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Flashcards in Receptors/Ligands/CNS Deck (32):
1

antagonistic cathecholamine

Beta adrenergic blocker

2

what kind of receptor is α1 ?

Gq

activates phospholipase C (PLC)

second messenger: IP3 and DAG

effect: elevated PKC and free Ca++

 

3

Syntetic agonist cathecholamine 

Isoprotenerol (Isuprel, Medihaler-Iso)

Dobutamine

4

what are the main areas where you can find serotonin receptors

wall of interstine

blood

CNS

5

alpha 1 (α1) activation

  • peripheral blood vessels (smooth muscle) → vasoconstriction
  • heart → increased force of contraction (synergistic wih Beta 1)
  • gut → relaxation of muscles
  • sphincters (smooth muscle) → contraction

 

  • bronchi (smooth muscle)→ contraction
  • iris (radial mucle)→ contraction → mydriasis (dilation of pupil)
  • prostate and uterus → contraction
  • pancreas → decrease insulin secretion (opposite of beta 2)

6

activation of dopaminergic 2 receptors

presynaptic:

  • inhibition of NE release
  • nausea and vomiting (affecting the stomach, nucleus tractus solitarus, chemoreceptor trigger zone)

postsynaptic:

  • constriction
    • stomach contraction = vomiting

7

what serotonin receptors do we target pharmacologically?

the CNS ones

8

ß receptor cathecholamine affinity

isoprotenerol > epi > norepi 

(ß2 - no response to norepi)

9

which receptor does not react to neorepinephrine?

Beta 2 receptor

10

postsynaptic α2 receptor activation

  • coronaries → constriction
  • CNS → sedation and analgesia (via decreased SNS outflow from brainstem)
  • platelets → aggregation

11

what kind of receptor is α2 ?

Gi

inactivates adenyl cyclase

decreases cAMP and increases K+ conductivity

12

what kind of organic compounds are cathecholamines?

mono-amines

has catechol - a benzene with 2 hyroxyl side groups 

13

where do you find dopaminergic 1 receptors?

postsynaptic in:

  • renal smooth muscle
  • mesenteric smooth muscle
  • splenic smooth muscle
  • coronary vessel smooth muscle
  • cerebral blood vessels

14

presynaptic α2 receptor activation

  • peripheral vascular smooth muscle → vasodilation (if you inhibit the inhibition of adenyl cyclase you end up with more cAMP)
  • coronaries→ vasodilation
  • adrenergic and cholinergic nerve terminals → inhibits NE release → inhibits sympathetic outflow → decerased BP and HR
  • inhibits CNS activity
  • GI tract→ relaxation

15

α receptor cathecholamine affinity 

norepi > epi > isoprotenerol

16

who makes catecholamines?

neurons and adrenal gland

17

what type of receptor is dopaminergic 1 receptor?

Gs

activates adenyl cyclase

increased cAMP

18

what type of receptor is dopaminergic 2 receptor?

Gi

inhibits adenyl cyclase

decreased cAMP

19

natural agonist cathecolamines

Epi

Norepi

Dopamine

20

What kind of receptor is the serotonin receptor?

5-hydroxytryptamine receptors or 5-HT receptors

there are at least 14 subtypes - different kinds of receptors, different functiomn, all over the body

some are GPCR and some are ligand-gated ion channels

21

where do you find dopaminergic 2 receptors?

presynaptic

  • nerve endings
  • CNS (nucleus tractus solitarus, chemoreceptor trigger zone)

postsynaptic

  • smooth muscle

22

beta 2 activation

  1. bronchial (smooth muscle) → bronchodilation 
  2. vascular (visceral smooth muscle) → vasodilation 
  3. GI, GU (visceral smooth muscle) → decreased motility, delayed digestion, contract sphincters
  4. uterine (visceral smooth muscle) → relaxation (inhibits labor)
  5. skin (smooth muscle)
  6. mast cells  → decreased histamine release
  7. myocardium → increased atrial contractility, increased HR (but less than ß1)
  8. coronaries → vasodilation
  9. kidneys → delay micturition; release renin
  10. skeletal muscle → vasodilation and increased Kuptake
  11. liver  → glycogenolysis and gluconeogenesis
  12. pancreas → increased insulin secretion
  13. adrenergic terminal → increased release of NE

23

activation of dopaminergic 1 receptors

vasodilation

 

  • renal smooth muscle
  • mesenteric smooth muscle
  • splenic smooth muscle
  • coronary vessel smooth muscle
  • cerebral blood vessels

24

where do you find beta 2 receptors?

  1. bronchial (smooth muscle)
  2. vascular (visceral smooth muscle)
  3. GI, GU (visceral smooth muscle)
  4. uterine (visceral smooth muscle)
  5. skin (smooth muscle)
  6. mast cells
  7. myocardium
  8. coronaries
  9. kidneys
  10. skeletal muscle
  11. liver
  12. pancreas
  13. adrenergic terminal

25

where is α1 found?

Postsynaptic in 

  • peripheral blood vessels (smooth muscle)
  • heart
  • gut - sphincters (smooth muscle)
  • glands

 

  • bronchi (smooth muscle)
  • iris (radial mucle)
  • prostate and uterus
  • pancreas

26

dopamine receptor affinity?

dopamine ONLY

)no other catecholamines)

27

 what kind of receptors are  beta 1 receptors?

Gs

activation of adenyl cyclase

increased cAMP

28

what kind of receptors are  beta 2 receptors?

Gs

activation of adenyl cyclase

increased cAMP

29

where do you find beta 1 receptors?

  • myocardium
  • SN node
  • ventricular conduction system
  • coronaries
  • kidneys

30

where is postsynaptic α2 receptor found?

  • coronaries
  • CNS
  • platelets

31

beta 1 activation

  • myocardium → increased inotropy
  • SN node → increased chronotropy 
  • ventricular conduction system → increased conduction velocity
  • coronaries → relaxation
  • kidneys → renin release

32

where is presynaptic α2 receptor found?

  • peripheral vascular smooth muscle 
  • coronaries
  • brain (especially in brainstem - adrenergic and cholinergic nerve terminals)
  • GI tract