Girisopam (GYKI 51189), a 2,3-benzodiazepine, is a compound with anxiolytic and antipsychotic action. It has shown these effects in several animal models. Girisopam differs from the traditional 1,4-benzodiazepines because of its selective anxiolytic action without muscle relaxant and anticonvulsive activity, and because it does not have affinity for 1,4-benzodiazepine receptors. Antidepressant activity of girisopam was also reported. The binding site of girisopam in neuronal cells in the central nervous system is located exclusively to the basal ganglia. Because the danger of tolerance and dependence is lower for 2,3-benzodiazepine than 1,4-benzodiazepines, girisopam may potentially be used in treatment of addiction and affective disorders. No clinical trials were conducted in the US.

Flutroline, an antipsychotic drug that was studied to treat patients with schizophrenia. Clinical trials have shown that the drug was a safe, effective, and 20 mg and above offered the best potential for optimal clinical effectiveness. However, information about the further development of this drug is not available.

Sulazepam is a desmethylbenzodiazepine. It is the thioamide derivative of diazepam. It has sedative, muscle relaxant, hypnotic, anticonvulsant and anxiolytic properties like those of other benzodiazepines. Sulazepam in vivo in experimental animals undergoes enzymic desulfonation, demethylation, and [3C] hydroxylation, with the formation of basic metabolites: diazepam, desmethyldiazepam, and oxazepam.

Quindoxin (quinoxaline-1,4-dioxide), a former 'growth promoter' used in animal husbandry, has been taken from the market because of its photoallergic properties. Quindoxin increased the live weight gain in young chickens, pigs, and poultry. Quindoxin showed little antibacterial activity in vitro against common gram-positive or gram-negative species under aerobic conditions, but its activity was 10-100 times greater under anaerobic conditions. Under anaerobic conditions, Quindoxin inhibited the growth of Staphylococcus aureus and Escherichia coli. Quindoxin derivatives olaquindox and carbadox have been used as feed additives for growth promotion in pigs, rabbits, and other animals. It is extremely difficult for breeders to avoid exposure to dust containing relatively high concentrations of olaquindox. A very low dose of olaquindox produces contact dermatitis mainly by phototoxic or photoallergic mechanisms.

Bicyclomycin has been used to treat diarrhea in humans and bacterial diarrhea in calves and pigs and is marketed by Fujisawa (Osaka, Japan) under the trade name Bicozamycin. This drug is the selective inhibitor of rho, a member of the RecA-type ATPase class of enzymes that use nucleotide contacts to couple oligonucleotide translocation to ATP hydrolysis.

Clemeprol is an antidepressant drug of the 3,3-diraylpropyl-amine type. It exhibits antireserpine activity in animal tests, inhibits the neuronal uptake of noradrenaline. The drug was used in the clinic for the treatment of depression in the 1980s, but no development was reported since.

Tigestol is an Estrene derivative patented by Organon Laboratories Ltd. as an anabolic, androgenic, and progestative agent.

Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.

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.