GPCRs 2 Flashcards

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?

A

Vasodilation

17
Q

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

A

M3

B2

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?

A

M3

B2

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?

A

M3

B2

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
Q

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

A

Bladder sphincter muscle contracts

urine is contained in bladder