Niaprazine is a potent and selective antagonist of 5-HT2A and alpha-1 adrenergic receptors. It was used for the treatment of sleep disturbances in children and was investigated for the treatment of sleep disorders in patients with attention-deficit hyperactivity disorder and autistic disorder.

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.

Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Changes in sleep with camazepam were minimal. However, non-anxious subjects reported being more relaxed the next day. Camazepam may cause skin disorders.

Apronalide is an acyclic analog of barbiturates. It was used under tradename "Sedormid" as a sedative an hypnotic agent. In 1934 it was discovered that the drug causes thrombocytopenic purpura. Apronalide is still marketed in Japan, where it is used in combination with caffeine and ibuprofen for the treatment of headache.

Veralipride (trade name Agreal, Agradil) is a benzamide neuroleptic medicine indicated in the treatment of vasomotor symptoms associated with the menopause when a contraindication or non-acceptance of hormone therapy (HT) exists. Veralipride is a dopaminergic antagonist of receptor D2, that induces prolactin secretion without any estrogenic or progestagenic effects. Veralipride is well absorbed when administered orally, achieving maximal concentrations at 2.5 hours. It is poorly metabolized and is eliminated in the urine and feces. After oral administration, the half-life is 4 hours, and 44% is excreted without any changes in urine in the first 120 hours. Most of the studies agree that the decrease of vasomotor symptoms associated with the menopause (hot flushes) with veralipride use is from 48.0% to 89.9% depending on the time of use and method of administration. One of the main secondary effects of veralipride use is hyperprolactinemia, which may or may not be accompanied by galactorrhea, and can disappear at 48 hours of treatment withdrawal. The most serious effects that have been reported with veralipride use are those extrapyramidal, such as acute dyskinesia, tardive dyskinesia, Parkinsonism, postural tremor, myoclonia, and dystonia. Many of these have been related to over-dosage and due to the lack of prescription instruction follow-up. The presentation of secondary adverse events is decreased using this medicament at a dose no greater than 100 mg/day, for short time spans, and leaving drug-free intervals between schedules. Veralipride has never gained approval in the United States. On July 2007, the EMA recommended the withdrawal of marketing authorizations for veralipride. The still in use Mexican Official Norm for the prevention and control of perimenopausal and postmenopausal diseases in women establishes that the drug can be useful in the control of vasomotor symptoms.

Dixyrazine is a typical antipsychotic of the phenothiazine group. Under a trademark Esucos, the drug was used in European countries as an antipsychotic, antiemetic and sedative with oral doses ranging from 20 to 75 mg daily. Dixyrazine has also been given by injection.

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.

Valnoctamide is a valproic acid derivative associated with a decreased risk for congenital abnormalities and developed by Beersheva Mental Health Center for treatment mania. Valnoctamide has been marketed as an anxiolytic and sedative in several European countries (as Nirvanil), including Italy, Holland, and Switzerland, until the year 2000 but was not actively promoted as an anticonvulsant. It was marketed in the U.S. as Axiquel by McNeil Laboratories in the 1970s. In mice, valnoctamide has been shown to be distinctly less teratogenic than valproic acid. Injection of 3 mkmol ⁄ kg at day 8 of gestation produced only 1% exencephaly (as compared to 0–1% in control mice and 53% in valproate-treated mice). Embryolethality rates showed similar results: 52% with valproate versus 5% in the controls and 2% with valnoctamide. Valnoctamide's patent is expired, and it is not the property of any major pharmaceutical company. Valnoctamide has potential as a therapy in epilepsy including status epilepticus (SE) and neuropathic pain and is currently being developed for the treatment of mania and Schizoaffective Disorder. In clinical trials, Valnoctamide was well tolerated but lacked efficacy in the treatment of symptoms in patients with acute mania.

Chlorhexadol (or Chloralodol), a hypnotic compound which is included in the list of Schedule III drugs of the United States Controlled Substances Act.

Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.