Difference between revisions of "Adrenergic Pharmacology"
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! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists | ! Receptor !! Binding Affinity !! Effects !! Mechanism !! Agonists !! Antagonists | ||
|- | |- | ||
| − | | | + | | α1 || NE > Epi >> Iso |
| | | | ||
| − | * | + | *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 | ||
| − | |||
|- | |- | ||
| − | | | + | | 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 | ||
|- | |- | ||
| − | | | + | | β1 || Iso > NE > Epi |
| + | | | ||
| + | *↑Chronotropy (myocytes), ↑Inotropy (SA node), ↑SBP | ||
| + | *↑Renin release/↑volume (JGA) | ||
| + | *Amylase secretion | ||
| + | | | ||
| + | G<sub>s</sub> → ↑AC → ↑cAMP | ||
| | | | ||
*Dobutamine | *Dobutamine | ||
| Line 36: | Line 51: | ||
*Esmolol | *Esmolol | ||
|- | |- | ||
| − | | | + | | 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 | ||
| Line 50: | Line 73: | ||
*Pindolol | *Pindolol | ||
*Timolol | *Timolol | ||
| + | *Carved'''ilol''' (anti-α1) | ||
| + | *Labet'''alol''' (anti-α1) | ||
|- | |- | ||
| − | | | + | | β3 || Iso > Epi = NE |
| + | | | ||
| + | *Lipolysis | ||
| + | *Bladder detrusor relaxation | ||
| + | | | ||
| + | G<sub>s</sub> → ↑AC → ↑cAMP → ↑PKA | ||
| | | | ||
*Mirabegron | *Mirabegron | ||
| | | | ||
| − | + | *SR 59230A | |
|} | |} | ||
Latest revision as of 06:17, 4 February 2023
| Receptor | Binding Affinity | Effects | Mechanism | Agonists | Antagonists |
|---|---|---|---|---|---|
| α1 | NE > Epi >> Iso |
|
Gq → PLC → IP3/DAG → [Ca2+]i |
|
α1 selective:
|
| α2 | Epi = NE >> Iso |
|
presynaptic Gi → ↓AC → ↓cAMP → ↓NT release |
|
Non-selective:
|
| β1 | Iso > NE > Epi |
|
Gs → ↑AC → ↑cAMP |
|
Cardiac Selective:
|
| β2 | Iso > Epi > NE |
|
Gs → ↑AC → ↑cAMP → ↑PKA |
|
Non-Selective:
|
| β3 | Iso > Epi = NE |
|
Gs → ↑AC → ↑cAMP → ↑PKA |
|
|