Receptors Flashcards

1
Q

M1

A

Gq-coupled: neurons

• Decrease in membrane PIP2 inhibits potassium conductance (M-channel) in neurons

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2
Q

M2

A

Gi-coupled: heart and presynaptic nerve terminals
• Neurons: phosphorylation of Cav reduces transmitter release
• Heart: βɣ activates GIRK decreasing HR

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3
Q

M3

A

Gq-coupled: exocrine/sweat glands, oxyntic cells, smooth muscle
• Muscle contraction
• Glandular secretion

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4
Q

α1

A
Gq-coupled (NA≥Adr)
• Vasoconstriction
• Contraction of uterine smooth muscle
• Relaxation of GI smooth muscle
• Salivary secretion
• Glycogenolysis
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5
Q

α2

A

Gi-coupled (Adr≥NA)

• Inhibits transmitter release (presynaptic)

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6
Q

β1

A

Gs-coupled (Adr=NA)
• Increases heart rate and force of contraction
• Relaxes GI muscle

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7
Q

β2

A

Gs-coupled (Adr>NA)
• Bronchodilation
• Vasodilatation in cardiac and smooth muscle
• Relaxation of uterine and bladder smooth muscle
• Muscle tremor (thermogenesis)

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8
Q

β3

A

Gi-coupled (NA≥Adr)
• Decreases heart rate and force of contraction
• Vasodilatation
• Relaxation of detrusor

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9
Q

A1

A

Gi-coupled
• Cardiac depression (similar to M2 activation)
• Bronchoconstriction in asthmatic subjects
• Presynaptic inhibition (reduce glutamate release in brain) - induces sleep and is an endogenous antiepileptic

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10
Q

A2

A
Gs-coupled - 2A/B
2A: 
• Vasodilation
• Decreased activation of neutrophils
2B:
• Vasodilation
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11
Q

A3

A

Gi or Gq-coupled

• Decrease eosinophil activation

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12
Q

P2X

A

Ionotropic (homo/heterotrimers) non-selective (allows calcium flux)
X1: mediate rapid phasic contraction of the vas deferens
X4: mediates ATP-mediated increases in force of contraction in the heart

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13
Q

P2Y

A

All GPCRs

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14
Q

H1

A

Gq-coupled
• Smooth muscle contraction in the bronchioles
• Blood vessel dilatation largely via NO
• Itching through activation of sensory nerves

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15
Q

H2

A

Gs-coupled
• Gastric acid secretion
• Increased heart rate

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16
Q

H3

A

Gi-coupled

• Inhibitory autoreceptors in the CNS

17
Q

H4

A

Gi-coupled

• Involved in chemotaxis and chemokine release

18
Q

B1

A

Gq-coupled, upregulated in inflammation
• Vascular endothelium: PGI2 synthesis (via PLA2) and NO (via eNOS)
• Activation and sensitisation of nociceptors (via PKC)
Activated by des-Arg-bradykinin, bradykinin is a poor agonist

19
Q

B2

A

Gq-coupled, constitutively
• Vascular endothelium: PGI2 synthesis (via PLA2) and NO (via eNOS)
• Activation and sensitisation of nociceptors (via PKC)

20
Q

CysLT

A

Gq-coupled
• Bronchoconstriction
• Vascular permeability
• Mucous secretion

21
Q

BLT

A

Gq/Gi-coupled

• Chemoattractant and activator of neutrophils and macrophages