Etilamfetamine (Apetinil) is a stimulant drug of amphetamine chemical class. It is an N-substituted amphetamine with an ethyl group on the amphetamine backbone. It was used as an anorectic or appetite suppressant. Etilamfetamine is a psychoactive drug, which can be used as a recreational drug. Etilamfetamine has been abused as a “designer drug” alternative to amphetamine and possibly methamphetamine. It is a dopamine releasing agent.

Zetidoline (DL-308) is an antipsychotic drug with antidopaminergic properties. It is a dopamine D2 receptor antagonist. DL-308 displayed sedative properties, as indicated by the sedated appearance of the subjects, by a decrease in subjectively rated alertness and by an impairment of performance on psychomotor tests. DL-308 appeared to be a more potent sedative than thioridazine. DL-308 (10 mg) caused an increase in subjectivey rated sweating and objectively measured heart rate, suggesting a sympathomimetic property for the drug. DL-308 had effects consistent with an alpha-adrenolytic action; it caused miosis, hypotension and a decrease in salivation. DL-308 had little effect on the motor system, as indicated by conventional clinical neurological examination.

Dipyrocetyl (2,3-diacetyloxybenzoic acid) is a drug used as an analgesics and antipyretics. Besides, was shown, that it may be useful in the treatment of acute lung injury (ALI) associated with acute respiratory distress syndrome (ARDS). Dipyrocetyl possesses the anticoagulation properties, which may contribute directly to improve tissue integrity as well as indirectly by the prevention of activation of pro-inflammatory cytokines. In addition, was made a suggestion, that the drug may function as an MMP inhibitor.

Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia (ALL) and may have applications in treating other disorders such as mantle cell lymphoma (MCL). The mechanism by which acadesine selectively kills B-cells is not yet fully elucidated. The action of acadesine does not require the tumour suppressor protein p53 like other treatments. This is important, as p53 is often missing or defective in cancerous B-cells. Studies have shown acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes. Antiapoptotic proteins of the Bcl-2 family regulate MCL cell sensitivity to acadesine and combination of this agent with Bcl-2 inhibitors might be an interesting therapeutic option to treat MCL patients. Acadesine has anti-ischemic properties that is currently being studied (Phase 3) for the prevention of adverse cardiovascular outcomes in patients undergoing coronary artery bypass graft (CABG) surgery. Adenosine itself has many beneficial cardioprotective properties that may therefore be harnessed by this new class of drugs. Unlike adenosine, acadesine acts specifically at sites of ischemia and is therefore void of the systemic hemodynamic effects that may complicate adenosine therapy. Animal and in vitro studies have established acadesine as a promising new agent for attenuating ischemic and reperfusion damage to the myocardium. Acadesine also possesses the theoretical (but unproven) benefit of attenuating reperfusion injury after acute myocardial infarction (MI). Further research is needed to define the full potential of this unique agent in various clinical situations involving myocardial ischemia.

Epristeride is a steroid 5-alpha-reductase inhibitor developed for the treatment of prostatic hyperplasia and acne. The drug reached phase III clinical trial for hyperplasia in the UK, the US and Japan, however, the current status of the drug is unknown.

Zenarestat (FK-366; FR-74366) is an aldose reductase (AR) inhibitor investigated as a treatment for diabetic neuropathy and cataract. Zenarestat is a highly specific AR inhibitor, it did not affect the activities of enzymes in the glycolysis pathway, the pentose-phosphate pathway and NADPH-dependent enzymes such as NOS and glutathione reductase. Zenarestat exhibited some inhibition of aldehyde reductase, the most closely related enzyme to AR, however, its IC50 was evidently higher than that for AR. Zenarestat dose-dependently reduced the elevated sorbitol concentration in the lens, retina sciatic nerve, and renal cortex. The most potent effect of zenarestat was seen in the sciatic nerve. Zenarestat inhibits cataract formation and to counteract reduced motor nerve conduction velocity in the streptozotocin-induced diabetic rat. Zenarestat had been in clinical trials for the treatment of diabetic neuropathy however future development was discontinued due to dose-dependent renal toxicity.

Gadofosveset trisodium is an intravenous contrast agent used with magnetic resonance angiography (MRA), which is a non-invasive way of imaging blood vessels. The agent allows for the vascular system to be imaged more clearly by the MRA. In this way, gadofosveset trisodium is used to help diagnose certain disorders of the heart and blood vessels. Gadofosveset binds reversibly to endogenous serum albumin resulting in longer vascular residence time than non-protein binding contrast agents. The binding to serum albumin also increases the magnetic resonance relaxivity of gadofosveset and decreases the relaxation time (Tl) of water protons resulting in an increase in signal intensity (brightness) of blood. The extended acquisition time and increased relaxivity of gadofosveset allows for longer steady-state acquisition times, and potentially submillimeter voxels. Overlay of veins in steady-state MR angiography is less of a problem in multiplanar reformats with this level of resolution. This is particularly promising for MR evaluation of the peripheral vasculature. In the United States, gadofosveset is FDA-approved only for use in aortoiliac disease, with other uses being off-label. It currently does not have a role in hepatic imaging.

Nafamostat mesilate (NM), a synthetic serine protease inhibitor, has anticoagulant and anti-inflammatory properties. Nafamostat is approved and marketed in Japan. It relieves symptoms such as pain due to inflammation of the spleen. It improves visceral disorders and bleeding tendency caused by blood clotting tendency in the vessels. It prevents coagulation in the blood circuit during hemodialysis. It is usually used to improve acute symptoms of pancreatitis (acute pancreatitis, acute exacerbation phase of chronic pancreatitis, post-operative acute pancreatitis, acute pancreatitis after pancreatography, traumatic pancreatitis) and to prevent disseminated intravascular coagulation (DIC) and clotting of perfusing blood in extracorporeal blood circuit. Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa.

Phosmet is a non-systemic, organophosphate insecticide used on both plants and animals. Phosmet is mainly used on apple trees for control of coddling moth, though it is used on a wide range of fruit crops, ornamentals and vines for the control of aphids, suckers, mites and fruit flies. Phosmet is a moderately potent cholinesterase inhibitor.

Sofalcone is a mucosal protective agent that has been reported to inhibit growth of Helicobacter pylori. It is considered safe and effective for the treatment of gastritis and gastric ulcer. It is used in Japan. Adverse reactions are: liver dysfunction, jaundice, rash, constipation, dry mouth, heartburn.