Rec

ept

Agonist potency

Selected action

order

of agonist

or

Smooth

Mechanism

1:

Norepinephrine > epi

A, B

nephrine >> isoprena musclecontraction,mydri

ase C (PLC)

, D

line

asis,vasoconstrictionin

activated,IP3,a

the skin, muscosa and

nd DAG, rise

abdominalviscera &

in calcium

sphincter contraction of
the GI tract andurinary

Gq:phospholip

Agonists

(Alpha-1
agonists)

bladder

Nor
adrenal
ine
Ph
enylep
hrine

Met
hoxami
ne

Cir
azoline

Xyl
ometaz
oline

Mid
odrine

Met
aramin
ol

Antagonis
ts

(Alpha-1
blockers)

Alf
uzosin

Do
xazosi
n

Ph
enoxy
benza
mine

Ph
entola
mine

Pr
azosin

Ta
msulo
sin

Ter
azosin

Tra
Chl
zodon
oroethy
e
lclonidi
ne
(TCA:s)

Am
itriptyli
ne

Clo
mipra
mine

Do
xepin

Tri
mipra
mine

Ty
pical
and
atypic
al
antips
ychotic
s

Antihistam
ines (H1
antagonist
s)

2:

Epinephrine norepi

Smooth musclemixed

Gi: adenylate

A, B

nephrine >> Isopren

effects, norepinephrine

cyclaseinactiv

,C

aline

(noradrenaline)

ated,cAMP do

inhibition,plateletactivati

wn

(Alpha-2
agonists)

Ag
matine

De
xmedet
omidin
e

Me
detomi
dine

on

Ro
mifidin
e
Clo
nidine

Hy
droxyz
ine

(Alpha-2
blockers)

Ph
entola
mine

Yo
himbin
e

Ida
zoxan

Ati
pamez
ole

Tra
zodon
e

Isoprenaline > epine

PositiveChronotropic,Dr

Gs: adenylate

phrine = norepinephr

omotropicand inotropicef

cyclaseactivat

ine

fects,

ed,cAMP up

increasedamylasesecreti
on

Chl
oroethy
lclonidi
ne

Bri
monidi
ne

Det
omidin
e

Lof
exidine

Xyl
azine

Tiz
anidine

Gu
anfacin
e

Ami
traz

Do
butami
ne

Iso
prenali
ne
Nor
adrenal
ine

Ty
pical
and
atypic
al
antips
ychotic
s

(Beta
blockers)

Me
toprolo
l

Ate
nolol

Bis
oprolol

Pr
oprano
lol

Ti

molol

Ne
bivolol

Vor
tioxeti
ne

(Short/long
)

Sal
butamo
l(Albut
erol in
USA)

Bito
lterol
mesyla
te
(Beta

For blockers)
moterol

But
oxami
Iso
ne
prenali
ne

Ti
molol
Lev

Gs: adenylate
Isoprenaline > epine
2

phrine >> norepinep

hrine

Muscle relaxation
(Ex.Bronchodilation)

cyclaseactivat

ed,cAMP up
(alsoGi,
see 2)

albuter
ol

Met
aproter
enol

Sal
meterol

Ter
butalin
e

Rit
odrine

Pr
oprano
lol

L796568
[4]

Isoprenaline = norepi Enhance lipolysis,

Gs: adenylate

nephrine > epinephri

promotes relaxation of

cyclaseactivat

ne

detrusor in the bladder

ed,cAMP up

Ami
begron

Sol
abegro
n

SR
59230
A

[5]

There is no 1C receptor. At one time, there was a subtype known as C, but was found to be identical

to one of the previously discovered subtypes. To avoid confusion, naming was continued with the
letter D.

receptors
receptors have several functions in common, but also individual effects. Common (or still
unspecified) effects include:

Vasoconstriction of veins[6]

Decrease motility of smooth muscle in gastrointestinal tract[7]

1 receptor[edit]
Main article: Alpha-1 adrenergic receptor
1-adrenergic receptors are members of the Gq protein-coupled receptor superfamily. Upon
activation, a heterotrimeric G protein, Gq, activates phospholipase C (PLC). The PLC
cleaves phosphatidylinositol 4,5-bisphosphate (PIP2), which in turn causes an increase in inositol
triphosphate (IP3) and diacylglycerols (DAG). The former interacts with calcium channels of
endoplasmic and sarcoplasmic reticulum, thus changing the calcium content in a cell. This triggers
all other effects.
Specific actions of the 1 receptor mainly involve smooth muscle contraction. It
causes vasoconstriction in many blood vessels, including those of the skin, gastrointestinal
system, kidney (renal artery)[8] and brain.[9] Other areas of smooth muscle contraction are:

ureter

vas deferens

hair (arrector pili muscles)

uterus (when pregnant)

urethral sphincter

urothelium and lamina propria[10]

bronchioles (although minor due to the relaxing effect of 2 receptor on bronchioles)

blood vessels of ciliary body (stimulation causes mydriasis)

Further effects include glycogenolysis and gluconeogenesis from adipose tissue[11] and liver, as well
as secretion from sweat glands[11] andNa+ reabsorption from kidney.[11]
Antagonists may be used primarily in hypertension, anxiety disorder, and panic attacks.
2 receptors
Main article: Alpha-2 adrenergic receptor
The 2 receptor couples to the Gi/o protein.[2] It is a presynaptic receptor, causing negative feedback
on, for example, norepinephrine. When NA is released into the synapse, it feeds back on the
2 receptor, causing less NA release from the presynaptic neuron. This decreases the effect of NA.
There are also 2 receptors on the nerve terminal membrane of the post-synaptic adrenergic neuron.
There are 3 highly homologous subtypes of 2 receptors: 2A, 2, and 2C.
Specific actions of the 2 receptor include:

Inhibition of insulin release in the pancreas.[11]

Induction of glucagon release from the pancreas.

contraction of sphincters of the gastrointestinal tract

negative feedback in the neuronal synapses - presynaptic inhibition of noradrenalin (NA)

release in CNS

increased thrombocyte aggregation

receptors[edit]
1 receptor[edit]
Main article: Beta-1 adrenergic receptor
Specific actions of the 1 receptor include:

Increase cardiac output by increasing heart rate (positive chronotropic effect), conduction
velocity (positive dromotropic effect), and stroke volume (by enhancing contractilitypositive
inotropic effect).

Increase renin secretion from juxtaglomerular cells of the kidney.

Increase ghrelin secretion from the stomach.[12]

2 receptor[edit]
Main article: Beta-2 adrenergic receptor

Beta-2 adrenergic receptor (PDB 2rh1), which stimulates cells to increase energy production and utilization.
The membrane is shown schematically with a gray stripe.

Specific actions of the 2 receptor include the following:

Smooth muscle relaxation, e.g. in bronchi,[11] GI tract (decreased motility).

Lipolysis in adipose tissue.[13]

Anabolism in skeletal muscle.[14][15]

Relax non-pregnant uterus

Relax detrusor urinae muscle of bladder wall

Dilate arteries to skeletal muscle

Glycogenolysis and gluconeogenesis

Inhibits insulin secretion

Contract sphincters of GI tract

Thickened secretions from salivary glands.[11]

Inhibit histamine-release from mast cells

Increase renin secretion from kidney

Relaxation of Bronchioles (salbutamol, a 2 agonist relieves bronchiole constriction)

Involved in brain - immune communication[16]

3 receptor[edit]
Main article: Beta-3 adrenergic receptor
Specific actions of the 3 receptor include:

Enhancement of lipolysis in adipose tissue. 3 activating drugs could theoretically be used as

weight-loss agents, but are limited by the side effect of tremors.