Ligands
- Agonists
- Butcher's Broom (Ruscus aculeatus)
- Cirazoline
- Etilefrine
- Metaraminol
- Methoxamine
- Midodrine
- Naphazoline
- Oxymetazoline
- Phenylephrine (decongestant)
- Synephrine
- Tetrahydrozoline
- Xylometazoline
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- Antagonists
- Alfuzosin (used in benign prostatic hyperplasia
- Arotinolol
- Carvedilol (used in congestive heart failure; it is a non-selective beta blocker)
- Doxazosin (used in hypertension and benign prostatic hyperplasia)
- Indoramin
- Labetalol (used in hypertension; it is a mixed alpha/beta adrenergic antagonist)
- Moxisylyte
- Phenoxybenzamine
- Phentolamine (used in hypertensive emergencies; it is a nonselective alpha-antagonist)
- Prazosin (used in hypertension)
- Silodosin
- Tamsulosin (used in benign prostatic hyperplasia)
- Terazosin
- Tolazoline
- Trimazosin
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Various heterocyclic antidepressants and antipsychotics are α1-adrenergic receptor antagonists as well. This action is generally undesirable in such agents and mediates side effects like orthostatic hypotension, and extrapyramidal symptoms