Rodocaine (R 22.700) is a biochemical that was found to be an effective anesthetic in ophthalmology. This compound is suitable for topical use but can be injected as well. A pharmaceutically acceptable, acid-addition salt of rodocaine can be prepared by reaction of the rodocaine free base with the desired acid. Rodocaine has furthermore been mentioned as a potential anesthetic agent in antimicrobial compositions.

Synthélabo developed a saripidem (also known as SL 850274) as a potential anxiolytic agent that modulates the benzodiazepine-binding site on GABAA receptor via primary binding with ω1 subtype. Saripidem was studied in phase II clinical trials for the treatment of patients with anxiety disorders. However, information about the further development of the drug is not available.

Etaminile is an antitussive agent.

Dextofisopam, a non-serotonergic agent currently being evaluated for the treatment of irritable bowel syndrome (IBS), is the R-enantiomer of racemic tofisopam, a molecule marketed and used safely outside the United States for over three decades for multiple indications including IBS. Dextofisopam represents a novel, first-in-class opportunity with a positive proof-of-concept study in an arena where there are few compounds with unique approaches or positive efficacy results. By structure, Dextofisopam is a member of the homophthalazine class; Dextofisopam binds to specific receptors in areas of the brain affecting autonomic function, including gastrointestinal (GI) function. Unlike the two 5-HT3 or 5-HT4 mediated IBS therapies currently available, both with significant safety concerns, Dextofisopam novel non-serotonergic activity offers a unique and innovative approach to IBS treatment. Recent studies have indicated that dextofisopam binds to a novel binding site within the central nervous system that may be responsible for mediating its actions. This receptor has been characterized as the 2,3-benzodiazepine receptor, which is distinct from the classical 1,4 or 1,5-benzodiazepine receptor. Dextofisopam has no significant binding at other receptors or ion channels

Cianopramine is a highly potent inhibitor of neuronal serotonin (5-HT) uptake developed by Hoffmann-La Roche for major depression treatment. In preclinical studies, acute and chronic treatment with Cianopramine shows clear behavioural effects Cianopramine increases neophobic reactions in the free exploration test, the avoidance reaction to a brightly illuminated chamber in the light/dark choice procedure as well as to open arms in the elevated plus-maze test. In a double-blind trial, Cianopramine effective in reducing scores on the Hamilton Psychiatric Rating Scale for Depression and on a global scale. Unfortunately, Cianopramine administrations were associated with significant adverse effects and future development was discontinued.

Ibuterol, a prodrug that is rapidly hydrolyzed to form a drug, terbutaline. Terbutaline, a beta-2 adrenergic agent used to treat asthma.

Carperone is a fluorobutyrophenone compound which in animal studies has showed calming or tranquilizing effects resembling those of haloperidol, trifluperidol, and other antipsychotic drugs

Prifelone (also known as R-830) is a thiophene derivative patented by American pharmaceutical company Riker Laboratories, Inc. As an antiinflammatory, analgesic, and antipyretic compound. In vitro, Prifelone acts as a nonsteroidal anti-inflammatory drug and inhibits guinea pig lung lipoxygenase and bovine seminal vesicle cyclooxygenase. In preclinical studies, Prifelone shows potent anti-inflammatory activity in carrageenan-induced edema and adjuvant arthritis of the rat and ultraviolet-induced erythema in the guinea pig

Revospirone (BAY VQ 7813) is a pyrimidinylpiperazine derivative that acts as partial agonist at 5-HT1A receptors. Head shakes were reported after administration of revospirone in pigs, and once daily administration for 3-5 days led to a reduction in this head shake response. No behavioral alterations were observed. This compound was never marketed

Methoxyphedrine (para-methoxymethcathinone, 4-methoxymethcathinone, bk-PMMA, PMMC, Methedrone, 4-MeOMC) is a phenethylamine, amphetamine, and cathinone derivative that acts as a triple reuptake/release/reversible monoamine oxidase inhibitor and used as a recreational drug. Methedrone has been found to be a potent serotonin transporter (SERT) and norepinephrine transporter (NET) inhibitor, but a weak dopamine transporter (DAT) inhibitor. Methedrone induces the transportation mediated release of NE, DA, and 5-HT from cells preloaded with monoamines making it a serotonin-norepinephrine-dopamine (SNDRA) releasing agent, also known as triple releasing agent (TRA), which is a common characteristic among drugs of abuse. The health risks associated with Methedrone are unknown but are expected to be similar to other cathinones. The deaths of two young men in southeast Sweden in 2009 were attributed to Methedrone overdose.