ANS Pharmacology Flashcards

1
Q

Major NT of parasympathetic nervous system

A

ACh

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2
Q

ACh binds what types of receptors?

A

Nicotinic (nAChR) = ionotropic

Muscarinic (mAChR) = metabotropic

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3
Q

Major NT of sympathetic nervous system

A

Norepinephrine (NE)

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4
Q

Synthesis of epinephrine only occurs where?

A

Adrenal medulla

[and in a few epinephrine containing neuronal pathways in brainstem]

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5
Q

What causes catecholamine (Epi and NE) release from the adrenal medulla?

A

Depolarization of preganglionic sympathetic neuron releases ACh, which binds nAChRs on adrenal medulla, causing release of catecholamines

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6
Q

Precursor to NE and Epi

A

Dopamine

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7
Q

Synthesis of ACh:

The choline transporter transports choline from the extracellular space into neurons and is dependent on extracellular ___ concentrations (needed for cotransport)

______ catalyzes the final step in the synthesis of ACh, which is then immediately sequestered within synaptic vesicles

A

Na+

Choline acetyltransferase (ChAT)

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8
Q

The _____-dependent ACh vesicular transporter is what transports ACh into neuronal vesicles

____ influx is what eventually promotes fusion of the vesicular and cell membranes, resulting in ACh release. The _____ protein complex is responsible for this fusion.

A

ATPase

Ca++; SNARE

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9
Q

Termination of acetylcholine signaling is done by acetylcholinesterase, which cleaves ACh into _____ and ______.

What is the fate of these two products?

A

Acetate — diffuses out of synapse

Choline — recycled into nerve terminal by choline transporter

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10
Q

Where are nicotinic vs. muscarinic ACh receptors found?

A

nAChRs are found in all ganglia (sympathetic and parasympathetic) and the adrenal medulla

mAChRs are found in smooth and cardiac muscle, gland cells, and nerve terminals (sympathetic and parasympathetic)

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11
Q

nAChRs are ligand-gated ion channels that allow ____ to pass through when activated. They are activated by both ACh and ______

A

Na+; nicotine

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12
Q

Predominant NT of the mammalian extrapyramidal system and of several mesocortical and mesolimbic neuronal pathways

A

Dopamine (DA)

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13
Q

Precursor to all catecholamines

A

Tyrosine

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14
Q

Synthesis of catecholamines and location of the steps

A

In the cytoplasm: Tyrosine —> Dopa —> Dopamine

In a vesicle: Dopamine —> NE —> Epi

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15
Q

For the storage of catecholamines, ______ transports DA into the vesicle during de novo synthesis. This transporter is relatively promiscuous and transports DA, NE, Epi, and serotonin across the vesicle membrane

A

VMAT2 (vesicular monoamine transporter)

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16
Q

The triggering event in the adrenal medulla for release of catecholamines is the release of ACh by a preganglionic fiber and its interaction with nAChRs on ____ cells to produce a localized depolarization

A

Chromaffin

17
Q

What type of receptors are alpha and beta catecholamine receptors?

A

GPCRs

18
Q

Methods of termination of catecholamine signaling

A

Reuptake

Dilution by diffusion

Metabolic transformation

19
Q

Reuptake of catecholamines occurs by what 2 neuronal membrane transporters? What happens after reuptake?

A

NET - norepinephrine transporter

DAT - dopamine transporter

After reuptake, catecholamines are stored in vesicles by VMAT-2

20
Q

Catecholamine signal termination by dilution/diffusion out of junctional cleft involves uptake at extraneuronal sites by the transporters ___, ___, and ____

A

ENT, OCT1, OCT2

21
Q

Termination oc catecholamine signaling by metabolic transformation occurs by what 2 enzymes?

A

MAO — metabolizes catecholamines that have been released and undergone reuptake within the nerve terminal; associated with outer surface of mitochondria

COMT — major role in the liver; largely cytoplasmic

22
Q

End result of adrenergic alpha-1 receptor activation

A

Muscle contraction

[vasoconstriction, glandular secretion]

23
Q

End result of adrenergic alpha-2 receptor activation

A

Vascular smooth muscle contraction
Decreased insulin secretion
Decreased release of NE

24
Q

Activation of any of the ____ catecholamine receptors results in activation of adenylyl cyclase and increased concentrations of cAMP through the stimulatory Gs protein

A

Beta

25
Q

End result of adrenergic beta-1 receptor activation, which are mainly found in myocardium

A

Increased force and rate of heart contraction and AV nodal conduction velocity

26
Q

End result of adrenergic beta-2 receptor activation, which are found on smooth muscle and most other sites

A

Vascular, bronchial, GU, and GI smooth muscle relaxation

27
Q

End result of adrenergic beta-3 receptor activation, which are found only in adipose tissue

A

Lipolysis

28
Q

Dopamine receptors are what type of receptors?

A

GPCRs

29
Q

Result of stimulation of D1 receptors

A

Vasodilation
Natriuresis
Diuresis

30
Q

Agonists of alpha1 receptors

A

Epi>NE

31
Q

Agonists at alpha2 receptors

A

Epi>NE

32
Q

Agonists at beta1 receptors

A

Epi=NE

33
Q

Agonists at beta2 receptors

A

Epi»NE

34
Q

Agonists at beta3 receptors

A

NE>Epi

35
Q

In response to a variety of stimuli, such as ACh, vasoactive products like bradykinin, or physical stimuli, blood vessel endothelial cells release a short-lived vasodilator called _________, which is now known as NO

A

Endothelium-derived relaxing factor (EDRF)

36
Q

Effects of EDRF release

A

EDRF release leads to ACh release, which activates mAChR on endothelial cells, leading to their dilation

37
Q

Parasympathetic cholinergic effects

A
Salivation
Lacrimation
Pupil constriction
Decrease HR
Urination
Increased secretions
Increased GI motility
38
Q

Sympathetic (adrenergic) effects

A
Pupil dilation
Increased HR
Urinary retention
Decreased secretions
Decreased GI motility