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Adrenore
ceptor
Agonist potency order Selected action of agonist Mechanism Agonists Antagonists
1:
A, B, D


Norepinephrine
> epinephrine
>> isoprenaline
Smooth muscle contraction Gq: phospholipase C(PLC) activated, IP3,and DAG, rise in calcium
(Alpha-1 agonists)
Noradrenaline
Phenylephrine
Methoxamine
Cirazoline
Xylometazoline
Midodrine
(Alpha-1 blockers)
Alfuzosin
Doxazosin
Phenoxybenzamine
Phentolamine
Prazosin
Tamsulosin
Terazosin
(TCA:s)
1. Amitriptyline
2. Clomipramine
3. Doxepin
4. Trimipramine
2:
A, B, C
Epinephrine

norepinephrine

>> isoprenaline
Smooth muscle mixed effects and neurotransmitter
inhibition & Cardiac
muscle relaxation platelet activation
Gi: adenylate cyclaseinactivated, cAMP down
(Alpha-2 agonists)
1. Dexmedetomidine
2. Medetomidine
3. Romifidine
4. Clonidine
5. Brimonidine
6. Detomidine
7. Lofexidine
8. Xylazine
9. Tizanidine
10. Guanfacine
11. Amitraz
(Alpha-2 blockers)
Phentolamine
Yohimbine
Idazoxan
Atipamezole
1
Isoprenaline

> epinephrine

= norepinephrine
Heart muscle contraction Gs: adenylate cyclaseactivated, cAMP up
Dobutamine
Isoprenaline
Noradrenaline
(Beta blockers)
Metoprolol
Atenolol
2
Isoprenaline

> epinephrine

>> norepinephrine
Smooth muscle relaxation Gs: adenylate cyclaseactivated, cAMP up (alsoGi, see 2)
(Short/long)
1. Salbutamol(Albuterol in USA)
2. Bitolterol mesylate
3. Formoterol
4. Isoprenaline
5. Levalbuterol
6. Metaproterenol
7. Salmeterol
8. Terbutaline
9. Ritodrine
(Beta blockers)
Butoxamine
Propranolol
3
Isoprenaline = norepinephrin
e > epinephrine
Enhance lipolysis, promotes relaxation of detrusor
muscle in thebladder
Gs: adenylate cyclaseactivated, cAMP up
1. L-796568
[2]

2. Amibegron
3. Solabegron
SR 59230A

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