Rilmazafone (previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan. It has sedative and hypnotic effects. Rilmazafone induces impairment of motor function and has hypnotic properties. Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg.

Bumetrizole is an ultraviolet light absorber (UVA) of the hydroxyphenyl benzotriazole class, which imparts outstanding light stability to plastics and other organic substrates. Bumetrizole is also approved by the FDA as a stabilizer in polymers used in producing, manufacturing, packaging, processing, and transporting food. Bumetrizole has a wide range of indirect food approvals in polyolefins. It has a low volatility at high temperatures and high resistance to thermal degradation and can, therefore, be used without significant loss or decomposition in the polyolefin compounding and molding processes.

Bucumolol is a beta-adrenergic antagonist. It can be used in the treatment of myocardial ischemia and hypertension.

Ditophal was used for the treatment of leprosy.

Levotofisopam is the S-enantiomer of racemic tofisopam Monotherapy with levotofisopam led to clinically meaningful reduction of Serum Uric Acid (SUA) in patients with hyperuricemia and gout. Treatment was generally well tolerated with 23% of the patients experiencing gout flare. Increased fractional excretion of uric acid suggests that levotofisopam reduces SUA primarily through uricosuric activity. These results support further studies to investigate the potential role of levotofisopam for in the treatment of hyperuricemia in gout. Levotofisopam prescribed outside the United States for such stress-related disorders as anxiety, functional gastrointestinal disorders, and symptoms of menopause. Thought to affect autonomic tone via interaction with subcortical 2,3-benzodiazepine receptors, levotofisopam has shown promise in animal models of stress-related gastrointestinal dysfunction and menopause. We conducted a trial of levotofisopam in healthy human volunteers.Also was showed, that levotofisopam significantly reduced both objective and subjective measures of hot flash frequency in postmenopausal women within 7 days of treatment.

Probicromil is a Histamine H1 antagonist. It was taken to the clinic and found to be effective in exercise and antigen challenge. Probicromil inhibited Ascaris-induced bronchoconstriction and the increase in plasma histamine levels seen after Ascaris inhalation. Therapeutic efficacy in seasonal rhinitis was also demonstrated. Further clinical studies were halted because of a side-effect associated with the compound, namely a sensation of warmth (especially in the perineal region) experienced by some volunteers after inhalation.

Butofilolol (trade name Cafide) is a beta-blocker drug for the treatment of high blood pressure (essential hypertension). Butofilolol constitute a good therapeutic approach to hypertension in plethoric subjects when the weight reduction has failed to correct it adequately

Alifedrine, a beta-adrenergic partial agonist, significantly improved performance of the failing heart. Alifedrine resulted in a significant dose-dependent increase in cardiac output. There were significant reductions in peripheral resistance, but little observed change in arterial pressure. With intravenous alifedrine, there were significant increases in stroke volume with little change in heart rate. With the 40 mg oral dose, there was a small increase in heart rate There were no clinically or statistically significant changes in arterial (non-invasive), pulmonary artery, pulmonary capillary or right atrial pressures with any dose of alifedrine. No significant arrhythmias were noted clinically with the doses studied.

Befunolol is a beta-adrenergic receptor blocker approved in Japan for the treatment of open-angle glaucoma. The current drug status is unknown.

Baxitozine is a Histamine H2 receptor antagonist. It has a cytoprotective, antisecretory and antiulcer properties. In situ, baxitozine inhibited acid secretion stimulated by histamine or pentagastrin but was inactive against carbachol. It also had antiulcer activity against stress ulcers (restraint plus cold). It had marked gastric cytoprotective activity in rats against the necrotizing effects of ethanol. This cytoprotective activity was not significantly affected by indomethacin pre-treatment. Baxitozine has been in phase II clinical trials for the treatment of gastric ulcer. However, this research has been discontinued.