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Adrenergic Pharmacology (view source)
Revision as of 06:17, 4 February 2023
, 06:17, 4 February 2023no edit summary
! 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 || NE > Epi >> Iso
|
|
*Norepi
*Smooth muscle contraction, ↑SVR, ↑MAP
*Phenylephrine
*Mydriasis, urethral sphincter contraction
|
G<sub>q</sub> → PLC → IP<sub>3</sub>/DAG → [Ca<sup>2+</sup>]<sub>i</sub>
|
*NE
*Phenylephrine (pure α1)
*Midodrine
*Midodrine
|
|
'''α1 selective:'''
*Prazosin
*Prazosin
*Tamsulosin
*Tamsulosin
|-
|-
| Alpha-2 || Epi = Norepi >> Iso || Mixed effects || Gi, presynaptic, cAMP down
| α2 || Epi = NE >> Iso
|
*↑SVR, ↑MAP
*↓insulin release, ↓lipolysis, ↓aqueous humor production
|
presynaptic G<sub>i</sub> → ↓AC → ↓cAMP → ↓NT release
|
|
*Dexmedetomidine
*Dexmedetomidine
*Clonidine
*Clonidine
|
|
'''Non-selective:'''
*Phenoxybenzamine
*Phenoxybenzamine
*Phentolamine
*Phentolamine
*Trazodone
*Trazodone
|-
|-
| Beta-1 || Iso > Norepi > Epi || Example || Gs, cAMP up
| β1 || Iso > NE > Epi
|
*↑Chronotropy (myocytes), ↑Inotropy (SA node), ↑SBP
*↑Renin release/↑volume (JGA)
*Amylase secretion
|
G<sub>s</sub> → ↑AC → ↑cAMP
|
|
*Dobutamine
*Dobutamine
*Esmolol
*Esmolol
|-
|-
| Beta-2 || Iso > Epi > Norepi || Example || Gs, cAMP up
| β2 || Iso > Epi > NE
|
*Smooth muscle relaxation, ↓SVR, ↓DBP, ↓MAP
*Bronchodilation
*↑Lipolysis, ↑Insulin release
*Relax uterine smooth muscle
*↑aqueous humor production
|
G<sub>s</sub> → ↑AC → ↑cAMP → ↑PKA
|
|
*Albuterol
*Albuterol
*Pindolol
*Pindolol
*Timolol
*Timolol
*Carved'''ilol''' (anti-α1)
*Labet'''alol''' (anti-α1)
|-
|-
| Beta-3 || Iso > Epi = Norepi || Example || Gs, cAMP up
| β3 || Iso > Epi = NE
|
*Lipolysis
*Bladder detrusor relaxation
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G<sub>s</sub> → ↑AC → ↑cAMP → ↑PKA
|
|
*Mirabegron
*Mirabegron
|
|
*SR 59230A
|}
|}