Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.

Epristeride is a steroid 5-alpha-reductase inhibitor developed for the treatment of prostatic hyperplasia and acne. The drug reached phase III clinical trial for hyperplasia in the UK, the US and Japan, however, the current status of the drug is unknown.

Naftopidil (INN, marketed under the brand name Flivas) is a drug used in benign prostatic hypertrophy which acts as a selective alpha1-adrenergic receptor antagonist, has been used for the treatment of benign prostatic obstruction and benign prostatic hyperplasia (BPH) associated lower urinary tract symptoms (LUTS). The Japanese Ministry of Health, Labor and Welfare approved naftopidil for treating men with BPH in 1996. Although well-designed, randomized studies are warranted to confirm the long-term outcomes and effector/target of naftopidil, the α1A-antagonist naftopidil, which also blocks α1D-adrenoceptor, improves voiding symptoms, and may also be useful for the management of men with storage symptoms represented by nocturia, retrieving their quality of life impaired by BPH-associated LUTS. The selective alpha1D-blocker naftopidil can significantly facilitate spontaneous passage of distal ureteral stones with few side effects, providing a new choice for medical expulsive therapy.

Guanoxabenz is an antihypertensive drug that was in clinical use in the 1980s. It acts as a selective agonist of alpha2A1 and alpha2B1 adrenergic receptors. Guanoxabenz is the main metabolite of the FDA-approved drug guanabenz.

Azaloxan is an antidepressant drug, developed in the 1980s but never marketed.

Aceperone, an alpha-noradrenergic antagonist, causes the learning impairment in rodents. This can be manifested when the animal is faced with a type of task that has not recently been performed.

Tymazoline (trade name Thymazen in Poland) is a nasal decongestant that can be used to treat rhinitis and nasal obstruction. Tymazoline is a drug with antihistaminic and sympathomimetic properties. It locally reduces swelling, inflammation and mucosal secretions of the nasal passages. Thymazen causes vasoconstriction of the nasal mucosa, reducing congestion and thus the swelling of the mucosa. Also reduces the secretions from the nose. Thymazen acts on alpha-adrenergic receptors, which reduces local inflammation of the nasal mucosa especially if their cause is an allergy.

Tramazoline is a sympathomimetic drug that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. Tramazoline is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus.

Adrafinil (CRL 40028) was synthesized by Louis Lafon Laboratories. The proprietary name of adrafinil is Olmifon®; its chemical name is (diphenylmethyl )sulfinyl-2-acetohydroxamic acid. Adrafinil is metabolized to modafinil. Adrafinil and modafinil both serve as α1-adrenergic–receptor agonists. The evidence in support of this hypothesis, however, is weak, and other mechanisms of action are probable. Adrafinil may modify the intracerebral release of amino acids (both GABA and glutamate) and adrafinil may increase cerebral metabolism. Olmifon ® tablets, 300 mg (adrafinil) were indicated for the treatment of disorders of vigilance, attention, and ideo-motor slowing in the elderly. It has been marketed in France since September 19, 1985. Cephalon announced their intent to stop marketing the drug, and has discontinued production and marketing of Olmifon in September 2011. Adrafinil is marketing as nootropic supplement to improve cognitive functions.