Ephedrine (l-form) is an alkaloid, which was initially purified from Ephedra plant. The extract form Ephedra has been used in China for medicinal purposes for several thousand years. Ephedrine acts as an agonist at alpha- and beta-adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons. The drug crosses the blood brain barrier and stimulates the central nervous system. Ephedrine products are now banned in many countries, as they are a major source for the production of the addictive compound methamphetamine. FDA has approved ephedrine only for the treatment of clinically important hypotension occurring in the setting of anesthesia.

Prizidilol (also known as SKF 92657) is arylpyridazinylhydrazine derivative patented by Smith Kline and French Laboratories Ltd. as an antihypertensive agent. In clinical trials, Supine and standing blood pressure measured 24--27 h after drug intake was reduced Slight but significant decreases in heart rate were seen after moderate doses of prizidilol. A more pronounced blood pressure reduction was noticed 2--7 h after drug administration. Prizidilol was well tolerated, although dizziness and tiredness were reported by four patients and edema by two.

Levomoprolol (L-moprolol) is a beta-adrenergic blocker which was introduced as an oral medication for treatment of systemic hypertension. It was found to be effective in 2% eyedrops in reducing the intraocular pressure in glaucoma. Observations on glaucoma patients treated with the eyedrop for 1.5 to 2.5 years was without undesirable side effects. L-moprolol and dipivefrin had an equivalent effect in lowering the intraocular pressure. The association of the two drugs caused a further reduction of intraocular pressure.

Amibegron (SR 58611A or SR 58611) is a highly selective agonist for atypical beta3-adrenoceptors. It stimulates neuronal activity in a specific area of the prefrontal cortex and also inhibits intestinal motility. Amibegron was in phase III trials worldwide for the treatment of depression and generalised anxiety disorder but development of the product was discontinued in 2008. Amibegron has been tested for its potential as a treatment for irritable bowel syndrome.

Talibegron (ZD2079) is a β3 adrenoceptor agonist and insulin sensitiser. It was developed as a potential treatment for obesity and non-insulin-dependent diabetes mellitus. Talibegron hydrochloride had been in phase II clinical trials by AstraZeneca for the treatment of type 2 diabetes and obesity. However, this research has been discontinued.

Sulfonterol is a benzenemethanol derivative patented by Smith Kline and French Laboratories as a bronchodilator. Sulfonterol acts as a β-adrenergic partial agonist.

Trecadrine is a beta3-adrenergic agonist. Trecadrine could have normalized the oxygen consumption by the liver, in which other metabolic pathways could be involved. The administration of Trecadrine produced a statistically significant decrease in glucose levels, which is not related to changes in insulin levels. Trecadrine administration to animals significantly inhibited galactose intestinal absorption, which was independently confirmed by additional in-vitro studies and decreased disaccharidase activities. Trecadrine enhance glucose storage in liver, probably through a non-insulin dependent mechanism of action. Trecadrine administration may have a therapeutic potential in disorders associated with hypertriglyceridemia such as obesity and some types of hyperlipidaemias. Trecadrine shows a potent hypoglycaemic effect in the alloxan-induced model of diabetes in rats by decreasing hepatic glucose output and improving muscle glucose uptake.

Tolamolol is a phenoxypropranolamine derivative that preferentially inhibits myocardial beta adrenoreceptors, possesses beta blocking potency equivalent to propranolol, has little or no direct cell membrane effect and lacks beta adrenergic stimulating action. Cardioselective beta adrenergic blockade with tolamolol was highly effective in controlling ventricular rate in supraventricular arrhythmias and reduced the frequency of ventricular ectopic beats in half of the small group of patients with this arrhythmia. It is particularly applicable in patients with obstructive pulmonary disease in whom cardiac beta adrenergic blockade is indicated. Hypotension is an important potential side effect. Tolamolol and propranolol are equal in anti-anginal efficacy but tolamolol has the advantage of being cardioselective. It is superior to practolol. Tolamolol had no effect on sperm motility.

Sanfetrinem cilexetil (formerly known as GV 118819), a beta-lactam antibiotic, is the oral prodrug of sanfetrinem. Experiments on rodents have revealed that sanfetrinem cilexetil had strong antibacterial activity in vitro and good pharmacokinetic behavior in mice. This drug was suitable for the treatment of infections caused by a variety of bacteria and participated in a phase II clinical trial. However, this study was discontinued.

Salmefamol is a beta2-adrenoceptor agonist that was studied in asthmatic patients. In clinical trials, the drug had shown marked efficacy with low toxicity and was generally well tolerated. However, information about the further development of salmefamol as a bronchodilator drug is not available.