Zotepine is a potent antipsychotic and antidepressive drug, which was developed in Japan and used in many countries for the treatment of schizophrenia. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity.The drug is still available in Asia.

Sultopride (trade names Barnetil, Barnotil, Topral) is an atypical antipsychotic of the benzamide chemical class used in Europe, Japan, and Hong Kong for the treatment of schizophrenia. It was launched by Sanofi-Aventis in 1976. Sultopride acts as a selective D2 and D3 receptor antagonist. It has also been shown to have clinically relevant affinity for the GHB receptor as well, a property it shares in common with amisulpride and sulpiride.

Remoxipride is a substituted benzamide. It is a weak, but relatively selective, central dopamine D2-receptor antagonist and appears to have preferential affinity for extrastriatal dopamine D2-receptors. It also has marked affinity for central sigma receptors. It was introduced by Astra (Roxiam) at the end of the eighties and was prescribed as an atypical antipsychotic. Remoxipride was withdrawn from the market worldwide by Astra because of several cases of aplastic anaemia associated with the drug.

Anisopirol is a neuroleptic and was used as antipsychotic drug. Anisopirol, the alcohol resulting from reduction of the carbonyl group of fluanisone, is an exception and is in fact about two times more potent than fluanisone itself. Anisopirol is poorly absorbed by the oral route. Dopamine receptor is known pharmacological target of anisopirol and NMDA receptor is predicted target.

Docarpamine (marketed under the tradename Tanadopa) is a dopamine prodrug developed in Japan for the treatment of chronic heart failure. The drug does not cross the blood-brain barrier and shows no effect on CNS activity. It is supposed that the drug exerts its action by activating dopamine receptor D1.

Metopimazine, a phenothiazine derivative, is a dopamine D2 receptor antagonist. It exerts its antiemetic effects via the chemoreceptor trigger zone. Metopimazine showed potent alpha-adrenergic blocking activity, showed histamine H1 antagonism, and induced palpebral ptosis. Metopimazine can occasionally be associated with orthostatic hypotension, which probably relates to its affinity for the α1-adrenoceptor. Therapeutic doses of metopimazine are likely to produce sedation and side-effects related to autonomic blockade. Metopimazine (Vogalene®) is indicated for the prevention and treatment of nausea and vomiting.

Phenothiazine, the parent compound of a multitude of present-day drugs, has been employed on an extensive scale for its insecticidal, fungicidal, antibacterial and anthelmintic properties. Phenothiazine was formerly used as an insecticide and as a drug to treat infections with parasitic worms (antihelminthic) in livestock and people. It was introduced as antihelminthic in livestock in 1940 and is considered, with thiabendazole, to be the first modern antihelminthic. Almost a catholicon, its widespread use in animals and man has led to the uncovering of many adverse reactions encompassing effects on blood elements, neuromuscular problems and photosensitization. Its potential side effects have now limited its use. The chemical structure of phenothiazine provides a most valuable molecular template for the development of agents able to interact with a wide variety of biological processes. Synthetic phenothiazines (with aliphatic, methylpiperazine, piperazine-ethanol, piperazine-ethyl, or piperidine side-chain) and/or phenothiazine-derived agents e.g., thioxanthenes, benzepines, imonostilbenes, tricyclic antidepressants, dimetothiazine, and cyproheptadine have been effective in the treatment of a number of medical conditions with widely different etiology. These include various currently clinically used drugs for their significant antihistamic, antipsychotic, anticholinergic (antiparkinson), antipruritic, and/or antiemetic properties.

Periciazine (INN), also known as pericyazine (BAN) or Propericiazine, is a drug that belongs to the phenothiazine class of typical antipsychotics. Pericyazine is not approved for sale in the United States. It is commonly sold in Canada and Russia under the tradename Neuleptil and in the United Kingdom and Australia under the tradename Neulactil. The primary uses of pericyazine include the short-term treatment of severe anxiety or tension and in the maintenance treatment of psychotic disorders such as schizophrenia. There is insufficient evidence to determine whether periciazine is more or less effective than other antipsychotics. Pericyazine is a rather sedating and anticholinergic antipsychotic, and despite being classed with the typical antipsychotics, its risk of extrapyramidal side effects is comparatively low. It has a relatively high risk of causing hyperprolactinemia and a moderate risk of causing weight gain and orthostatic hypotension.

Fluspirilene, a neuroleptic drug, which is used clinically to treat schizophrenic patients, by blocking of dopamine receptors, especially the dopamine D2 receptors. Fluspirilene also displays calcium channel-blocking activity; it inhibits glutamate release primarily by reducing presynaptic Ca2+ influx via N-type Ca2+ channels that also may contribute to the antischizophrenic action of the drug. Recently in the frame of a project of drugs repositioning, fluspirilene was studied as an anti-cancer drug. It was found, that fluspirilene demonstrates a significant inhibitory effect on the proliferation and invasion of glioma cells. Thus, it can be a promising drug for the treatment of glioblastoma. In addition, fluspirilene, as a potential cyclin-dependent kinase 2 inhibitor, was investigated in animal models for the treatment of human hepatocellular carcinoma. Taken into account that fluspirilene has a long history of safe human use, the drug can be applicable in clinical therapy for cancer’s disease immediately.

Opipramol (Insidon, Pramolan, Ensidon, Oprimol) is an antidepressant and anxiolytic used in Germany and other European countries. Although it is a member of the tricyclic antidepressants, opipramol's primary mechanism of action is much different in comparison, it doesn’t represent a tricyclic antidepressant drug as it does not inhibit the neuronal uptake of norepinephrine and/or serotonin. Opipramol also acts as a low to moderate affinity antagonist for the D2, 5-HT2, H1, H2, and muscarinic acetylcholine receptors. H1 and H2 receptor antagonism account for its antihistamine effects, and muscarinic acetylcholine receptor antagonism is responsible for its anticholinergic properties. Opipramol was developed by Schindler and Blattner in 1961. Opipramol is typically used in the treatment of generalized anxiety disorder (GAD) and somatoform disorders. Its anxiolysis becomes prominent after only one to two weeks of chronic administration. Upon first commencing treatment, opipramol is rather sedating in nature due to its antihistamine properties, but this effect becomes less prominent with time. The therapy with Opipramol indicates an additional therapy with neuroleptics, hypnotics and tranquilizers (e.g. Barbiturates, Benzodiazepines). Therefore, it should be noted that some specific reactions, particularly CNS depressant effects could be intensified and an intensification of common side effects may occur. If necessary the dosage may be reduced. Co-administration with alcohol can cause stupor. MAO Inhibitors should be discontinued at least 14 days before the treatment with Opipramol. Concomitant use of Opipramol with β-blockers, antiarrhythmics (of class 1c), as well as drugs from tricyclic antidepressant group and preparations which influence the microsomal enzyme system, can lead to change in plasma concentration of these drugs. Co-administration of neuroleptics (example- haloperidol, risperidone) can increase the plasma concentration.