Fospirate is an organophosphorus insecticide used in veterinary as an anthelmintic agent.

Pipequaline (PK-8165, 2-phenyl-4[2-(4-piperidinyl) ethyl]quinoline) is a benzodiazepine receptor partial agonist.

Gomisin A (BESIGOMSIN/GA) one of the major dibenzocyclooctadiene lignans isolated from Schisandra chinensis Baill, has proved to possess a variety of pharmacological effects. It has been found to promote hepatocyte growth factor, limit lipid peroxidation, and inhibit apoptosis in acute hepatic injury animal models. Besigomsine also acts as an anti-inflammatory by preventing the release of arachidonic acid in macrophages in vitro. Laboratory evidence suggests that Besigomsine may have anticarcinogenic effects. Chronic administration of Gomisin A had an antihypertensive effect in AngII-induced hypertensive mice. Gomisin A may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. Also it induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway.

Quinotolast (also known as FK021) is an orally active mast cell stabilizer which has a cytoprotective effect on the gastric mucosa. Quinotolast was patented in 1985 by Japanese pharmaceutical company Fujisawa Pharmaceutical Co., Ltd. as an antiallergic and antiulcer agent. In preclinical models, Quinotolast potently inhibited such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. Quinotolast inhibited histamine release from rat peritoneal cells, but it had no antagonistic effect on histamine-, serotonin-, platelet activating factor- or bradykinin-induced cutaneous reactions in rats. Moreover, it was clearly demonstrated that quinotolast and DSCG had a cross tachyphylaxis to inhibit PCA in rats, suggesting that these drugs, at least in part, share the same mechanism of action. Quinotolast caused a significant increase in the mucociliary transport rate in quails. Quinotolast significantly depressed the cough reflex induced by citric acid in normal and bronchitic guinea pigs.

Aranotin, a metabolite of Arachniotus aureus, possesses the antiviral and antibiotic properties. It inhibits viral RNA synthesis against strains of rhino-, coxsackie, polio- and parainfluenza viruses.

Sparfosate (PALA) is a stable transition state analogue for an aspartate transcarbamylase- cartalyzed reaction with antineoplastic activity. PALA is a potent inhibitor of aspartate transcarbamylase (Ki about 10(-8) M for ACTases of various origins), which in whole cells blocks the de novo synthesis of pyrimidines. Thus PALA inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA. In vivo, low doses of PALA inhibit whole body pyrimidine synthesis. While this action is cytotoxic in vitro, extensive human testing demonstrates that PALA alone is devoid of selective antitumor activity. Interest in the therapeutic action of PALA derives from the demonstration that its action potentiates the cytotoxicity of several cytotoxic drugs, notably 5-fluorouracil (5-FU). Development of Sparfosate for cancer and Hepatitis B treatment is assumed to have been discontinued.

Satigrel (previously known as E5510) was developed as an antithrombotic agent. Satigrel antagonized platelet activation by inhibiting phospholipase C and/or A2, which results in suppression of both phosphatidylinositol breakdown and arachidonic acid release from phospholipids, as well as by inhibiting cyclooxygenase. Satigrel was studied in patients with intermittent claudication due to arteriosclerosis obliterans, where the drug improved the cutaneous circulation and symptoms of patients. In addition, the therapeutic effect of satigrel was studied on biopsy-proven chronic rejection after kidney transplantation. Also was shown that the drug had a clinical benefit over aspirin for the treatment of transient ischemic attacks. However, all these studied were apparently discontinued.

Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.

Bucricaine is tetrahydroaminoacridine derivative that has been studied as acetylcholinesterase and monoamine oxidase inhibitor. In animal models, Bucricaine shows a wide spectrum of pharmacological properties, which include analgesic, local anesthetic, analeptic, and respiratory stimulant activities.

Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.