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Mechanism of Drug Action (Drugs) > NT receptors > Flashcards

NT receptors Flashcards

1
Q

Noradrenaline

A
  1. α1
  2. α2
  3. β1
  4. β2
  5. β3
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2
Q

α1-adrenoreceptor

A
  • Type: Gq/11
  • Functions:

Pupil dilation

Vasoconstriction

Salivary secretion

Decreased GI motility

Piloerection

Contraction of bladder smooth muscle

Ejaculation

Increased glycogenolysis and gluconeogenesis

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3
Q

α2-adrenoreceptor

A
  • Type: Gi/o
  • Functions:

Decreased NT (e.g. NA) release

Platelet aggregation

Inhibition of insulin release

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4
Q

β1-adrenoreceptor

A
  • Type: Gs
  • Functions:

Increased force of cardiac contraction

Increased heart rate

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5
Q

β2-adrenoreceptor

A
  • Type: Gs
  • Functions:

Bronchodilation

Vasodilation in myocardium/skeletal muscle

Relaxation of uterine smooth muscle

Gluconeogenesis

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6
Q

β3-adrenoreceptor

A
  • Type: Gs
  • Functions:

Lipolysis

Thermogenesis

Relaxation of bladder smooth muscle

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7
Q

Acetylcholine

A

Nicotinic:

  1. N1
  2. N2

Muscarinic:

  1. M1
  2. M2
  3. M3
  4. M4
  5. M5
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8
Q

M1 ACh receptor

A
  • Type: Gq/11
  • Functions:

Mediates synaptic transmission in CNS and PNS.

Can be found in nicotinic synapses. Binding of ACh to these cause a slow depolarisation (EPSP).

Gastric acid secretion

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9
Q

M2 ACh receptor

A
  • Type: Gi/o
  • Functions:

Involved in parasympathetic control of the heart and feedback pre-synaptic inhibition in nerve terminals.

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10
Q

M3 ACh receptor

A
  • Type: Gq/11
  • Functions:

Sweat secretion

Salivation

Pupil constriction

Ciliary muscle contraction

Vasodilation (via NO)

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11
Q

M4 ACh receptor

A
  • Type: Gq/11
  • Functions:

CNS transmission

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12
Q

M5 ACh receptor

A
  • Type: Gq/11
  • Functions:

CNS transmission

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13
Q

Histamine

A

H1-4

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14
Q

Histamine H1 receptor

A
  • Type: Gq/11
  • Functions: Inflammatory response
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15
Q

Histamine H2 receptor

A
  • Type: Gs
  • Functions: Gastric acid secretion
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16
Q

Histamine H3 receptor

A
  • Type: Gi/o
  • Functions: Inhibitory CNS autoreceptor
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17
Q

Histamine H4 receptor

A
  • Type: Gi/o
  • Functions: Chemotaxis/cytokine release
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18
Q

Serotonin

A
  1. 5-HT1A, B, D - F
  2. 5-HT2A - C
  3. 5-HT3
19
Q

5-HT1

20
Q

5-HT2

A

Type: Gq/11

21
Q

5-HT3

22
Q

Bradykinin

23
Q

B1 bradykinin receptor

A
  • Type: Gq/11
  • Functions: Expressed following induction by pro-inflammatory cytokines (e.g. IL-1) and binds to des-arg-bradykinin to cause pain and vasodilation
24
Q

B2 bradykinin receptor

A
  • Type: Gq/11
  • Function: Expressed constitutively and binds to bradykinin/kallidin to cause vasodilation
25
Q

Tackykinins

A
  • Substance P: NK1R
  • Neurokinin A: NK2R
26
Q

NK1R

A
  • Type: Gq/11
  • Functions:

Mast cell degranulation

Smooth muscle contraction

Vasodilation

Pain sensitisation

27
Q

NK2R

A
  • Type: Gq/11
  • Functions:

Mast cell degranulation

Smooth muscle contraction

Vasodilation

Pain sensitisation

28
Q

Lipoxins

29
Q

FRP2

A
  • Type: Gi/o
  • Functions: Antagonises effects of CysLT1 receptors and has anti-inflammatory effects
30
Q

Leukotrienes

A

LTB4: BLT1 + BLT2 (Gq or Gi)

CysLTs: CysLT1 + CysLT2 (Gq)

31
Q

PGD2

32
Q

DP

A
  • Type: Gs
  • Functions:

Vasodilation

Inhibition of platelet aggregation

Smooth muscle relaxation (GI/uterine)

33
Q

PGE2

34
Q

EP1

A
  • Type: Gq/11
  • Functions: Bronchial/GI smooth muscle contraction
35
Q

EP2

A
  • Type: Gs
  • Functions:

Bronchodilation

Vasodilation

Smooth muscle relaxation (GI)

36
Q

EP3

A
  • Type: Gi/o
  • Functions:

Smooth muscle contraction (GI)

Fever

Inhibition of gastric acid secretion

Promotion of gastric mucous secretion

37
Q

EP4

A
  • Type: Gs
  • Sensitisation of nociceptors
38
Q

PGI2

39
Q

IP

A
  • Type: Gs
  • Functions:

Vasodilaton

Inhibition of platelet aggregation

40
Q

PGF2a

41
Q

FP

A
  • Type: Gq/11
  • Functions: Uterine contraction
42
Q

TXA2

43
Q

TP

A
  • Type: Gq/11
  • Functions:

Vasoconstriction

Bronchoconstriction

Platelet aggregation

Mechanism of Drug Action (Drugs) (26 decks)

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