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Section 6 - (PT2) Drugs Affecting the Autonomic Nervous System
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Category: Pharmacology
Type: Lecture Notes
Tags: noradernergic, muscle, contraction, neuron, activation, smooth, treat, adrenoreceptors, drugs, effect, inhibits, biosynthesis, adrenaline, synaptic, noradrenergic, action, receptors, inhibitors, depression,
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Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
w
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
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Second level
Third level
Fourth level
Fifth level
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Action Potential
Na
Target Cell
acetylcholine
Preganglionic neuron
Postganglionic neuron
AKA Noradrenergic Neuron
Nicotinic acetylcholine
receptor
Depolarization and possible
Action Potential
noradrenaline
Sympathetic System
Pre Synaptic
Nerve terminal
NA
NA
NA
Reserpine
NA
NA
Cocaine
amphetamines
Post Synaptic
Cell
U1
NA
Metabolite
MAO
U2
MAO
inhibitors
Normetan-
ephrine
GP
PLC
IP3
Ca2
Ca2
Ca2
NA
Contraction
ER or SR
1
Activate PLC and increase IP3
Involved in smooth muscle contraction vasoconstriction (Stimulatory)
NA
GP
AC
1
PK
Ca2
Ca2
cAMP
Contraction
Activate AC and increase cAMP formation
Increase heart rate and force of contraction (Stimulatory)
NA
GP
AC
2
PK
cAMP
Acts to reduce muscle
contraction
Activate AC and increase cAMP formation
In smooth muscle, cAMP activates enzymes (protein kinase) that reduce contraction (Inhibitory)
GP
PLC
IP3
Ca2
Ca2
Ca2
Lig
Contraction
ER or SR
NA
GP
AC
1
PK
Ca2
Ca2
cAMP
NA
GP
AC
2
PK
cAMP
Acts to reduce muscle
contraction
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Drugs Affecting Noradrenergic Transmission
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
.
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
GP
PLC
IP3
Ca2
Ca2
Ca2
NA
Contraction
ER or SR
1
Activate PLC and increase IP3
Involved in smooth muscle contraction vasoconstriction (Stimulatory)
3
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
@
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
NA
GP
AC
2
PK
cAMP
Acts to reduce muscle
contraction
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
NA
GP
AC
2
PK
cAMP
Acts to relax SM
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
NA
GP
AC
2
PK
cAMP
Acts to relax SM
Activate AC and increase cAMP formation
In smooth muscle, cAMP activates enzymes (protein kinase) that cause SM relaxation (Inhibitory)
3
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and
cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
Pre Synaptic
Nerve terminal
NA
NA
NA
Reserpine
0
Principles of Pharmacology and Toxicology (BIOL3020)
Noradernergic Transmission
Adrenaline Biosynthesis
Adrenaline Biosynthesis
Noradernergic Neuron
Noradrenaline is then transported to vesicles
Vesicles are loaded by transporters
Drugs such as reserpine block this transport and
cause nerve terminals to become depleted of NA.
Used to treat hypertension
Noradernergic Neuron
NA is also taken up by both presynaptic neuron and post synaptic cell
Uptake transporters can be inhibited by drugs
NA is metabolized by monoamine oxidase (MAO)
MAO inhibitors treat depression
Noradernergic Receptors
Drugs that effect Adrenoreceptors
Drugs that effect other adrenoreceptors
Putting it together
Drugs Affecting Noradrenergic Transmission
Some General Rules
Smooth muscle contraction is via activation of Phospholipase C
Cardiac muscle contraction is via Adenylate Cyclase activation
This opposes the action of the M2 mAChR that inhibits AC
In Smooth muscle activation of AC inhibits contraction
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