Intro To Autonomic System Flashcards

1
Q

Which presynaptic receptor provides feedback inhibition of NE

A

alpha2 receptors

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2
Q

Inhibition of alpha 2 receptor cause

A

Increase of NE

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3
Q

Location of alpha 1 receptors

A
  1. Blood vessels of skin, viscera, kidney , salivary glands

2. Most sympathetic organs (except heart)

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4
Q

Location of alpha 2 receptors

A
Platelets
Vascular smooth muscles
Exocrine gland of pancreas
Never terminals
Fat cells
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5
Q

Beta 1 receptor location

A

Heart - + ve chronotrophic and inotrophic

kidney- increase renin production

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6
Q

Which adrenergic receptors are inhibitory(hyperpolarize)

A

Alpha 2

Beta 2

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7
Q

Which receptor binds only to epinephrine

A

Beta 2

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8
Q

Action of alpha 2 and G protein

A

G protein- Gi

  1. constriction of vasculature
  2. Inhibit lipolysis
  3. Inhibit insulin secretion
  4. Increase platelet aggregation
  5. Inhibit transmitter release
  6. Decrease secretions
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9
Q

Action of beta 2receptors G protein

A

G protein- Gs

  1. Dilation of bronchiole
  2. Dilation of blood vessels to lund and heart
  3. Lipolysis
  4. Glycogenolysis
  5. Decrease motility of GIT
  6. Tremors of skeletal muscles
  7. Relaxation of urinary bladder
  8. Increase HR and force
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10
Q

Where are beta 3 receptor found

A

Fat cells

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11
Q

Location and function of D1 receptors

A
  1. Splanchnic vessels-dilates

2. Renal vessels- dilate

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12
Q

D2 receptor location and function

A

Presynaptic nerve terminals- inhibit adenylyl cyclase

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13
Q

Mechanism of action of alpha 1

A
  1. Ligand binds
  2. Gq protein activated
  3. Activates PLC
  4. Hydeolyzes PIP2
  5. Form DAG and IP3
  6. IP3 cause increase in intracellular Ca2+
  7. Ca bind calmodulin cause phosphorylation
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14
Q

Mechanism of alpha 2

A
  1. Activation Gi
  2. Inhibits adenylyl cyclase - dec cAMP
  3. activate K+ channels or inhibit voltage gates Ca2+ channels
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15
Q

Beta receptor with least affinity

A

Beta 3 but is resistant to desensitization

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16
Q

G protein of D1

A

Gs - activates adenylyl cyclase-increase cAMP- vasodilation of renal and splanchnic vessels

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17
Q

Mechanism of D2

A

Activate Gi protein - inhibit adenylyl cyclase- dec cAMP- open K+ channels and Ca 2+ influx

18
Q

NE more potent at which receptors

A

alpha 1 and beta 3

19
Q

Phenylephrine and methoxamine have greater affinity at

A

Alpha1 more than alpha 2

20
Q

Clonidine and methylnorepinephrine greater affinity to which receptor

A

Alpha 2 greater than alpha 1

21
Q

Phenylephrine and methoxamine receptor, features, action

A
  1. Alpha 1
  2. Not a cathecol derivative
    not activated by COMPT
    Longer duration of action
  3. Vasoconstriction
22
Q

Treat hypotension, nasal congestion and cause local mydriasis

A

Phenylephrine and methoxamine

23
Q

Milodrine acts on

A

Selective alpha 1 receptor

24
Q

Effects if alpha 1 agonist

A
  1. mydriasis (ciliary muscle contact)
  2. Increased BP (arterioles and veins constrict)
  3. Piloerection
  4. Bladder sphincters contacted
25
Hypertension treatment
Presynaptic Alpha 2 agonist- Clonidine, guanabenz, guanfacine, methyldopa, moxonidine Feedback inhibition of NE release
26
Side effects of presynaptic Alpha 1 agonist
1. Drug withdrawn too quickly- withdrawal symptoms- rebound hypertension 2. Dry mouth in 50%patient 3. Sexual dysfunction in males 4. Nausea 5. Dizziness 6. Sleep disturbances
27
Clonidine acts on and effect
1. Brain stem alpha 2 receptors 2. Dec symp outflow to CVS - hypotension - bradycardia
28
Clonidine acts on and effect
1. Brain stem alpha 2 receptors 2. Dec symp outflow to CVS - hypotension - bradycardia
29
Fusion proteins
vSNARES- VAMPs ( synaptobrevin) | tSNARES- SNAPs (syntaxin, SNAP 25)
30
Enzyme that converts Acetyl CoA +choline-> Ach
Choline acetyltransferase
31
Where is Acetyl and choline got from
Acetyl CoA synthesised in mitochondria | Choline got from outside the cell transported by- choline transporter (CHT) Na dependent
32
Drugs that act on CHT
HEMICHOLINIUMS
33
Ach transported in to vesicle by
VAT (vesicle associated transport) driven by proton efflux
34
VAT anther is blocked by
Vesamicol
35
Ach in the vesicle is bound to
Negatively charged vesicular proteoglycan ( VPG)
36
Ca entering the cells interested with what protein to trigger fusion
Ca binds with VAMPs- synaptotagmin on vesicle never
37
How is Ach vesicle release blocked
Botulinum toxin cleaves 2aa from one or more SNARE proteins
38
Converts tyrosine to dopa | And drug that invite this process
Tyrosine hydroxylase | Metyrosin
39
Catecholamine enter vesicle through | This protein is blocked by
VMAT (vesicle monoamine transporter) | Reserpine
40
1. Dopa is converted to dopamine by | 2. Dopamine is converted to NE by
1. Dopa decarboxylase | 2. Dopamine-β - hydroxylase