DSA | Autonomic Pharmacology (Kruse) Flashcards

1
Q

What is the major neurotransmitter of the parasympathetic nervous system?

What are the receptors?

A

ACh

nAChR, mAChR

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2
Q

What is the major neurotransmitter of the sympathetic nervous system?

What are the receptors?

A

NE, Epi, DA, ACh

Receptors: alpha, beta, (D), nAChR, mAChR

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3
Q

Acetylcholine

Cholinergic/Adrenergic?

A

Cholinergic

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4
Q

Norepinephrine

Cholinergic/Adrenergic?

A

Adrenergic

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5
Q

Epinephrine

Cholinergic/Adrenergic?

A

Adrenergic

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6
Q

What is the major neurotransmitter of the PNS vs the SNS?

A

PNS : Acetylcholine

SNS: Norepinephrine

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7
Q

What is the precursor to NE and Epi?

A

Dopamine

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8
Q

Synthesis of epinephrine only occurs in __________

A

The adrenal medulla

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9
Q

Describe the basics of cholinergic neurotransmission

A
  1. ACh synthesis
  2. ACh storage
  3. ACh release
  4. ACh destruction
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10
Q

nACHR (ionotropic)

Tissue location:

Function:

Agonists:

A

Tissue location: CNS, Autonomic Ganglia, Adrenal medula

Function: Excitatory, release of catecholamines

Agonists: ACh, Nicotine

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11
Q

mAChR (metabotropic)

Tissue location:

Function:

Agonists:

A

Tissue location: CNS, Autonomic ganglia, effector organs, sweat glands

Function: Excitatory and inhibitory, sweat secretion

Agonists: ACh, Muscarine

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12
Q

M1

Location

Structural Features

Mechanism

A

Location: CNS, ganglia

Structural Features: GPCR, Gq/11

Mechanism: Actication of PLC, IP2, DAG cascade

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13
Q

M2

Location

Structural Features

Mechanism

A

Location: Heart, nerves, smooth muscle

Structural Features: GPCR, Gi/o

Mechanism: Inhibition of adenylyl cyclase (AC); decreases cAMP production, activation of K+ channels

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14
Q

M3

Location

Structural Features

Mechanism

A

Location: Glands, smooth muscle, endothelium

Structural Features: GPCR, Gq/11

Mechanism: Activation of PLC, IP3, DAG cascade

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15
Q

M4

Location

Structural Features

Mechanism

A

Location: CNS

Structural Features: GPCR, G i/o

Mechanism: Inhibition of AC, decrease cAMP production, activation of K+ channels

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16
Q

M5

Location

Structural Features

Mechanism

A

Location: CNS

Structural Features: GPCR, Gq/11

Mechanism: Activation of PLC, IP3, DAG cascade

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17
Q

Nm

Location

Structural Features

Mechanism

A

Location: Skeletal muscle neuromuscular junction

Structural Features: Ligand gated ion channel

Mechanism: N+, K+ depolarizing ion channel

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18
Q

Nn

Location

Structural Features

Mechanism

A

Location: Postganglionic cell body, Dendrites, CNS

Structural Features: Ligand gated ion channel

Mechanism: N+, K+ depolarizing ion channel

19
Q

Describe the basic mechanism of the adrenergic nerve terminal

A
  1. Synthesis
  2. Storage
  3. Release
  4. Reuptake
20
Q

What is the precursor for all catecholamines?

A

Tyrosine

21
Q

Describe the pathway how Epinephrine is created

A

Tyrosine –> DOPA –> Dopamine –> Norepinephrine –> Epinephrine

22
Q

What transports Tyrosine into the nerve terminal?

A

Na+ dependent tyrosine transporter

23
Q

What transports NE, Epi, DA and serotonin into vesicles?

A

Vesicular monoamine transporter (VMAT - 2)

24
Q

What imports NE into the nerve terminal?

A

NE Transporter (NET)

25
Q

What drug blocks NE transporters (NET)?

A

Cocaine

*increases concentration of NE in the synapse

26
Q

What is the major mechanism used to terminate actions of catecholamines?

A

Reuptake into the nerve terminals via

NET (norepinephrine transporter) and DAT (dopamine transporter)

27
Q

After reuptake, catecholamines are stored in vesicles by the _______

A

VMAT-2

28
Q

What is the secondary method of terminatng actions of catecholamines?

A

Metabolism (2 enzymes)

Monoamine oxidase (MAO)

Catechol-O-methyltransferase (COMT)

29
Q

Alpha receptors exhist as ___ subtypes

A

2

Alpha1, Alpha2

30
Q

Beta receptors exhist as ___ subtypes

A

3

B1, B2, B3

31
Q

Dopamine receptors exhist as ___ subtypes

A

5

D1, D2, D3, D4, D5

32
Q

Alpha1

G protein and effectors:

Agonists:

Tissue:

Responses:

A

G protein and effectors: Gq

Agonists: Epi, NE

Tissue: Vascular, Liver, Heart

Responses: Contraction

33
Q

Alpha 2

G protein and effectors:

Agonists:

Tissue:

Responses:

A

G protein and effectors: Gi, Go

Agonists: Epi > NE

Tissue: Pancreatic islets

Responses: Decreased insulin secretion

34
Q

Beta 1

G protein and effectors:

Agonists:

Tissue:

Responses:

A

G protein and effectors: Gs

Agonists: Epi=NE

Tissue: Juxtaglomerular cells, Heart

Responses: Increased Renin secretion

35
Q

Beta 2

G protein and effectors:

Agonists:

Tissue:

Responses:

A

G protein and effectors: Gs

Agonists: Epi >>> NE

Tissue: Smooth muscle, skeletal muscle

Responses: Relaxation, Glycogenolysis

36
Q

Beta3

G protein and effectors:

Agonists:

Tissue:

Responses:

A

G protein and effectors: Gs

Agonists: NE > Epi

Tissue: Adipose tissue

Responses: Lipolysis

37
Q

RULES OF THUMB FOR SMOOTH MUSCLE and AUTONOMIC RECEPTORS

Alpha1 receptors?

A

Activation causes:

Stimulate contraction of all smooth muscle

VASOCONTRICTION

38
Q

RULES OF THUMB FOR SMOOTH MUSCLE and AUTONOMIC RECEPTORS

Beta2?

A

Actiavation causes:

Smooth muscle relaxation; vasodilation

39
Q

RULES OF THUMB FOR SMOOTH MUSCLE and AUTONOMIC RECEPTORS

Muscarinic?

A

Activation causes:

Contract smooth muscle

(different intracellular signal than alpha1 receptor)

40
Q

Smooth muscle of blood vessels is ____ innervated by parasympathetic neurons

A

NOT

41
Q

Epi and NE release is triggered by…

A

The release of ACh from the preganglionic fibers

42
Q

_________ reflex is an example of compensatory changes in the ANS

A

Baroreceptor reflex

43
Q
A