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.

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.

Sprodiamide is a nonionic paramagnetic dysprosium chelate agent patented by Salutar, Inc.as diagnostic imaging contrast media. Compare with gadolinium-based agents Sprodiamide shows a stronger T2 effect and negligible T1 effect. This property makes Sprodiamide useful for blood volume imaging. In a preclinical model of reperfused ischemia of the rat intestine administration of Sprodiamide improved the contrast between the normal and ischemic intestine on T2-weighted images, and administration of both gadodiamide and Sprodiamide improved the contrast on T1- and T2-weighted images.

Binodenoson, a selective adenosine A(2A) receptor agonist, was being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging. Binodenoson for injection under the brand name CorVue was developed for use in patients with or at risk for coronary artery disease (CAD) who are unable to perform a cardiac exercise stress test. CorVue was designed to minimize side effects such as dyspnea, flushing, heart block, and chest pain. Binodenoson did not achieve FDA approval in 2009 due to concerns over equivalence of its efficacy with adenosine.

Nebicapone (BIA 3-202) is a reversible, and tight-binding peripheral inhibitor of the enzyme catechol-O-methyltransferase (COMT) being developed for use as an adjunct to levodopa/dopa decarboxylase inhibitor in the treatment of PD. Nebicapone dose dependently and significantly decreased COMT activity. Nebicapone also increased systemic exposure to levodopa and improved motor response. The tight-binding nature of the inhibition produced by BIA 3-202 was evaluated by performing an Ackermann-Potter plot. The true K(i) for BIA 3-202, derived from the nonlinear regression analysis, was 0.19+/-0.02 nM. In substrate competition studies, an increase in the concentration of adrenaline resulted in a linear increase in IC(50) values for BIA 3-202.