Alqhuist classify adrenoreceptors?

A

by comparing relative potencies of 5 catecholamines

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8
Q

Which receptor is innervated and excitatory?

A

β1

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9
Q

Which receptor is not innervated and inhibitory?

A

β2

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10
Q

What are the effects of β1 stimulation?

A
  1. Heart rate increases

2. Increased renin release

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11
Q

What are the effects of β2 stimulation?

A
  1. Bronchodilation
  2. Vasodilation of smooth muscle
  3. Smooth muscle relaxation -> decrease in G.I. motility
  4. Increase of insulin production -> mediates glycogenesis in liver and glycogen breakdown to lactic acid in skeletal muscle (hyper acidaemia) + K+
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12
Q

What are the effects of β3 stimulation?

A
  1. Increased lipolysis

2. Relaxed bladder

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13
Q

Which G protein is coupled to β receptors?

A

Gs

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14
Q

The adrenal gland releases ___% Adrenaline and ___% Noradrenaline

A

80, 20

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15
Q

β receptor general mechanism of action

A

Activation leads to increase in cAMP + protein phosphorylation via PKA

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16
Q

α1 agonists

A

NA, AD, Phenylephrine, a-methyl

17
Q

β receptor’s in the heart are

A

excitatory

18
Q

α2 agonists

A

NA, AD, clonidine, a-methyl

19
Q

β1 agonists

A

AD, IsoP, NA, Salbutamol

20
Q

β2 agonists

A

AD, IsoP, Salbutamol

21
Q

α1 antagonists

A

Phentolamine, Phenoxybenzamine, Prazosin

22
Q

α2 antagonists

A

Phentolamine, Phenoxybenzamine, Prazosin

23
Q

β1 antagonists

A

Propranolol, Atenolol

24
Q

β2 antagonists

A

Propranolol, Atenolol

25
Q

What are the unwanted effects of β2 antagonists?

A

Tremor, hypokalaemia, vasodilation