Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.

Dipraglurant (ADX48621) is a novel, potent mGluR5 negative allosteric modulator that reduced the severity of drug-induced dyskinesia in Parkinson's disease. Dipraglurant pharmacokinetic variables were similar to those of levodopa, suggesting that both drugs can be co-administered simultaneously in further studies. Dipraglurant might be useful in torsion dystonia treatment also. Detected adverse events are: sweating, dyskinesia, nausea, dizziness, and anxiety. One serious adverse event described as possible syncope.

Soretolide is an orally active benzamide derivative with anticonvulsant effects and a similar profile of activity to carbamazepine. In animal models, soretolide showed an anticonvulsant profile similar to carbamazepine, being active in the maximal electroshock test and poorly active against pentylenetetrazole-induced seizures. Researchers at the University of Washington, USA and Laboratoires Biocodex, France were investigating the potential use of soretolide as an anticonvulsant. However, development of the compound appears to have been discontinued.

Altinicline (SIB-1508Y, SIB-1765F) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models, and progressed as far as Phase II clinical trials for Parkinson's disease, where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear.

Taranabant is a highly selective cannabinoid-1 (CB1) receptor inverse agonist developed by Merck & Co for the treatment of obesity. The Phase III taranabant study involved about 2,400 patients and was to be conducted for two years. In March 2008, after completion of 52 weeks of the study, Merck reported positive results of the drug in conjunction with diet and exercise in obese patients. The patients experienced double the amount of weight loss by taking 2mg of taranabant when compared to the patients treated with placebo. However, in October 2008, the company discontinued the Phase III programme and clinical development of taranabant because of its side effects. The drug showed gastrointestinal and psychiatric side effects such as increased anxiety, depression and irritability. Merck had previously planned to file for regulatory approval with the US Food and Drug Administration in 2008, but subsequently withdrew it.

Meobentine is an antiarrhythmic agent. Meobentine significantly increases the electrical ventricular fibrillation threshold in animal models. Meobentine may prevent induction of ventricular tachycardia or fibrillation, or reduce frequency of complex ventricular ectopy in selected patients refractory to other antiarrhythmic agents, but the response rate is relatively low.

Nerisopam [EGIS 6775, GYKI 52322] is a novel 2,3-benzodiazepine derivative with both anxiolytic and antipsychotic activity in animal studies. Nerisopam induces rapid, intense expression of Fos-like immunoreactivity in the rostral, dorsomedial and lateral parts of the striatum in the rat. The striatal neurons are the primary targets of this anxiolytic and antipsychotic drug in the central nervous system. Nerisopam does not bind to the central dopamine receptors, but it shows affinity to the 5-HT1 receptors (IC50 = 7.1 x 10(-6) mol/l) and inhibits brain cAMP-phosphodiesterase (IC50 = 2.4 x 10(-5) mol/l). Nerisopam development for the treatment of anxiety disorder and schizophrenia were discontinued in phase 1.

Beloxamide, a hypolipidemic agent, produced regression of the lipid deposits that was shown during experiments with rodents.

Epetirimod (S-30563 or TAK-851) is an immunostimulant. The compound is structurally related to the marketed topical imidazoquinoline drug, imiquimod, an agonist of Toll-like receptor 7. Epetirimod was under development with Takeda Pharmaceutical as a topical treatment for cervical high-risk HPV infection and cervical dysplasia. Takeda has discontinued epetirimod development as it did not meet the predefined efficacy end points in a US Phase II trial.