Milveterol (also known as GSK159797) was developed as a longer-acting beta2 adrenoceptor agonist for the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Milveterol completed phase II clinical trials for asthmatic subjects. However further development of the drug was discontinued.

Elopiprazole [DU 29894 or 1-(7-benzofuranyl)-4-[[5-(4-fluorophenyl)-1-H-pyrrol-2yl]methyl]piperazine) is an antagonist at dopamine D2 and D3 receptors and an agonist at serotonin1A receptors. Elopiprazole development for the treatment of psychotic disorders has been discontinued.

Manifaxine (GW 320659) is a highly selective neuronal norepinephrine and dopamine re-uptake inhibitor. It has been in phase II clinical trials by GlaxoSmithKline for the treatment of attention deficit hyperactivity disorder and obesity. Manifaxine development has been discontinued.

Albutoin has been shown to have an anticonvulsant activity against clonic and tonic experimental seizures in mice and rats, particularly those induced by pentylenetetrazol. The first report, in 1959, of the clinical use of albutoin indicated that the drug was more effective in tonic-clonic seizures than in absence seizures. Albutoin was marketed in Europe as CO-ORD and Euprax by Baxter Laboratories. Albutoin was not approved by the United States Food and Drug Administration.

Lesopitron is a non-benzodiazepine anxiolytic with pre- and post-synaptic 5-HT1A agonist activity. Its structure is similar to that of buspirone. Lesopitron has negligible effects on alpha-adrenergic and dopaminergic receptors [162653], and was more potent than structurally-related 5-HT1A agonists in rat social interaction and marmoset anxiety models. It also countered benzodiazepine withdrawal-induced anxiety in rodents. The acute toxicity of lesopitron is low and it does not potentiate the effects of alcohol or barbiturates. Long-term usage led to reductions in plasma glucose, triglycerides, phospholipids and cholesterol. The most common adverse events associated with lesopitron were somnolence, headache, pharyngitis, and dyspepsia.

Tefludazine (Lu 18-012) is a mixed D2 and 5-HT2 receptor antagonist that was developed as a potential antipsychotic compound. It was shown that tefludazine induced a dose-dependent decrease in both nigra pars compacta (SNC) and ventral tegmental area (VTA) dopamine (DA) activity. The development of the drug was discontinued in Phase I due to toxicological findings in dogs.

Clothixamide is a dopamine antagonist. The compound was invented by Pfizer in the 1960s and is claimed to be useful for the chemotherapy of mental diseases and especially for the control of excited states. Also, clothixamide is claimed to have potent antiemetic properties.

Climazolam is a benzodiazepine derivative, developed by Hoffman-LaRoche. It was used in veterinary for anesthetizing animals.

Dopamantine is the adamantine derivative. It combined elements of both amantadine and dopamine in its structure, shares some pharmacological effects of amantadine. Dopamantine is the anti-Parkinson drug, which has passed clinical trials. Dopamantine showed a high activity against Plasmodium berghei parasites that cause malaria.

Mepiprazole is a psychotropic pyrazole derivative. Mepiprazole is a serotonin reuptake inhibitor and adrenolytic. In clinical studies, it demonstrated anxiolytic properties.