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Boards Pharm 03: Autonomics > 0. Receptors > Flashcards

0. Receptors Flashcards

1
Q

Autonomic G-Protein Linked Receptors

A

Sympathetics

  • alpha-1 - Gq protein
  • alpha-2 - Gi protein
  • beta-1 - Gs
  • beta-2 - Gs

Parasympathetics

  • M1 - Gq protein
  • M2 - Gi
  • M3 - Gq

Dopamine

  • D1 - Gs
  • D2 - Gi

Histamine

  • H1 - Gq
  • H2 - Gs

Vasopressin

  • V1 - Gq
  • V2 - Gs

“Qiss (kiss) and qik (kick) till you’re siq (sick) of sqs (sex)”

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2
Q

Alpha-1 Adrenergic Receptor

A

Gq linked

  • Increase IP3 –> Increase Intracellular Ca
  • Increase DAG –> Activate protein kinase C

Actions:

  • Contract vascular smooth muscle
  • Contract pupillary dilator muscle - mydriasis
  • Contract intestinal and bladder sphincters
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3
Q

Alpha-2 adrenergic receptor

A

Gi linked

  • Inhibit adenylyl cyclase –> Decrease cAMP –> prevent protein kinase A activation

Actions:

  • Decrease sympathetic outflow
  • Decrease insulin release
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4
Q

Beta-1 adrenergic receptor

A

Gs linked

  • Activate adenylyl cyclase –> Increase cAMP –> Activate protein kinase A

Actions:

  • Increase HR
  • Increase contractility
  • Increase Renin release
  • Increase lipolysis
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5
Q

Beta-2 adrenergic receptor

A

Gs linked

  • Activate adenylyl cyclase –> Increase cAMP –> Activate protein kinase A

Actions:

  • Vasodilation
  • Bronchodilation
  • Increase HR
  • Increase contractility
  • Increase lipolysis
  • Increase insulin release
  • Decrease uterine tone
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6
Q

M1 muscarinic receptor

A

Gq linked

  • Increase IP3 –> Increase Intracellular Ca
  • Increase DAG –> Activate protein kinase C

Actions:

  • CNS and enteric nervous system signalling
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7
Q

M2 muscarinic receptor

A

Gi linked

  • Inhibit adenylyl cyclase –> Decrease cAMP –> prevent protein kinase A activation

Actions:

  • Decrease HR of atria
  • Decrease contractility of atria
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8
Q

M3 muscarinic receptor

A

Gq linked

  • Increase IP3 –> Increase Intracellular Ca
  • Increase DAG –> Activate protein kinase C

Actions:

  • Increase exocrine gland secretions (sweat, gastric acid)
  • Increase gut peristalsis
  • Increase bladder contraction
  • Bronchoconstriction
  • Pupillary sphincter muscle contraction - Miosis
  • Ciliary muscle contraction - accommodation
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9
Q

D1 dopamine receptor

A

Gs linked

  • Activate adenylyl cyclase –> Increase cAMP –> Activate protein kinase A

Actions:

  • Relax renal vascular smooth muscle
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10
Q

D2 dopamine receptor

A

Gi linked

  • Inhibit adenylyl cyclase –> Decrease cAMP –> prevent protein kinase A activation

Actions:

  • Modulate transmitter release, especially in the brain
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11
Q

H1 histamine receptor

A

Gq linked

  • Increase IP3 –> Increase Intracellular Ca
  • Increase DAG –> Activate protein kinase C

Actions:

  • Increase nasal and bronchial mucus production
  • Contract bronchioles
  • Pruritus
  • Pain
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12
Q

H2 histamine receptor

A

Gs linked

  • Activate adenylyl cyclase –> Increase cAMP –> Activate protein kinase A

Actions:

  • Gastric acid secretion
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13
Q

V1 vasopressin receptor

A

Gq linked

  • Increase IP3 –> Increase Intracellular Ca
  • Increase DAG –> Activate protein kinase C

Actions:

  • Contract vascular smooth muscle
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14
Q

V2 vasopressin receptor

A

Gs linked

  • Activate adenylyl cyclase –> Increase cAMP –> Activate protein kinase A

Actions:

  • Increase H2O permeability and reabsorption in the collecting tubules of the kidney

“V2 in the 2 Kidneys”

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15
Q

Receptor coupled Gq protein

A

Linked to H1, a-1, V-1, M-1, M-3 receptors

  • Activates Phospholipase C –> Make PIP –> PIP becomes DAG and IP3 –> DAG activates protein kinase C, and IP3 increase intracellular Ca

“HAVe 1 M&M”

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16
Q

Receptor coupled Gs protein

A

Linked to b-1, b-2, D-1, H2, V-2 receptors

  • Activate adenylyl cyclase –> Increase cAMP levels –> Activate protein kinase A –> Increase intracellular Ca (heart), and inhibit myosin light chain kinase in smooth muscle
17
Q

Receptor coupled Gi protein

A

Linked to M-2, a-2, D-2 receptors

  • Inhibit adenylyl cyclase –> Decrease cAMP levels –> Inhibit protein kinase A –> Decrease intracellular Ca (heart), and not inhibit myosin light chain kinase in smooth muscle

“the MAD 2’s”

Boards Pharm 03: Autonomics (3 decks)

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