Introduction to Autonomic Pharmacology Flashcards

1
Q

list the 4 main processes ANS regulates

A
  • smooth muscle contraction / relaxation
  • ALL exocrine secretions; certain endocrine secretions
  • heartbeat
  • certain steps in intermediary metabolism
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2
Q

SNS responds to the following situations (or stresses on the body)…

A
  • trauma
  • fear
  • hypoglycemia
  • cold
  • exercise
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3
Q

SNS stimulation effects on:

(1) HR, BP
(2) energy metabolism
(3) blood flow/distribution
(4) pupils
(5) bronchioles

A

1- inc HR, inc BP
2- inc mobilization of energy stores, glycogenolysis and fat stores
3- divert blood from skin and internal organs –> skeletal muscle and heart
4- mydriasis (pupil dilation)
5- bronchiole dilation

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4
Q

PSNS is important in (1) functions and having (2) towards the SNS.

A

(rest and digest)
1- maintain essential bodily functions: digestion, elimination of waste
2- oppose/balance SNS actions

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5
Q

heart is mainly under (SNS/PSNS) control

BP is mainly under (SNS/PSNS) control

A

Heart- PSNS (M2 AChR, Gi)

BP (vasculature, α1, Gq)- SNS

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6
Q

list the areas only innervated by the SNS

A
  • adrenal medulla
  • kidney
  • pilomotor muscles
  • sweat glands
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7
Q

list the neuronal fibers that release ACh

A
  • all preganglionic efferent ANS fibers
  • all PSNS postganglionic fibers
  • all somatic motor fibers to skeletal muscle
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8
Q

list the neuronal fibers that release NE

A

MOST postganglionic SNS fibers (exceptions: postganglionic sweat glands ACh is released, postganglionic kidney mostly DA is released, adrenal medulla is postganglionic to release Epi./NE)

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9
Q

Renal vascular smooth muscle is innervated by (SNS/PSNS/both) with postganglionic fibers releasing (2)

A

1- SNS

2- Dopamine (mostly)

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10
Q

adrenal medulla is special because it is innervated by (1) and responds to (2) neurotransmitter to release (3)

A

1- preganglionic SNS fibers
2- ACh (AChN receptors)
3- Epi (80%), NE (20%)

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11
Q

sweat glands are innvervated by (SNS/PSNS/both) with postganglionic fibers releasing (2) onto (3) receptors

A

1- SNS
2- ACh
3- ACh-M3

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12
Q

all preganglionic ANS fibers release (1) to postganglionic neurons with (2) receptors

A

1- ACh

2- AChN(n)

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13
Q

list the steps for the formation and release of ACh from neuron

A

1a) Na+/choline CHT1 symporter on axonal membrane into cytoplasm
1b) acetyl CoA from mitochondria into cytoplasm
2) choline + acetyl CoA –> ACh via ChAT enzyme
3) ACh into vesicle via VAChT antiporter; H+ out
4) Ca++ influx stimulates ACh vesicle release at synaptic membrane
5) ACh breakdown in synapse by AChE –> acetyl CoA + choline

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14
Q

in the release of ACh, presynaptic membranes will have (1) receptors for ACh in order to (2)

A

1- M2 receptors (Gi)

2- inhibit ACh release (via Ca++, negative feedback)

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15
Q

Describe the following:

(1) ChAT
(2) CHT1
(3) VAChT

A

1- choline acetyltransferase, forms ACh from choline + acetyl CoA
2- choline transporter, axonal choline-Na+ symporter into pre-ganglionic neuron
3- vesicular ACh transporter, ACh into vesicles in exchange for H+

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16
Q

list the steps for NE formation and release form neuron

A

1) Tyr influx via System L on axonal membrane
2) Tyr -(rate-limiting)-> DOPA –> DA
3) DA into vesicle via VMAT antiporter; H+ out
4) DA –> NE w/in vesicle
5) Ca++ influx stimulates NE vesicle release into synapse
6) NE reuptake via NET, or NE diffusion away from synapse

17
Q

in the release of NE, presynaptic membranes will have (1) receptors for NE in order to (2)

A

1- α2 adrenergic receptors (Gi)

2- inhibit NE release (via Ca++, negative feedback)

18
Q

Describe the following:

(1) COMT
(2) MAO
(3) NET
(4) System L
(5) VMAT

A

1- catechol-O-methyltransferase for NE/Epi breakdown (mitochondria)
2- monoamine oxidase for NE/Epi. breakdown (ER)
3- norepinephrine transport, reuptake NE into presynaptic neuron
4- for Tyr influx
5- vesicular monoamine transporter, for DA into vesicles for NE conversion

19
Q

AChR-N receptors come in type (1) and (2). They bind to (3) ACh molecules to allow (4) to occur. [include the locations for (1)/(2)]

A

1- Nm (muscle type- at skeletal NMJ)
2- Nn (neuronal type- ANS postganglionic cells, adrenal medulla, brain)
3- 2 ACh
4- Na+ influx => depolarization
(nicotinic receptors are ION channel linked)

20
Q

AChR-M receptors are (1) type receptors with the following different types: (2), (3), (4). They are found on the following: (5).

