Proheptazine is a substituted azacycloalkane patented by American Home Products Corp. as an opioid analgesic. Proheptazine produces similar effects to other opioids, including analgesia, sedation, euphoria, dizziness and nausea.

Tinisulpride is a sulfamoylbenzoic acid patented by Fabre, Pierre, S. A. as an antiemetic agent.

Dimeprozan is a tranquillizer. It is equipotent with chlorpromazine in producing ataxia, decreased motor activity, and loss of righting reflex in mice.

Quisultazine is a phenothiazine derivative patented by MARPHA Societe d'Etude et d'Exploitation de Marques as pentagastrin antagonist. In preclinical studies, Quisultazine weakly inhibited pentagastrin-stimulated gastric secretion but was a powerful inhibitor of nocturnal gastric secretion. Quisultazine possesses a very weak affinity to muscarinic receptors in vitro and in vivo. It has negligible anticholinergic properties in rats and mice at the peripheral level but no effect at the central level.

Litronesib is a specific, ATP-uncompetitive, allosteric, and potent small-molecule inhibitor of Eg5 with potential antineoplastic activity. Litronesib selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and consequently cell death in tumor cells that are actively dividing. Histone-H3 phosphorylation of tumor and proliferating skin cells is a promising pharmacodynamic biomarker for in vivo anticancer activity of litronesib. Litronesib had been in phase I clinical trial for the treatment of solid tumors. The most frequent-related adverse events were hematologic such as neutropenia.

Cipralisant (GT-2331) is an H3-receptor ligand developed by Gliatech in the late 1990s. The drug exhibits complex pharmacology: it behaves as an antagonist in a guinea pig jejunum contraction assay and mouse disogenia model, as a partial agonist in a rat brain synaptosome model, and as a full agonist at recombinant H3 receptors. In preclinical models, cipralisant enhanced wakefulness and improved learning in developmental rat models. In 2000 cipralisant was investigated in the clinical trials for the treatment of attention-deficit hyperactivity disorder, but due to the bankruptcy of Gliatech the development of the drug was discontinued.

Metethoheptazine (WY-535) is an analgesic agent.

Alagebrium (formerly known as ALT-711) - is one of the better known compounds discovered and developed with the intent of repairing a type of accumulated damage that leads to age-related degeneration. In this case, the damage is the buildup of extracellular protein crosslinks, and amongst them the type known as advanced glycation endproducts. The formation of advanced glycation end-products is associated with arterial stiffness in experimental models and alagebrium, an advanced glycation end-product cross-link breaker, has been shown to reduce arterial stiffness in elderly subjects. Alagebrium is an AGE-lowering agent with beneficial effects in renal structural and functional parameters in diabetes, decreased diabetes-accelerated atherosclerosis, and age-related myocardial stiffening. ALT-711 exhibits a structural homology to thiamine, and it was suggested to interfere with thiamine metabolism. Enzyme kinetic experiments showed that ALT-711 dose-dependently decreased TDPK activity with K(i)s, calculated by different experiments and fitting models ranging from 0.88 to 1.09 uM. Alagebrium has been investigated for the treatment and prevention of aging, heart failure, physical activity, diabetic nephropathy, and cardiovascular disease, among others. However, this research has been discontinued.