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α1 Receptor Location
Smooth muscle of most blood vessels, iris radial muscle, bladder sphincter, prostate.
α1 Receptor Effect
Smooth muscle contraction causing vasoconstriction, pupil dilation (mydriasis), and sphincter contraction.
Clinical Use of α1 Agonists
Increase blood pressure during hypotension or shock.
Clinical Use of α1 Antagonists
Treat hypertension and benign prostatic hyperplasia (BPH).
α2 Receptor Location
Presynaptic sympathetic nerve terminals.
Function of α2 Receptors
Negative feedback that decreases norepinephrine release.
Effect of α2 Agonists
Reduce sympathetic activity and lower blood pressure.
Example of an α2 Agonist
Clonidine.
Additional Use of α2 Agonists
Reduce aqueous humor production in glaucoma.
β1 Receptor Location
SA node, AV node, and cardiac muscle.
β1 Receptor Effects
Increase heart rate, contractility, and cardiac output.
Positive Chronotropic Effect
Increased heart rate.
Positive Inotropic Effect
Increased force of cardiac contraction.
Clinical Use of β1 Blockers
Treat hypertension and arrhythmias by lowering heart rate and contractility.
β2 Receptor Location
Bronchioles, uterus, liver, and skeletal muscle blood vessels.
β2 Receptor Effects
Bronchodilation, uterine relaxation, vasodilation, glycogenolysis, and gluconeogenesis.
Clinical Use of β2 Agonists
Treat asthma by causing bronchodilation.
Example of a β2 Agonist
Albuterol
Additional Clinical Use of β2 Agonists
Relax the uterus to delay premature labor.
β3 Receptor Location
Adipose tissue
β3 Receptor Effect
Lipolysis (breakdown of triglycerides into glycerol and fatty acids).
Why Aren't β3 Agonists Used for Weight Loss?
They are not selective and may stimulate β1 receptors, causing hypertension and cardiovascular complications.
α1 Agonists
Increase blood pressure through vasoconstriction.
α1 Antagonists
Lower blood pressure through vasodilation.
α2 Agonists
Decrease norepinephrine release and reduce blood pressure.
β1 Agonists
Increase heart rate and contractility.
β1 Antagonists
Decrease heart rate, contractility, and blood pressure.
β2 Agonists
Cause bronchodilation and uterine relaxation.
β3 Agonists
Stimulate lipolysis.