Difference between revisions of "Adrenergic Pharmacology"

Latest revision as of 06:17, 4 February 2023

Adrenergic Receptors
Receptor	Binding Affinity	Effects	Mechanism	Agonists	Antagonists
α1	NE > Epi >> Iso	Smooth muscle contraction, ↑SVR, ↑MAP Mydriasis, urethral sphincter contraction	G_q → PLC → IP₃/DAG → [Ca²⁺]_i	NE Phenylephrine (pure α1) Midodrine	α1 selective: Prazosin Tamsulosin
α2	Epi = NE >> Iso	↑SVR, ↑MAP ↓insulin release, ↓lipolysis, ↓aqueous humor production	presynaptic G_i → ↓AC → ↓cAMP → ↓NT release	Dexmedetomidine Clonidine	Non-selective: Phenoxybenzamine Phentolamine Trazodone
β1	Iso > NE > Epi	↑Chronotropy (myocytes), ↑Inotropy (SA node), ↑SBP ↑Renin release/↑volume (JGA) Amylase secretion	G_s → ↑AC → ↑cAMP	Dobutamine Isoprenaline Norepi	Cardiac Selective: Metoprolol Atenolol Esmolol
β2	Iso > Epi > NE	Smooth muscle relaxation, ↓SVR, ↓DBP, ↓MAP Bronchodilation ↑Lipolysis, ↑Insulin release Relax uterine smooth muscle ↑aqueous humor production	G_s → ↑AC → ↑cAMP → ↑PKA	Albuterol Formoterol Isoprenaline Salmeterol Terbutaline Ritodrine	Non-Selective: Propranolol Nadolol Pindolol Timolol Carvedilol (anti-α1) Labetalol (anti-α1)
β3	Iso > Epi = NE	Lipolysis Bladder detrusor relaxation	G_s → ↑AC → ↑cAMP → ↑PKA	Mirabegron	SR 59230A

@@ Line 59: / Line 59: @@
 *&uarr;aqueous humor production
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-G<sub>s</sub> &rarr; &uarr;AC; &rarr; &uarr;cAMP &rarr; &uarr;PKA
+G<sub>s</sub> &rarr; &uarr;AC &rarr; &uarr;cAMP &rarr; &uarr;PKA
 |
 *Albuterol
@@ Line 77: / Line 77: @@
 |-
 | &beta;3 || Iso > Epi = NE
+|
 *Lipolysis
 *Bladder detrusor relaxation
 |
-G<sub>s</sub> &rarr; &uarr;AC; &rarr; &uarr;cAMP &rarr; &uarr;PKA
+G<sub>s</sub> &rarr; &uarr;AC &rarr; &uarr;cAMP &rarr; &uarr;PKA
 |
 *Mirabegron