Autonomic Drugs

Introduction to
Autonomic Pharmacology

Autonomic nervous system (ANS) is

largely independent on consciousness.
Vegatable

1
Anatomy of the Peripheral Nervous System
The
The peripheral nervous
nervous system
is divided
system intoisthe
(PNS) further
divided nervous
central into the
system
afferent (CNS) and
NS bringing
the peripheral
information from the
nervous
peripherysystem
to the CNS
(PNS).
and

efferent NS carrying
signals away from the
CNS to the peripheral
tissues.
The efferent
NS is further
divided into
the
autonomic
nervous
system (ANS)
and somatic
motor
nervous
system
 The somatic motor nervous system
innervates skeletal muscles which receive
only one efferent neuron.

precise
The ANS is further
divided into
sympathetic and
parasympathetic
nervous systems

The autonomic nervous

system innervates viscera
such as heart, smooth
muscle, and glands etc.
Target tissues receive two
types of efferent neurons,
sympathetic and
parasympathetic nerves.
Chemical Transmission in Autonomic NS
Transmitter:
Synapse:
ItIt isisthe
thejunction
chemical
of nerve
agent released
terminal from
with the next
neuron
nerveorterminaleffector that
cell,
consisting
transmitsofinformation
presynaptic
membrane, postsynaptic
across synapse and
membrane and synaptic
to
space. effectors.
pre post
Synapse
Neurotransmitter Chemistry of ANS
The classification of efferent nerves is based on the
transmitter--acetylcholine (ACh)or norepinephrine (NE)
released from their terminals.
1) Cholinergic
fibers:

It is fibers
releasing ACh
2) noradrenergic
fibers:

3) Other fibers:
 1) Cholinergic fibers include:
Cholinergic
• somatic motor fibers,
2) noradrenergic fibers: fibers:

• Most postganglionic
preganglionic sympathetic
autonomic fibers, fibers release
It is fibers
norepinephrine.
• parasympatheticThey are noradrenergic fibers.
fibers, releasing
ACh
3) Other fibers: release adrenaline, dopamine and peptides.

• a few sympathetic
postganglionic
fibers (controlling
sweat gland and
blood vessel in
skeletal muscle)

• nervous fibers

controlling adrenal

medulla.
There are ganglia between the CNS and the
effectors innervated by autonomic nerve system.

Preganglionic fiber, ganglion, postganglionic fiber

This triggers
Action the fusion of The transmitters diffuse
potential
（AP）passing
vesicles containing across the cleft and bind
down an axon to the
neurotransmitters and cell to receptors on the
axon terminal
membrane, and causes thepostsynaptic membrane
neurochemical to induce a response in
changesofmembrane
release
polarization the postsynaptic neuron.
(neurotransmitter) into the
synaptic cleft.

resulting in
Ca2+ entry into
the cell.
Chemical Transmission in synapse
 Cholinergic Transmission Choline is
transported into
ACh is the presynaptic
synthesized nerve terminal
from acetyl
by a carrier (A)
coenzyme A
(Ac-CoA) and Once
choline synthesized, ACh
through the is transported
catalytic into and
action of packaged in the
choline acetyl vesicles.
transferase
(ChAT).
 Cholinergic Transmission When an AP reaches
the terminal and
triggers influx of Ca2+
which facilitates the
After release, fusion of the vesicular
ACh bind to membrane with the
terminal membrane
and activate and results in the
pre- and release of ACh into
postsynaptic synaptic space.

acetylcholine Then, ACh is

receptors hydrolyzed rapidly
(cholinocept by acetylcholin-
or), showing esterase (AChE),
the action of terminating the
action of the
transmitter.
transmitter.
 Cholinergic
Transmission

 Fig. Action potential-

induced release of the
neurotransmitter
acetylcholine (ACh)
and its metabolism at
the neuromuscular
junction.
Adrenergic Transmission
Tyrosine is
transported actively
Norepinephrine,NE
. into the
Dopa is
noradrenergic ending
decarboxylated to
and is converted to
dopamine by
dopa by tyrosine
dopa
hydroxylase
decarboxylase.
Dopamine is
transported into the
vesicles and then
converted to NE by
dopamine-beta-
hydroxylase. In the
adrenal medulla, NE is further
converted to epinephrine.
 An action potential
causes an influx of
.
Ca2+ into the nerve
terminal, fusion of the
vesicle with the
plasma membrane
and exocytosis of NE.

The transmitter
then activates
receptors in the
postsynaptic
membrane.
 NE in the synaptic
space is actively
. reuptaken into the
nerve and the
storage vesicles
(uptake l). It is the
most important
NE penetrates
mechanism forinto
smooth cells of
termination (uptake
the 2)
and diffuses away
action.
from the receptor
site, is inactivated
by COMT (enzyme) to
normetanephrine
(NMN).
Another portion of the NE
reuptaken into the nerve is
deaminated by MAO enzyme.

NE can also
activate
presynaptic (α2)
receptors, to
inhibit further
release of NE.
Autonomic Receptors G protein-coupled receptor

Receptor: The
膜受体的最大家系 receptive
substances (protein) of a
cell that specifically bind,
肾上腺素 多巴胺
interact with ligands, and
Receptors of
5-HT M-乙酰胆碱 autonomic nerve
transmit information.
多肽类 前列腺素
阿片类 嘌呤类
system include
cholinoceptors,
adrenoceptors
第二信使
蛋白激酶A、 C、 G
and dopamine
钙调素依赖蛋白 receptors
DNA依赖蛋白激酶
 1 Cholinoceptors :
The receptors combined with ACh are classified
as muscarinic and nicotinic receptors.
 2 Adrenoceptors:
The receptors combined with NE and adrenaline
include two groups

西安交大医学院药理学系 曹永孝 yxy@xjtu.edu.cn; 029-82655140

Receptor’s Function

Most of organs are

innervated by both of
the sympathetic and
parasympathetic
nervous system.

The two systems

generally have
opposing effects.
But, they are uniform
in vivo
 3. Dopamine receptors

There are 5 subtypes of dopamine receptors.

Dl receptor is the most important. It locates in

vascular smooth muscle cells, brain etc.
It can dilate blood vessel, decrease
peripheral vascular resistance and increase
urinary volume.