Tizolemide is a sulphonamide diuretic. The effect on transepithelial Na transport of tizolemide was investigated in isolated frog skin (Rana temporaria). It was found that tizolemide (2-5 mM, serosal side) decreased transepithelial Na transport (measured as short circuit current and as net sodium flux) within 60 min to 25-40% of the control level resulting from reduction of the unidirectional sodium influx. Tizolemide has alkaline properties and is cleared by a tubular transport system which differs from the PAH-excreting system which transports thiazide diuretics. Tizolemide was almost completely absorbed from the gastrointestinal tract. The drug was mainly eliminated via tubular secretion. Renal clearance of the drug was much lower in patients with compensated cardiac failure than in healthy subjects because of low renal plasma flow. As a consequence, plasma half-life was prolonged considerably in some patients. It was concluded that drugs with mainly tubular renal elimination may have a reduced elimination rate in patients with cardiac diseases despite normal glomerular filtration rate.

Phenethyl isothiocyanate (PEITC) presents in cruciferous vegetables which have been shown to decrease the risk of various types of malignancies. PEITC targets multiple proteins to suppress various cancer-promoting mechanisms such as cell proliferation, progression and metastasis. PEITC induces apoptosis in human colon cancer HT-29 cells, prostate cancer cells, and osteogenic sarcoma U-2 OS cells. Unique to prostate cancer is that PEITC downregulates the transcriptional factor Sp1, a regulator of AR expression. PEITC suppresses 4-(methylnitrosamino)-1-(3-pyridyl)-1-butoneinduced pulmonary neoplasia in A/J mouse lung, exhibits cancer chemopreventive activity in rat and reduces azoxymethane-induced colonic aberrant crypt foci formation. PEITC appears to be a promising agent for cancer therapy and is already under clinical trials for leukemia and lung cancer.

Meclinertant (SR-48692) is the first non-peptide antagonist of neurotensin receptors. It is potent and selective vs the high-affinity binding sites and with a small activity on the levocabastine-sensitive binding sites. It is active on several species including man without partial agonist properties. In vivo, it is active by oral route with a long duration of action and it is able to cross the blood-brain barrier. Meclinertant may be considered a powerful tool for investigating the role of neurotensin in physiological and pathological processes. Meclinertant has been developing for the treatment of anorexia nervosa; colorectal cancer; irritable bowel syndrome; pain; pancreatic cancer; prostate cancer; schizophrenia; small cell lung cancer however its development was discontinued.

Ciclotropium is quaternary ammonium compound with anticholinergic and parasympatholytic activity. Oral Cyclotropium bromide inhibited fasting and meal-stimulated colonic motility significantly without causing adverse side effects. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying.

Seletracetam, a pyrrolidone derivative is a new drug in epilepsy development. Seletracetam has high binding affinity to the synaptic vesicle 2A (SV2A) protein. In addition, was discovered, that the drug bound to N-type calcium channels and inhibited high-voltage-activated Ca2+ currents and intracellular Ca2+ increase. Seletracetam participated in Phase III clinical trials; however, all these studies for the treatment of epilepsy were terminated. Moreover, it is unknown whether planned phase IIb/III trials will begin.

Saperconazole, a N-1-substituted triazole antifungal that is a selective inhibitor of the cytochrome P-450-dependent ergosterol synthesis in Candida albicans, Aspergillus fumigatus, and Trichophyton mentagrophytes. Saperconazole participated in a clinical trial for the treatment of mycoses. However, further, development was discontinued because of concerns about the possibility of drug-induced carcinogenesis.

Ormaplatin (NSC 363812, tetraplatin) is a stable platinum (IV) analog. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. Ormaplatin showed marked antitumor activity both in vitro and vivo. The severe, cumulative and irreversible peripheral neurotoxicity observed in phase I studies resulted in termination of further clinical development of ormaplatin.

Cetylamine is an aliphatic primary amine that possesses surface-active properties and widely used in water treatment. Cetylamine shows moderate anti-tuberculosis activity. Cetylamine also may be used as a source of fluoride in the prevention of dental caries.

Furomazine, a sedative agent, was studied as a neuroleptic. However, information about the current use of this compound is not available.