GPCRs 2 Flashcards

(25 cards)

1
Q

What does PKA in the heart do?

A

Phosphorylates VOCCs

which increases their activity

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2
Q

What are the effects of increased VOCC activity in the heart?

A

Increased calcium ion influx into the cell
increased contractility
positive inotropic effect

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3
Q

What does inotropy mean?

A

Force of contraction

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4
Q

What types of GPCRs are located in presynaptic neurones in the CNS and PNS?

A

M-opioid GPCRs

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5
Q

What type of G-protein are M-opioid GPCRs coupled to?

A

Gi

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6
Q

What effect do activated M-opioid receptors have on pre-synaptic neurones in the CNS and PNS?

A

Reduce neurotransmitter release

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7
Q

How do activated M-opioid receptors on pre-synaptic neurones in the CNS and PNS reduce neurotransmitter release?

A

Free beta-gamma subunit binds to VOCCs

inhibits calcium ion influx

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8
Q

What are the types of GPCRs located in the heart?

A

M2

B1

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9
Q

Where are M2 receptors in the heart located?

A

SA node

AV node

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10
Q

What is the outcome of activation of the different M2 receptors in the heart?

A

SA node - negative chronotropy

AV node - reduced cardiac conduction velocity

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11
Q

Where are B1 adrenoceptors located in the heart?

A

SA node

Ventricles

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12
Q

What is the outcome of activation of the different B1 adrenoceptors in the heart?

A

SA node - positive chronotropy

Ventricles - positive inotropy

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13
Q

What does chronotropy mean?

A

Heart rate

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14
Q

What are the types of GPCRs located in vascular smooth muscle?

A

A1

B2

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15
Q

What is the outcome of activation of A1 adrenoceptors in vascular smooth muscle?

A

Vasoconstriction

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16
Q

What is the outcome of activation of B2 adrenoceptors in vascular smooth muscle?

17
Q

What are the types of GPCRs located in bronchiolar smooth muscle?

18
Q

What is the outcome of activation of M3 receptors in bronchiolar smooth muscle?

A

Bronchoconstriction

19
Q

What is the outcome of activation of B2 adrenoceptors in bronchiolar smooth muscle?

A

Bronchodilation

20
Q

What are the types of GPCRs located in intestinal smooth muscle?

21
Q

What is the outcome of activation of M3 receptors in intestinal smooth muscle?

A

Contraction of smooth muscle

giving increased motility

22
Q

What is the outcome of activation of B2 adrenoceptors in intestinal smooth muscle?

A

Relaxation of smooth muscle

decreased motility

23
Q

What are the types of GPCRs located in bladder smooth muscle?

24
Q

What is the outcome of activation of M3 receptors in bladder smooth muscle?

A

Contraction of bladder detrusor muscles
relaxation of sphincter muscles
giving passing of urine

25
What is the outcome of activation of B2 adrenoceptors in bladder smooth muscle?
Bladder sphincter muscle contracts | urine is contained in bladder