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CPR Test 2 > Introduction to Pharmacology of the autonomic nervous system > Flashcards

Introduction to Pharmacology of the autonomic nervous system Flashcards

1
Q

what are some examples of drug targets found in the body?

A

Proteins:

  • Hormone Growth Factor
  • Growth factors
  • Transcription factor receptors
  • Nerurotransmitter receptors
  • Ion channerls
  • Enzymes
  • Transport proteins
  • Enzymes
  • Transport proteins
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2
Q

what are the main neurotransmitters, and receptors for the parasympathetic Nervous system

A

Neurotransmitter: ACh

Receptors: nAChR, mAChR

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3
Q

What are the main neurotransmitters and receptors for the sympatheric nervous system

A

Neurotransmitters: NE>Epi (DA); ACh

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

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4
Q

where is the Acetylcholine Neurotransmitter found in the ANS

A
  • Major neurotransmitter of the PNS
  • All preganglionic autonomic fibers
  • All postganglionic parasympathetic fibers
  • Few postganglionic sympathetic fibers (sweat glands)
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5
Q

where is the Norepinephrine (adrenergic) neurotransmitter found in the ANS

A
  • Major neurotransmitter of the sympathetic nervous system

- Vast majority of postganglionic sympathetic fibers

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6
Q

where is the Epinephrine neurotransmitter found in the ANS

A

Synthesis only occurs in the adrenal medulla and in a few epinephrine containing neuronal pathways in the brain stem

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7
Q

where is Dopamine found in the ANS

A

NE and Epi precursor

-acts on the CNS and the renal vascular smooth muscle

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8
Q

Review of the cholinergic neurotransmitter

A

1) choline enters the cell and combines with AcCoA
- choline can get blocked by Hemicholinium

2) ACh is packaged into Vesicles for storage and transport
- can be blocked via Vesamicol

3) ACh is released into the synapse via VAMPS and SNAPS when the Action potential comes and an enter of Ca into the cell
- release of ACh can be blocked by Botulinium Toxin

4) Ach destruction via acetylcholinesterase

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9
Q

Receptor, Tissue Location, Function, and Agonists of the nAChR

A

ionotropic,

Tissue Location: CNS

  • Autonomic ganglia (Nn)
  • Adrenal medula for sympathetic NS

Function: Excitatory
-release of catecholamines for SNS

Agonists:
Acetylcholine, Nicotine

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10
Q

Receptor, Tissue Location, Function, and Agonists of the mAChR

A

metabotropic

Tissue Location: CNS

  • Autonomic ganglia
  • Effector organs (cardiac and smooth muscle, gland cells, nerve terminals)
  • Sweat glands for the SNS

Function: Excitatory and inhbitory

Agonists: Acetylcholine
muscarinic

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11
Q

Cholinergic Receptors, Location, Structural Features, Mechanism: M1

A

Receptor Type: M1

Location: CNS, ganglia

Structural Features: GPCR, Gq/11

Mechanism: Activation of Phospholipase C; IP3; DAG cascade

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12
Q

Cholinergic Receptors, Location, Structural Features, Mechanism: M2

A

Receptor Type: M2

Location: Heart, nerves, Smooth muscle

Structural Features: GPCR, Gi/o

Mechanism: Inhibition of adenyl cyclase decrease in cAMP production, activation of K+ channels

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13
Q

Cholinergic Receptors, Location, Structural Features, Mechanism: M3

A

Receptor Type: M3

Location: Glands, Smooth muscle, endothelium

Structural Features: GPCR, Gq/11

Mechanism: Activation of PLC; IP3; DAG cascade

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14
Q

Cholinergic Receptors, Location, Structural Features, Mechanism: M4

A

Receptor Type: M4

Location: CNS

Structural Features: GPCR, Gi/o

Mechanism: Inhibition of AC; decrease in cAMP and activation of K+ channels

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15
Q

Cholinergic Receptors, Location, Structural Features, Mechanism: M5

A

Receptor Type: M5

Location: CNS

Structural Features: GPCR, Gq/11

Mechanism: Activation of PLC; IP3; DAG cascade

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16
Q

Cholinergic Receptors, Location, Structural Features, Mechanism Nm

A

Receptor Type: Nm

Location: Skeletal muscle neuromuscular junction

Structural Features: Ligand gated ion channel

Mechanism: N+, K+ depolarizing ion channel

17
Q

Cholinergic Receptors, Location, Structural Features, Mechanism Nn

A

Receptor Type: Nn

Location: Postganglionic cell body, dendrites, CNS

Structural Features: Ligand gated ion channel

Mechanism: N+, K+ Depolarizing ion channel

18
Q

How does catecholamines synthesis occurs and in what locations?

