Dioxifedrine is the putative metabolite of 3,4-methylenedioxymethamphetamine. It is the sympathomimetic agent and beta-2 -adrenergic agonist with bronchodilator activity. Dioxifedrine selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. In stimulatory studies dioxifedrine increased locomotor activity from 15 to 30 min following the drug administration. Following intracerebroventricular injection dioxifedrine rapidly reduced blood pressure and heart rate.

Bipenamol is a benzenemethanol derivative used to prepare novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I.

Sulfinalol is a hydroxyphenylalkanolamine derivative patented by Sterling Drug Inc. as the antiarrhythmic, antihypertensive, vasodilating, and adrenergic agent. Oral administration of sulfinalol reduces the pressure of conscious spontaneously hypertensive rats. Antihypertensive action of sulfinalol was inhibited by propranolol pretreatment. Sulfinalol demonstrates effective beta-adrenergic blockade at the antihypertensive dose tested as judged by inhibition of the chronotropic responses to sympathetic stimulation and isoproterenol in pithed rats. In the renal hypertensive dog. sulfinalol lowered both systolic and diastolic blood pressure to normal values with an only slight change in heart rate.

FENYRIPOL is a skeletal muscle relaxant.

Dioxethedrin is the ephedrine derivative. It is the beta-adrenergic agonist. As a bronchodilator and sympathomimetic agent is was used in antitussive syrup Bexol.

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.

Amiterol, a phenethylamine derivative, is an oral anti-asthma drug (bronchodilator).

FEPRADINOL is an analgesic, antipyretic and anti-inflammatory agent. Its anti-inflammatory activity does not seem to be related to an inhibitory effect on prostaglandin biosynthesis.

LEDAZEROL is a derivative of mivazerol. It was under development as an antianginal agent.

Metaterol is a beta-adrenoceptor agonist. It exerts sympathomimetic and broncholytic properties.