Tamitinol (also known as EMD 21657), a neurotropic drug that was developed as a cognition enhancer for the treatment of diffuse cerebral disease and organic brain syndrome. Tamitinol participated in clinical trials where the therapeutic effects of the drug were shown to be statistically significant compared to placebo in the global response. However, the treatment was interrupted because of side effects (increased aggressiveness, rash) in 2 cases.

Gamfexine (WIN 1344) was introduced in the literature in 1966 as an anti-depressant. Although it was reported to be effective in the treatment of withdrawal in schizophrenia, it worsened psychotic symptoms.

Arecoline is a natural alkaloid and is an effective constituent of Areca catechu L. (Arecaceae) with various pharmacological activities including effects on nervous, cardiovascular, digestive and endocrine systems and anti-parasitic effects. Antinociception of arecoline is mediated by the activation of the muscarinic acetylcholine receptors. It was found that this compound leads to oral submucosal fibrosis and oral cancer. Lung cancer is a severe type of carcinoma with high cell motility that is difficult to treat. As a result, further studies are needed to reduce or eliminate the toxicity of the compound before developing into a new drug.

Sematilide (CK-1752) was developed as a novel class III antiarrhythmic agent for the arrhythmia treatment. Sematilide blocks the inward rectifier potassium channel (IK1). The further development of the drug was discontinued.

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.

Eproxindine (KC 3791) is an antiarrythmic. It is able to inactivate voltage-dependent sodium channels. Eproxindine also proved to be capable of blocking open potassium channels at outwardly directed potassium currents

Cetocycline (formerly chelocardin or cetotetrine) is tetracycline derivative with potent antibacterial activity against a number of Gram-positive and Gram-negative multi-resistant pathogens. Cetocycline was found to be more active than tetracycline against many clinical isolates of aerobic gram-negative bacilli, but is less active against staphylococci, and has no activity against Pseudomonas. At low concentrations, like classical tetracyclines, chelocardin induces the proteomic signature for peptidyl transferase inhibition demonstrating that protein biosynthesis inhibition is the dominant physiological challenge. At higher concentrations B. subtilis mainly responds to membrane stress indicating that at clinically relevant concentrations the membrane is the main antibiotic target of chelocardin.

Sodium taurodeoxycholate is a bile salt-related, anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. It is formed by the conjugation of ursodeoxycholic acid (UDCA) with taurine. Sodium taurodeoxycholate and ursodeoxycholic acid are major constituents of black bear bile, which has been used in traditional Chinese medicine for thousands of years. Bear bile was historically employed to treat a number of diseases including jaundice, summer diarrhea, abdominal pain due to hepatobiliary diseases and gastric malfunction, biliary ascariasis, infectious skin diseases, the common cold, intestinal worms, and inflammation of the throat. Sodium taurodeoxycholate has been shown to inhibit apoptosis by modulating mitochondrial membrane perturbation and pore formation, B cell lymphoma 2 (Bcl-2)-associated protein X (BAX) translocation, cytochrome c release, and caspase activation. Sodium taurodeoxycholate inhibits amyloid beta (Ab)-induced apoptosis and attenuates the endoplasmic reticulum (ER) stress, which are thought to be key components of the pathological process in certain diseases. In clinical studies, Sodium taurodeoxycholate is shown to be very safe with oral administration of 1500 mg/day for up to 6 months. In a more recent clinical study, a dose of 1750 mg/day for up to 4 weeks was well tolerated in healthy obese persons. One of the major adverse effects of Sodium taurodeoxycholate is diarrhea. Based on the related information from ursodeoxycholic acid, other gastrointestinal side effects are possible including abdominal pain, flatulence, nausea, dyspepsia, and anorexia.

Revenast is an anti-allergic compound that is rapidly and extensively metabolized in animals. It is not acting as an anti-histaminic. Revenast has low bioavailability (reported in monkeys) and high protein binding (in humans). Information about current use of this compound is not available.

FETOXYLATE, a phenoxyethyl ester of diphenoxylate, is an opioid receptor agonist. It is used as antidiarrheal.