Introduction to Autonomic Pharmacology Flashcards
The nervous system is divided into the
CNS and the PNS
The peripheral nervous system is subdivided into the
autonomic NS and the somatic NS
The autonomic nervous system is subdivided into the
sympathetic NS and the parasympathetic NS
Parasympathetic neurons respond to
acetylcholine
Parasympathetic neurons are called
cholinergic neurons
Sympathetic neurons are activated by
endogenous NE and Ep (adrenaline and noradrenaline)
Sympathetic neurons are known are
adrenergic neurons
Describe the anatomical pathway that sympathetic fibers take to get to their targets?
sympathetic preganglionic fibers leave the CNS through the thoracic and lumbar spinal nerves, most preganglionic nerves are short and terminate in the vertebral ganglia, the longer postganglionic sympathetic nerves then run to the tissues innervated
Sympathetic neurons are known are
adrenergic neurons
Describe the anatomical pathway that parasympathetic fibers take to get to their targets?
parasympathetic preganglionic fibers leave the CNS through the cranial nerves in the medulla, the majority of long parasympathetic preganglionic nerves terminate in ganglion cells in the walls of the organs innervated, the postganglionic paraysmpathetic nerves are short
All preganglionic nerves release what, where?
release Ach onto post-ganglionic nerves expressing nicotinic cholinergic receptors (Nn)
The somatic nerve system motor neurons release what, where?
release Ach directly onto nicotinic cholinergic receptors expressed on skeletal muscle of organs (Nm)
Parasympathetic postganglionic nerves release what?
release Ach onto organs expressing muscarinic receptors (M)
Sympathetic postganglionic nerves primarily release what?
release NE that can bind to adrenergic receptors
Sympathetic postganglionic nerves innervating the skin release
release Ach acting on muscarinic receptors on thermoregulatory sweat glands
Postganglionic nerves innervating the kidney release
release dopamine (D) to bind to dopamine D1 receptors causing vasodilation
Separate postganglionic nerves that terminate in the adrenals cause what?
the release of Epi and to a lesser extent NE into the bloodstream
The primary source of Epi that acts on the heart and blood vessels?
postganglionic nerves that terminate in the adrenals
Acetylcholine receptors found post-synaptically
M1, M3, (M4), and M5
Acetylcholine receptors that are located pre-synaptically
M2 and M4
What do M2 and M4 function as?
inhibitory autoreceptors
What is Ach released from axons metabolized by and into?
metabolized by acetylcholinesterase and butylcholinessterase into acetate and choline
What transports choline back into the synapse
choline transporter (ChT)
How does choline acetyltransferase (ChAT) reform Ach?
ChAT transfers an acetyl group from acetyl-CoA to choline to reform Ach
How does Ach get taken back up into the synaptic vesicles?
taken back up into synaptic vesicles by vesicular acetylcholine transporter (vAchT)
Epinephrine receptors found post-synaptically
alpha1, beta1, beta2
Epinephrine receptors located pre-synaptically
alpha2 and beta2
Describe the synthesis of norepinephrine (NE)
NE is formed from tyrosine which is converted by tyrosine hydroxylase into DOPA, which is converted into dopamine by aromatic amino acid decarboxylase
Dopamine is transformed into NE by
dopamine beta-hydroxylase (taken up into vesicles to be released upon stimulation)
How is NE transported back into the synapse
by the norepinephrine transporter (NET)
What are the two different things that can happen to NE in the axon?
it can either be metabolized by monoamine oxidase (MAO) into dihydroxyphenylglycol or it can be taken up into vesicles by the vesicular monamine transporter (VMAT)
How is Ach taken back up into synaptic vesicles?
by vesicular acetylcholine transporter (vAchT)
Postsynaptically, NE is metabolized by what, into what?
metabolized by catechol-methyl-transferase (COMT) into normetanephrine
How do drugs influence the ANS?
either block or activate (mimic endogenous response) the adrenergic and cholinergic receptors
Cholinergic receptors can be subdivided into
nicotinic and muscarinic receptors
Nicotinic receptors are expressed in the
ganglia, CNS and skeletal muscles
Describe nicotinic cholinergic receptors
ion channels consisting of 5 subunits
Muscarinic receptors can be divided into
Gq-coupled (M1, M3, and M5) and Gi-coupled receptors (M2 and M4)
most common and most important muscarinic receptors in the parasympathetic nervous system
presynaptic M2 and post-synaptic M3
M2 is primarily located where?
in the heart and bladder, but can also be found in certain brain regions