Trifluperidol is an antipsychotic butyrophenone derivative. It is a high-affinity sigma receptor blocker and it was strongly selective for NR1a/2B receptors. It exhibit pharmacological effects and a mechanism of action very similar to that of phenothiazines and thioxanthenes in that it blocks dopaminergic receptors. It is more selective with respect to D2 receptors. Trifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. Trifluperidol has been suspected as a cause of cataract in Japan. Patients receiving trifluperidol treatment may develop a parkinsonian-like syndrome which responds to withdrawal of the drug or concurrent administration of an anti-parkinsonian drug. Acute dystonias and akathisia are other acute extrapyramidal effects; tardive dyskinesia may supervene after longer periods of treatment.

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.

Setiptiline Maleate is a tetracyclic antidepressant that has been used in the treatment of depression. It has antihistamine and hypnotic–sedative effects, but almost no anticholinergic effects. It is a weak inhibitor of norepinephrine reuptake in vitro and strongly stimulates the release of central norepinephrine by blocking presynaptic α2-adrenoceptors similar to mianserin. It also acts as a 5-HT2A, 5-HT2C, and 5-HT3 receptor antagonist. Unlike most conventional antidepressants, it has no efficacy as a serotonin reuptake inhibitor. It can induce drowsiness and thirst, but it displays low toxicity. Setiptiline Maleate was launched in 1989 for the treatment of depression in Japan.

Oxypertine (Equipertine, Forit, Integrin, Lanturil, Lotawin, Opertil) is a neuroleptic drug and was originally introduced as a treatment for schizophrenia in the 1960s. Oxypertine is an indole derivative with general properties similar to those of the phenothiazine, chlorpromazine. It has been given by mouth in the treatment of various psychoses including schizophrenia, mania, and disturbed behaviour, and of severe anxiety. Like reserpine and tetrabenazine, oxypertine depletes catecholamines, though not serotonin, possibly underlying its neuroleptic efficacy. The molecular structure is strongly similar to solypertine and milipertine.

Chlorpromazine pamoate (also known as chlorpromazine embonate) is a salt of pamoic acid and a chlorpromazine. Pamoate salts are used in pharmaceutical formulations because they show slow dissolution and are useful in formulations where extended duration of action is required. Chlorpromazine is a phenothiazine antipsychotic. It also exerts sedative and antiemetic activity. The precise mechanism whereby the therapeutic effects of chlorpromazine are produced is not known. It has a wide range of activity arising from its depressant actions on the CNS and its alpha-adrenergic blocking and antimuscarinic activities. Chlorpromazine is a dopamine inhibitor; the turnover of dopamine in the brain is also increased. There is some evidence that the antagonism of central dopaminergic function, especially at the D2-dopaminergic receptor, is related to therapeutic effect in psychotic conditions.

Sulpiride is an atypical antipsychotic drug (although some texts have referred to it as a typical antipsychotic) of the benzamide class used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Europe, Russia and Japan. Sulpiride is a selective antagonist at dopamine D2 and D3 receptors. This action dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine receptors accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Racemic and L-sulpiride significantly decreased stimulated serum gastrin concentration, but they did not affect fasting serum gastrin or basal and stimulated gastric acidity. D-sulpiride significantly decreased gastric acid secretion, without affecting serum gastrin levels.

Bromperidol (marketed as Bromidol, Bromodol) is a butyrophenone derivative. It is a potent and long-acting neuroleptic, used as an antipsychotic in the treatment of schizophrenia. It was discovered at Janssen Pharmaceutica in 1966. Bromperidol is a bromine analog of Haloperidol hydrochloride (sc-203593) which functions as a D2DR (dopamine D2 receptor) antagonist. Studies suggest that cytochrome CYP3A4 catalyzes the dehydration of Bromperidol and N-dealkylation of Bromperidol. In addition, CYP3A4 can oxidize N-dealkylated Bromperidol back into Bromperidol. Alternately, Bromperidol antagonizes the Neuroendocrine DA receptors which regulate hypothalamic LH-RH release.

Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor with antiemetic, anxiolytic and nootropic effects in animal models. Zacopride also has pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Zacopride has been tested in clinical trials for the treatment of schizophrenia but was found unsuccessful.

Sodium anthranilate is an excipient (pharmacologically inactive substance). Sodium anthranilate (Aminobenzoate sodium ,C7H6NNaO2), also known as sodium 2-aminobenzoate, is an organic amine. Aminobenzoate sodium exists as a yellow powder for use in pharmaceutical processing.

Penfluridol is a highly potent; first generation diphenylbutylpiperidine antipsychotic was developed by Janssen Pharmaceutica in 1968 and is used to treat schizophrenial and similar psychotic disorders. It is, however, like most typical antipsychotics, being increasingly replaced by the atypical antipsychotics. This drug is long-acting dopamine receptor blocker.