Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.

Nitecapone (3-(3,4-dihydroxy-5-nitrobenzylidine)-2,4- pentanedione, OR-462) is a selective, short-acting catechol-O-methyltransferase (COMT) inhibitor, whose main site of action is in the gastrointestinal tract. Nitecapone displays in vivo activity in peripheral tissues but does not penetrate the blood-brain barrier. The compound increases mechanical and thermal nociception and reduces neuropathic pain in diabetic rats and in a spinal nerve ligation model. Nitecapone has been shown to have a protective effect against ischemia-reperfusion injury in experimental heart transplantation and in Langendorff preparations. Nitecapone added to cardioplegia solution reduces cardiac neutrophil accumulation and transcoronary neutrophil activation during clinical cardiopulmonary bypass. Reflected by better left ventricular stroke volume, nitecapone treatment may be an additional way of reducing the deleterious effects of neutrophil activation during cardiopulmonary bypass. Nitecapone was patented as an antiparkinsonian agent but was never marketed.

Relcovaptan is a potent, orally active nonpeptide vasopressin V1a antagonist that was undergoing clinical development with Sanofi-Synthélabo (formerly Sanofi) in France. SR49059 is specifically and selectively antagonizes the effect of vasopressin on the V1a receptor in animals’ and in humans. The drug has been shown to have an excellent safety profile in single and repeated dose toxicological studies in animals. In the human uterus in vitro, SR49059 caused a dose-dependent inhibition of vasopressin V1a receptor-mediated activity of myometrial strips and isolated uterine arteries. In vivo in nonpregnant women, an inhibition of vasopressin-induced uterine activity has been observed.

Furegrelate (previously known as U-63557A), a selective orally active thromboxane synthase inhibitor, with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders, arrhythmias, but these studies were discontinued.

Potassium guaiacolsulfonate also known as sulfoguaiacolum is a salt of GUAIACOLSULFONIC ACID, which is used as an expectorant, to relieve symptoms of cough and mucus in the chest due to respiratory infections, asthma, colds, or hay fever. It works by thinning mucus (phlegm) in the lungs, making it less sticky and easier to cough up. This reduces chest congestion by making coughs more productive.

Broxaldine, also known as brobenzoxaldine, is a dibromo derivative of quinaldine. It was used in combination with other halogenated hydroxyquinoline compound broxyquinoline (INTESTOPAN) for the treatment of intestinal amoebiasis and childhood diarrhea. In a specific ratio of 5/1, they were shown to act synergistically against several pathogens.

Coumermycin is from the aminocoumarin class of antibiotic compounds which acts by inhibiting DNA gyrase. Coumermycin is effective against gram-positive bacteria, but not gram-negative bacteria. Coumermycin its derivatives have been studied since the 1950's as potential antibiotic. However, it has seen little to no clinical development because of its low water solubility, toxicity profile, and ineffectiveness against gram-negative bacteria.

Nafomine is the muscle relaxant. It was tested on lower extremity spasms in spinal cord injuries.

Mevinic acid is reversible competitive inhibitors of HMG-CoA reductase (Ki in the range of 0.2-1 nM). Mevinic acid is a precursor of a Mevastatin (mevinic acid lactone) -- a hypolipidemic agent that belongs to the statins class. Mevastatin inactive until metabolized in the liver to the open-ring hydroxy acid (Mevinic acid). Mevastatin might be considered the first statin drug; clinical trials on mevastatin were performed in the late 1970s in Japan, but it was never marketed.

Nicaraven is a hydroxyl radical scavenger with antivasospastic and neuroprotective effects. Chugai (the Japanese subsidiary of Roche) is developing nicaraven (Antevas), a water-soluble antioxidant, for the potential treatment of disorders caused by acute cerebrovascular diseases. A registration application was filed in April 1995, and in April 2002, nicaraven was still awaiting registration in Japan. By August 2002, Chugai had filed an NDA in Japan for the additional indication of subarachnoidal bleeding.