Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) was synthesized by various routes in the 1930s and 1940s and clinically evaluated as anorectic as well as a treatment of hypotension and symptoms of the common cold. It was widely used for the treatment of the common cold or hypotonic conditions. Due to its stimulating properties and its rapid metabolism resulting in major degradation products such as methylpseudoephedrine and methcathinone, it has been considered relevant for doping controls by the World Anti-Doping Agency (WADA). Metamfepramone was marketed as an appetite suppressant, but was made illegal in 2006.

Enciprazine also known as WY-48624 or, D-3112 is a GABA A receptor agonist which was in the phase III of clinical trial for the treatment of anxiety disorders. Enciprazine was well tolerated, with low levels of sedative and asthenic side effects reported. However, research was discontinued.

Efegatran (GYKI 14766; LY 294468) is a tripeptide D-methyl-phenylalanyl-prolyl-arginal thrombin inhibitor. It was developed by IVAX for the potential treatment of thromboembolic disorders, mainly myocardial infarction. However, information about the further development is not available.

Bemarinone (ORF 16600) is a positive inotropic and vasodilator agent with potential clinical utility in the management of congestive heart failure. The compound selectively and competitively inhibited cyclic AMP phosphodiesterase fraction III. However, further studies were discontinued

Bunolol is non-selective beta-adrenoreceptor antagonist with significant antihypertensive, antiarrhythmic and local anesthetic activities. Bunolol is a racemic mixture and Levobunolol is greater than 60 times more potent than its dextro isomer in its beta-blocking activity. Bunolol is 3 times as potent as propranolol by i.v. administration in anesthetized dogs in antagonizing the cardiovascular actions of isoproterenol and the response to cardioaccelerans nerve stimulation. When oral doses were given to unanesthetized dogs with subsequent induction of anesthesia, Bunolol was 20 times as potent as propranolol. The β-adrenergic blocking activity of Bunolol appeared to be competitive, and the activity was largely restricted to the l-isomer. Bunolol is extensively metabolized by both oxidative and reductive routes.

Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.

Bendacalol (also known as CGS 10078B) is an alpha- and beta-adrenergic receptor inhibitor with calcium entry blocking effect was studied for the treatment of hypertension. Animal experiments have sown some positive results. However, information about further studies is not available.

IRALUKAST, a leukotriene D4 analog, has potent peptido-leukotriene antagonist activity. It was under clinical development and in phase II clinical trials as a potential treatment for asthma.

Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. The effects of mafosfamide on various types of cancer cells were determined during preclinical investigations and clinical trials. Its development has been discontinued.