Adrenergic Receptors

Adrenaline is the original name for what we now call epinephrine.

Stimulation of the adrenal medulla by the sympathetic nervous system
causes the secretion of both epinephrine (E) (80%) and norepinephrine
(NE)(20%) into circulation. Epinephrine is a hormone; norepinephrine is
both a hormone and a neurotransmitter.
There are two categories of receptors, alpha and beta. There are also
subtypes of each. Useful generalizations concerning these are:
Activation of alpha 1 and beta 1 receptors cause stimulatory responses
Activation of alpha 2 , beta 2 & B3 receptors cause inhibitory responses
NE causes a greater response than E when activating alpha 1 receptors
E causes a greater or equal response than NE when activating alpha 2 receptors
E and NE cause equal responses when activating beta 1 receptors
E causes a significantly greater response than NE when activating beta 2 receptors
Alpha Receptors
Alpha 1 Receptors
Alpha 1 receptors are more responsive to NE than to E.
This is interesting as alpha 1 receptors are abundantly
found on vascular smooth muscle as seen in the diagram.
The relationship between the activated receptor and the
cell's response is direct -- the activity (muscle tone)of the
cell is increased. Alpha 1 receptors are located on:
all vascular smooth muscle, although densities vary
thoughout the body
GI & urinary sphincters
dilator muscle of the iris
arrector pili muscle of hair follicles
Increase in tone of vascular smooth muscles reduces the
ability of blood pressure to expand vessel diameter thus
reducing blood flow to downstream organs. Increased tone in urinary and gastrointestinal
sphincters reduces the passage of contents past them. Increased tone of the dilator muscle of the
iris enlarges the pupil. Increased tone of arrector pili muscles pulls on the hair follicle causing hair
to 'stand on end'.
Alpha 2 Receptors
Alpha 2 receptors are located on secretory terminals of some postsynaptic adrenergic neurons.
When these terminals secrete norepinephrine the neurotransmitter binds with these receptors as
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well as with adrenergic receptors on the other side of the synapse. The presynaptic neuron's
response is to decrease the amount of NE being released -- it is a negative feedback mechanism.
Current research is involved with determining if alpha 2 receptors are located elsewhere.
Beta Receptors
Beta 1 Receptors
The relationship between beta 1 activation by E
and/or NE is direct -- the cell's activity is increased.
Beta 1 receptors are located on:
cardiac pacemaker
myocardium
salivary gland ducts
eccrine and apocrine sweat glands
The cardiac pacemaker responds by increasing the
heart rate. Simultaneously the myocardium contracts
more forcefully. The physiology of the response of
salivary duct cells to beta 1 activation is unclear; it
appears that beta 1 activation of certain duct cells
reabsorbs some water in the slowly passing saliva
making it more viscous. The secretory portion of both
types of sweat gland is stimulated only by E and NE from the blood, not via nerves.
Note that beta 1 activation in the heart is both neural and hormonal. In the salivary glands the
activation is solely neural while in both type sweat glands it is solely due to E and NE in the blood.
Beta 2 Receptors
Beta 2 receptors are located on smooth muscle. The
relationship between E (hormonal) / NE (neurological) activation
and the response of the cell is inverse -- activity (muscle tone)
of the cell is decreased. Beta 2 receptors are located on smooth
muscle in:
the gastrointestinal tract
the urinary bladder
skeletal muscle arteries
the bronchial tree
some coronary vessels
Also notice there are beta 3 (B3)receptors on the smooth
muscle cells of the urinary bladder that decrease their tone in
response to receptor activation.
The diagram to the right emphasizes the main locations
of beta 2 receptors throughout the GI tract -- stomach,
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small intestine, colon, rectum. Their activation results in
decreased muscle tone and motility. In the urinary
bladder this decreased muscle tone enables greater
filling.
The diagram to the left shows relaxation of the circular
smooth muscle in the bronchial tree is due to
epinephrine -- note the lack of innervation at this
location. Beta 2 receptors are also on small coronary arterioles thus increasing hormonally induced
blood flow within the musculature of the heart. These receptors are the primary receptor in skeletal
muscles arteries resulting in enhanced blood flow especially when epinephrine is present.
Inspection of the main diagram to determine which arteries have alpha 1 sites and which have beta
2 sites. Remember that epinephrine is the best activator of B2 sites.
Last update: 10/4/2013
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