GPCR Flashcards
List All Gq
“Q can HAVe 1 M&M”
H1, Alpha1, V1, M1, M3
List all Gi
“MAD 2s”
M2, Alpha2, D2
List all Gs
Beta1, Beta2, D1, H2, V2
Receptor that:
- Increases SM contraction
- Increases pupillary dilator contraction
- Increase intestinal and bladder sphincter muscle contraction
Alpha1
Receptor that:
- Decreases HR
- Decreases contractility of atria
M2
Receptor that:
- Increases nasal and bronchial mucus production
- Increases vascular permeability
- Contracts bronchioles
- Causes pruritis/pain
H1
Receptor that:
-Increases H2O permeability and reabsorption in collecting tubules of kidney
V2 (found in 2 kidneys)
Receptor that causes:
- Vasodilation
- Bronchodilation
- Increased HR
- Increased contractility
- Increased lipolysis
- Increased insulin release
- Decreased uterine tone (tocolysis)
- Ciliary muscle relaxation
- Increased aqueous humor production
Beta-2
Receptor that causes:
- Decreased sympathetic outflow
- Decreased insulin release
- Decreased lipolysis
- Increased platelet aggregation
Alpha-2
Receptor that causes:
- Increased exocrine gland secretions (ex. lacrimal, salivary, gastric acid)
- Increased gut peristalsis
- Increased bladder contraction
- Bronchoconstriction
- Increased pupillary sphincter contraction (miosis)
- Ciliary muscle contraction (accommodation)
M3
Receptor that causes:
-Relaxed renal vascular SM
D1
Receptor that causes:
-Increased vascular SM contraction
V1
Receptor that modulates transmitter release (especially in brain)
D2
Receptor that:
- Increases HR
- Increases contractility
- Increases Renin release
- Increases lipolysis
Beta-1
Receptor that works in CNS and enteric nervous system
M1
Receptor that increases gastric acid secretion
H2
Epinephrine specificity
Beta > alpha
Norephinephrine specificity
Alpha1 > Alpha2 > Beta1
Isoproterenol specificity
Beta1 = Beta2
Dopamine specificity
D1 = D2 > Beta > alpha
Dobutamine specificity
Beta1 > Beta2 > alpha
Phenylephrine specificity
Alpha1 > Alpha2
Albuterol and terbutaline specificity
Beta 2 > Beta 1
Clonidine and Alpha-Methyldopa
Alpha2 agonist
Phenoxybenzamine
Irreversible, nonselective alpha blocker
Phentolamine
Reverxible, nonselective alpha blocker
Acebutolol, Metrolol
Beta 1 > Beta 2
Prazosin, Tamsulosin
Alpha1 selective blocker
Carvedilol, labetalol
Nonselective alpha and beta blocker
Mirtazapine
Alpha2 selective blocker
Nadolol, Propranolol
Beta1 = Beta2 blocker
Nebivolol
Beta1 block with stimulation of Beta3