Fazadinium (used as a bromide salt) is a muscle relaxant, which was applied in anesthesia under the name Fazadon. The current marketing status is unknown and the drug is supposed to be discontinued.

Fabomotizole (also known as Afobazole) is a selective non-benzodiazepine anxiolytic which was developed in Russia and launched in 2006. The drug is used for the treatment of wide range of diseases: generalized anxious disorders, neurasthenia, adaptation disorders, sleep disorders, for alleviation of withdrawal syndrome. According to the drug label (in Russian), its action is related to the interaction with sigma-1 receptors.

Butanilicaine (Hostacain) is a local anesthetic. It uses may associate with a risk of allergy. Butanilicaine has a vasodilator effect.

Xylamidine is a peripherally-restricted antagonist of 5HT2A and 5HT1A receptor. It is used to study the role of the serotonin receptors in the regulation of food intake, cardiovascular function, and regulation of body temperature.

Toliprolol is beta-adrenergic blocker. It was developed as antianginal and antihypertensive agent. Toliprolol is moderately lipophilic. It appears to have the appropriate characteristics for cerebral beta-adrenoreceptor imaging. However, tissue uptake of toliprolol was dominated by the nonspecific binding, both in the brain and in peripheral target organs, such as heart and lung. Toliprolol seems unsuitable for visualization of cerebral beta-adrenoceptors. After application of ethanol to mice, the content of glycogen of the liver and the brain decreased. By pretreatment with the beta-sympatholytic agent toliprolol, the ethanol-induced break-down of glycogen was partially blocked in the liver and completely abolished in the brain. In contrast, mainly synergistic effects of ethanol and toliprolol on the glycolysis of the liver and the brain were found. Toliprolol reduced the greater variance during the emotionally stressful situation in doses insufficient to diminish the mean increase in forearm blood flow.

Aclatonium (also known as aclatonium napadisilate) is a cholinergic agonist that has been developed and used in Asia as an activator of gastrointestinal motility.

Indisetron dihydrochloride (N-3389) was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004. It was co-developed and co-marketed as Sinseron by Kyorin & Yakult Honsha in Japan. Indisetron is a dual serotonin 5-HT3 and 5-HT4 receptor antagonist. It is indicated for the treatment of prophylaxis of chemotherapy-induced nausea and vomiting, it’s administered once daily. Indisetron is metabolized in the liver, and CYP1A1, CYP2C9, CYP2D6, and CYP3A4 are involved in its metabolism. However, indisetron is unlikely to cause drug interactions at clinical doses because the effective plasma concentrations are lower than those necessary for inhibiting the metabolic enzymes. No drug interaction has been reported. Indisetron antagonizes 5-HT4 receptors, as well as 5-HT3 receptors, and this characteristic is expected to contribute to its clinical efficacy.

Indanazoline, an imidazoline derivative, (E-VA-16, as monohydrochloride active substance of Farial) is a nasal decongestant. As a nasal spray it can be used for the treatment of acute, chronic and allergic rhinitis. It is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically Indanazoline being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives.

Propiram is an orally administered analgesic with partial morphine-like agonist and weak antagonist properties. Analgesic efficacy of propiram, usually 50 or 100mg, appears comparable to that of standard dosages of other oral opioid drugs [i.e. pentazocine, pethidine (meperidine)] in patients with acute pain of moderate to severe intensity arising from various gynaecological and surgical procedures, and may be superior to codeine in gynaecological and postoperative dental pain. Propiram is a non-addictive analgesic for the relief of moderate-to-severe pain. Propiram reached Phase III clinical trials in the United States and Canada, but was discontinued. Propiram is a partial opioid mu receptor agonist.

Mefenorex or (+/-)N-(3-chloropropyl)-1-methyl-2-phenylethylamine is an N-alkylated analogue of amphetamine. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. Mefenorex is considered to be racemic mixture, no available data regarding enantiospecific pharmacological activity of the compound.