Taziprinone was studied as an antitussive agent. Information about the current use of this compound is not available.

Gliflumide is a compound with a long-lasting hypoglycemic effect. This blood glucose lowering sulfonamide has shown a large decrease of blood glucose levels in healthy volunteers who where administered the drug orally or intravenously. A very similar reaction but delayed and prolonged response was observed for this drug compared to other insulin secretion-stimulating compounds (such as glibenclamide). High affinity of gliflumide to plasma proteins has been suggested to contribute to this delayed activity.

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.

Mesocarb (sydnocarb or 3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychomotor stimulant N-alkylated amphetamine derivative. Mesocarb is a selective inhibitor of dopamine uptake, it potently blocks dopamine transporter. It is very likely that mesocarb is being used by drug addicts. Mesocarb is included in the World Anti-Doping Agency’s list of substances and methods that are prohibited in sports. It is used in Russia for the treatment of a variety of neuropsychiatric comorbidities.

Modithromycin (EDP-420, EP-013420, S-013420) is 6-11-bicyclic erythromycin derivative patented by Enanta Pharmaceuticals, Inc as an antibacterial agent. In preclinical studies, Modithromycin exhibited high levels of in vitro activities against N. gonorrhea, including isolates resistant to azithromycin, cefixime, ceftriaxone, spectinomycin, ampicillin, tetracycline, and ciprofloxacin. Modithromycin also has the good in vivo efficacy against S. pneumoniae and H. influenzae, which might be due to its lasting intracellular activity. In healthy adults, clinical trials Modithromycin shows long half-life and its high systemic exposure. Modithromycin was well tolerated, with no serious or severe adverse events reported, and no subject was discontinued from the study due to an adverse event. In 2005 Modithromycin was studied in phase II clinical trials but no further development reports were published.

Fluorescein Lisicol (NRL972) is a fluorescent-labelled bile acid analog that is used as an investigational marker for liver function, specifically hepatic biliary transporter function. Fluorescein Lisicol has been used in trials investigating the pharmacokinetics of hepatic cirrhosis, viral hepatitis, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.

NeuroSearch was developing brasofensine (or NS 2214), an oral dopamine reuptake inhibitor for the treatment of Parkinson's disease. Brasofensine successfully passed phase II clinical trial in patients with Parkinson's disease, The drug was safe and well tolerated. However, NeuroSearch discontinued the development of the drug because of the cis-anti isomerization of the 2α-methyloxime group of brasofensine in favor of NS 2230.

Dexsecoverine ia an antimuscarinic drug.

Cathinone is one of the biologically active alkaloids found in the khat shrub (Catha edulis). Due to its psychoactive properties, khat has been known and utilized for ages by the inhabitants of East Africa and the northeastern parts of Arabian Peninsula. In many regions, chewing of freshly collected khat leaves (thus liberating cathinone, which affects the central nervous system) is considered a matter of culture and local tradition. Because of their structural similarity to amphetamine, cathinone and its analogs are often denoted as “natural amphetamines”, and the only structural difference between amphetamine and cathinone is the presence of a carbonyl group in the α-position of cathinone’s side chain. Similar to amphetamine, cathinone and its analogs are characterized by stimulating, euphoric, and empathogenic properties. Due to their effects on the central nervous system, the first synthetic cathinone derivatives were synthesized for medicinal purposes in the early twentieth century, but they began attracting wider attention around the year 2000. At that time, synthetic cathinones were included in a broader group of psychoactive compounds denoted as “legal drugs” or “designer drugs”