Difference between revisions of "Adrenergic Pharmacology"

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! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists
 
! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists
 
|-
 
|-
| Alpha-1 || Norepi > Epi >> Iso || Smooth muscle contraction || Gq, PLC -> IP3/DAG  
+
| α1 || Norepi > Epi >> Iso || Smooth muscle contraction || Gq, PLC -> IP3/DAG  
 
|  
 
|  
 
*Norepi
 
*Norepi
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*Trazodone
 
*Trazodone
 
|-
 
|-
| Alpha-2 || Epi = Norepi >> Iso || Mixed effects || Gi, presynaptic, cAMP down  
+
| α2 || Epi = Norepi >> Iso || Mixed effects || Gi, presynaptic, cAMP down  
 
|  
 
|  
 
*Dexmedetomidine
 
*Dexmedetomidine
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*Trazodone
 
*Trazodone
 
|-
 
|-
| Beta-1 || Iso > Norepi > Epi || Example || Gs, cAMP up
+
| β1 || Iso > Norepi > Epi || Chronotropy, Inotropy, Amylase secretion || Gs, cAMP up
 
|
 
|
 
*Dobutamine
 
*Dobutamine
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*Esmolol
 
*Esmolol
 
|-
 
|-
| Beta-2 || Iso > Epi > Norepi || Example || Gs, cAMP up
+
| β2 || Iso > Epi > Norepi || Smooth muscle relaxation || Gs, cAMP up
 
|
 
|
 
*Albuterol
 
*Albuterol
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*Pindolol
 
*Pindolol
 
*Timolol
 
*Timolol
 +
*Carved'''ilol''' (anti-α1)
 +
*Labet'''alol''' (anti-α1)
 
|-
 
|-
| Beta-3 || Iso > Epi = Norepi || Example || Gs, cAMP up  
+
| β3 || Iso > Epi = Norepi || Lipolysis, bladder detrusor relaxation || Gs, cAMP up  
 
|
 
|
 
*Mirabegron
 
*Mirabegron
 
|
 
|
Example
+
*SR 59230A
 
|}
 
|}

Revision as of 23:00, 1 February 2023

Adrenergic Receptors
Receptor Binding Affinity Effects Mechanism Agonists Antagonists
α1 Norepi > Epi >> Iso Smooth muscle contraction Gq, PLC -> IP3/DAG
  • Norepi
  • Phenylephrine
  • Midodrine
  • Phenoxybenzamine
  • Phentolamine
  • Prazosin
  • Tamsulosin
  • Trazodone
α2 Epi = Norepi >> Iso Mixed effects Gi, presynaptic, cAMP down
  • Dexmedetomidine
  • Clonidine
  • Phenoxybenzamine
  • Phentolamine
  • Trazodone
β1 Iso > Norepi > Epi Chronotropy, Inotropy, Amylase secretion Gs, cAMP up
  • Dobutamine
  • Isoprenaline
  • Norepi

Cardiac Selective:

  • Metoprolol
  • Atenolol
  • Esmolol
β2 Iso > Epi > Norepi Smooth muscle relaxation Gs, cAMP up
  • Albuterol
  • Formoterol
  • Isoprenaline
  • Salmeterol
  • Terbutaline
  • Ritodrine

Non-Selective:

  • Propranolol
  • Nadolol
  • Pindolol
  • Timolol
  • Carvedilol (anti-α1)
  • Labetalol (anti-α1)
β3 Iso > Epi = Norepi Lipolysis, bladder detrusor relaxation Gs, cAMP up
  • Mirabegron
  • SR 59230A