A
1- G protein coupled receptors
2- M1 (Gq)
3- M2 (Gi)
4- M3 (Gq)
5- organs with PSNS innervation, sweat glands (SNS), some cells in CNS
21
Q

activation of cardiac M2 has the following end result

A

(Gi- note that β/γ subunits are the direct actors, not α subunit)
K+ efflux (via K+ channel) => hyperpolarization

22
Q

list the M1 locations (and functions)

A

(Gq)

  • ganglia (depolarization)
  • CNS (inc cognitive function)
  • vomiting center (emesis)
23
Q

list the M2 locations (and functions)

A

(Gi)

  • heart/atria (cardiac inhibition)
  • presynaptic nerve terminals (inhibits ACh release, neg. feedback)
24
Q

list the M3 locations (and functions)

A

(Gq)

  • smooth muscle (contraction)
  • secretory glands (secretion)
  • vascular endothelium (vasodilation, via NO on vascular smooth muscle)
25
Q

describe the function of M3 on vascular endothelial cells

A

(uninnervated M3 receptors- Gq)

1) M3 activation => inc Ca –> activates endothelial NO synthase => NO formation
2) NO diffusion to adjacent vascular smooth muscle (vessel wall)
3) NO activates guanylyl cyclase => GTP –> cGMP
4) cGMP activates cGMP-dependent protein kinase –> phosphorylation of proteins => smooth muscle relaxation = vasodilation

26
Q

describe Epi/NE binding among β-adrenergic receptors

A

(all Gs)
β1/β3: equal Epi/NE affinity
β2: Epi affinity&raquo_space; NE [i.e. skeletal muscle vasculature responds well to circulating Epi.)

27
Q

α1/β1 adrenergic receptors are generally found in (1)

α2/β2 adrenergic receptors are generall found in (2)

A

1- (Gq, Gs) adrenergic nerve terminals

2- (Gi, Gs) remote from adrenergic nerve terminals (preferential to circulating Epi)

28
Q

list the β1 locations (and functions)

A

(Gs)

  • heart (inc HR, force of contraction, AV conduction velocity)
  • juxtaglomerular cells (renin release)
  • adipocytes (inc lipolysis)
29
Q

list the β2 locations (and functions)

A

(Gs)

  • smooth muscle (relaxation)
  • skeletal muscle (inc glycogenolysis, inc K+ uptake)
  • pancreatic β-cells (inc insulin secretion, less effect than α2 dec secretion)
  • pancreatic α-cells (inc glucagon secretion)
  • liver (inc glycogenlysis, gluconeogenesis)
  • adipocytes (inc lipolysis)
30
Q

list the β3 locations (and functions)

A

(Gs)

adipocytes (inc lipolysis)- generally limited and unclear function

31
Q

list the α1 locations (and functions)

A

(Gq)

  • vascular smooth muscle (contraction)
  • GU smooth muscle (contraction- no urination)
  • liver (inc glycogenolysis, gluconeogenesis)
32
Q

list the α2 locations (and functions)

A

(Gi)

  • presynaptic terminals (inhibit NE release, neg. feedback)
  • platelets (aggregation)
  • adipocytes (lipolysis inhibition)
  • pancreatic β-cells (dec insulin secretion- larger effect than β2 inc secretion)
  • vascular smooth muscle (contraction)
33
Q

DA receptors important in the ANS are (1) and (2) found in (3) which functions to (4)

A

1/2- D1, D5 (inc cAMP)
3- smooth muscle of renal vasculature bed
4- relaxation

34
Q

vasculature (arterioles, veins) are predominant with ____ receptors

A

α1-adrenergic receptors (Gq)

35
Q

list the areas that predominantly have M3 receptors

A

(Gs)

  • ciliary muscle (lens focusing)
  • GI tract (peristalsis)
  • urinary bladder (contraction => urination)
  • salivary glands (inc secretion)
  • sweat glands (although SNS, inc secretion)