Kynurenic acid is a product of the normal metabolism of amino acid L-tryptophan which has been shown to have a neuroactive profile. It exhibits activity against NMDA receptors and Neuronal acetylcholine receptor subunit alpha-7. It has been investigated as a potential therapeutic compound and as a biomarker in a number of neurological disorders. Although Kenyruic acid exhibits a poor penetration of the blood-brain barrier, it remains to be of particular interest to those researching Schizophrenia.

Panadiplon (previously known as U-78875) was investigated as a compound with a high affinity for the benzodiazepine receptors. It was studied as a unique anxiolytic agent with a minimum of central nervous system depression for the treatment of anxiety disorders. However, panadiplon was dropped from clinical development due to unexpected hepatic toxicity in human volunteers. It was shown that the drug-induced mitochondrial dysfunction in the liver, and suggested that this dysfunction could be attributed to the carboxylic acid metabolite.

Rolafagrel (FCE 22178) is a selective thromboxane synthase inhibitor that has been evaluated for use in the treatment of diabetic nephropathy and thrombosis. Rolafagrel inhibits platelet and glomerular thromoxane synthase in animal and human kidney disease. A phase I clinical trial did not report drug-related adverse events. No information is available on current use of rolafagrel.

Pamaqueside, an 11-ketotigogenin cellobioside was developed as a cholesterol absorption inhibitor for the treatment of hypercholesterolemia. This drug participated in phase III clinical trial; however, information about the further development of this drug is not available.

Ripisartan (UP-269-6) is a specific nonpeptide angiotensin II receptor antagonist. Oral administration of ripisartan in rats and dogs resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response. It did not show agonistic properties in animals. In vitro, ripisartan was found to bind selectively to AT1 receptors. In humans, it showed high biliary excretion and reabsorption. Canine studies have suggested it might have cardioprotective properties after acute ischemia-reperfusion.

Lubeluzole is a medication, developed by Janssen Research Foundation for the treatment of acute ischemic stroke. The drug action is discussed to involve the inhibition of NMDA receptor and sodium channels.

Piclamilast (RP 73401), is a selective PDE4 inhibitor. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. It has been investigated for its applications to the treatment of conditions such as asthma, dermatitis, rheumatoid arthritis. Emesis is the most commonly cited side effect of piclamilast.

Carbendazim is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities widely used as a fungicide in agriculture and home gardening, and as an antihelminthic in veterinary medicine. As a fungicide, carbendazim used for controls Ascomycetes, Fungi Imperfecti, and Basidiomycetes on a wide variety of crops, including bananas, cereals, cotton, fruits, grapes, mushrooms, ornamentals, peanuts, sugarbeet, soybeans, tobacco, and vegetables. Carbendazim is a chemically stable and relatively persistent fungicide which only metabolizes to a limited extent in plants and in soil. The only detected metabolite is 2-aminobenzimidazole, which constitutes less than 5% of the total residues in leaves. Carbendazim may be anticipated to metabolize in the animal into hydroxylated analogues which may appear in meat and milk products. Carbendazim acts as a mitotic poison by altering tubulin binding and microtubule formation. This has been proposed as a possible mechanism of action for the developmental abnormalities seen in animal studies with high concentrations.