Alletorphine (R & S 218-M) is a potent analgesic said to have a reduced respiratory depressant action. It was isolated by Bentley and Hardy (1967) while they were examining a series of derivatives of tetrahydrothebaine of which the potent analgesic etorphine (propylorvinolhydrochloride: M99 Reckitt) is a member. R&S 218-M bears the same relationship to etorphine as does nalorphine to morphine. It has been the subject of experiments in animals and human volunteers.

Sulmepride (also known as TER 1546) is a sulfamoylbenzamide derivative patented by Heumann, Ludwig, und Co. G.m.b.H. as neuroleptic. Sulmepride acts as a specific antagonist of dopamine D-2 receptors.

Cyproximide is a psychoactive drug discovered by American Cyanamid company. The drug exhibited activity as a central nervous system depressant and was claimed to be useful as a tranquilizing agent, hypnotic agent or muscle relaxant. The phenobarbital-like activity of cyproximide after intraperitoneal administration was demonstrated in rod traversal, clinging and righting reflex tests in mice. In addition to CNS depressant activity, cyproximide had a mild stimulant and antidepressant effects, which were shown by the restoration of exploratory behavior and an increase in locomotor activity in mice. Chronic administration of the drug led to a greater incidence of proliferative lesions in the liver of treated rats; however, the incidence of hepatocellular neoplasms was the same in treated and control rats.

Traboxopine (EGYT-2509) revealed specific dopamine-antagonistic activity with potentially minimal undesirable side effects. EGYT-2509 behaved as a dopamine receptor antagonist in all functional in vitro biochemical-pharmacological tests (striatal adenylate cyclase, striatal dopamine release, prolactin release from pituitary). The drug exhibited a marked preference for adenylate cyclase-coupled (D1) dopamine receptors, followed by the 3H-spiperone displacing potency at striatal receptors. Traboxopine exerts pharmacological and biochemical effects that seem to be partially similar to those of traditional neuroleptics, except for some undesirable side effects (e.g. cataleptogenic, influencing prolactin level). Traboxopine proved to be diversely influential on the dopaminergic components of the integration of sympathetic output and somato-autonomic reflexes. The apomorphine-induced stereotypy was potentiated by lower, and antagonized by higher doses of EGYT-2509. The in vitro potency of EGYT-2509 to block dopamine-mediated inhibition of prolactin release was weaker by three orders of magnitude than that of haloperidol.

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.

D-glucitol hexanicotinate (sorbinicate, SN) is a derivative of nicotinic acid. In rabbits kept on a diet containing 1 g/day cholesterol for 12 weeks, sorbinicate displayed greater hypolipemic and antiatherogenic activity than an equidose of plain nicotinic acid at much lower and more constant plasma nicotinic acid levels. By modulating the bioavailability of nicotinic acid, sorbinicate maintains and in some cases enhances the pharmacological activity of the acid, avoiding at least some of its major side effects. Sorbinicate has effective lipid-lowering activity; the combination of hypolipidemic and anti-aggregating properties may prove important in primary and secondary prevention of atherosclerotic disease. It is suggested that the antilipolytic activity of sorbinicate is at least partly mediated by an inhibition of glucagon secretion (and/or synthesis).

Bensalan was studied as a disinfectant.

Etoprindole is an antiinflammatory agent.

Cinfenine is diphenylmethoxyethylamine derivative that acts as antidepressant in some animal models.