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 & beta 3 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 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 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 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
isinverse -- 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 vesselsAlso 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, 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.