A

Tyrosine to DOPA to Dopamine
-occurs in the nerve cytoplasm

Dopamine to Norepinephrine to eninephrine
-Occurs in the vesicle

Norepinephrine to epinephrine
-occurs mainly in the adrenal medulla

19
Q

Synthesis, Storage, release, reuptake of Catecholamines

A

Na+ dependant tyrosine transporter
-transports tyrosine into the nerve terminal

Vesicular Monomine transporter (VMAT-2)

  • Transports NE, Epi, DA and serotonin into the vesicles
  • can be blocked via reserpine
  • release upon action potential and Ca+ influx

NE tranporter (NET)

  • IMports NE into the nerve terminal
  • DAT imports DA into the nerve termina
20
Q

Termination of the catecholamine signaling:

A

Reuptake into the nerve terminals

  • Major mechanism that terminates catecholamines
  • NET and DAT
  • After reuptake, catecholamines are stored in vesivles by the VMAT-2

Metabolism of catecholamines (2 main enzymes)

  • Monoamine oxidase (MAO)
  • Catechol-O-methyltransferase (COMT)

degradative enzymes is nonexistent in adrenergic signaling

21
Q

Receptor, G protein and effectors, Agonists, Tissue, Responses of: Alpha 1 adrenergic receptors

A

Receptor: Alpha 1

Gprotein: Gq, increase in phospholipase C; IP3; DAG to increase intracellular Ca

Agonist: Epi>NE

Tissue: Vascular, GU smooth muscle, liver, intestinal smooth muscle, heart

Responses: Contraction, GLycogenolysis, gluconeogenesis, hypepolarization and relaxation, increased contractile force; arrythmias

22
Q

Receptor, G protein and effectors, Agonists, Tissue, Responses of: Alpha 2 adrenergic receptors

A

Receptor: Alpha 2

Gprotein: Gi, decrease in adenyl cyclase, decrease in cAMP

Agonist: Epi>NE

Tissue: Pancreatic islets, platelets, nerve terminals, vascular smooth muscle

Responses: Decreased insulin secretion, aggregation, decreased release of NE, contraction

23
Q

Receptor, G protein and effectors, Agonists, Tissue, Responses of: Beta 1 adrenergic receptors

A

Receptor: Beta 1

Gprotein: Gs, increase adenyl cyclase, increase cAMP, increase of L type Ca channels

Agonist: Epi=NE

Tissue: Juxtaglomerular cells, Heart

Responses: increased renin secretion, increased force and rate of contraction of AV nodal and conduction velocity

24
Q

Receptor, G protein and effectors, Agonists, Tissue, Responses of: Beta 2 adrenergic receptors

A

Receptor: Beta 2

Gprotein: Gs, increase adenyl cyclase, increase cAMP, increase of L type Ca channels

Agonist: Epi»NE

Tissue: Smooth muscle (vascular, bronchial, GI, GU)
Skeletal muscle

Responses: Relaxation
Glycogenolysis, uptake of K+

25
Q

Receptor, G protein and effectors, Agonists, Tissue, Responses of: Beta 3 adrenergic receptors

A

Receptor: Beta 3

Gprotein: Gs, increase adenyl cyclase, increase cAMP, increase of L type Ca channels

Agonist: Epi>NE

Tissue: Adipose tissue

Responses: Lipolysis

26
Q

what is the preference of Epinephrine and Norepinephrine to adrenergic receptors

A

Epinephrine (a1 = a2, B1 = B2)

Norepinephrine (a1 = a2, B1&raquo_space;B2)

27
Q

Rule of thumb for the Alpha 1 receptors

A
  • Stimulate contraction of all smooth muscle
  • Vascular smooth muscle: vasoconstriction

if inhibit theses than the opposite happens

28
Q

Rule of thumb for the Beta 2 receptors

A

Relax smooth muscle = vasodilation

if inhibit these the opposite happens

29
Q

Rule of thumb for the Muscarinic receptors

A

Contract smooth muscle (different intracellular signal than a1 receptors)

inhibit these the opposite will happen

30
Q

How is that there is no Parasympathetic innervation to blood vessels but, parasympathetic activity causes vasodilation?

A

due to the parasympathetic innervation to the endothelium which releases NO causing vasodilation

31
Q

Response of Blood vessels to autonomic nerve impulses

A

Sympathetic = constriction

parasympathetic: indirectly causues vasodilation by telling endothelium to release NO

32
Q

How is the Adrenal Medulla innervated and what neurotransmitter/ receptor does it?

A

Sympathetic innervation

  • Epi and NE release is triggered by the releaseof ACh from the preganglionic fibers
  • Ach binds to NnAChRs and produce a localized depolarization

releases 80 percent Epi and 20 percent NE

33
Q

Cholinomimetic Agents?

A

drugs that mimic ACh

  • AChR agonists
  • Acetylcholinesterase inhibitors
34
Q

Colinoreceptor - blocking drugs

A

AChR antagonists

35
Q

Sympathomimetic agents

A

Drugs that mimic or enhance alpha and B receptor stimulation

-Agonists that enhance catecholamine release, drugs that block reuptake

36
Q

Adrenoreceptor-blocking drugs

A

alpha and beta antagonists

CPR Test 2 (25 decks)

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