Cyprazepam is a benzodiazepine tranquilizer, developed by Warner-Lambert Pharmaceutical Company in the 1960s. The combination of cyprazepam with pentaerythrityl tetranitrate was found advantageous for the treatment of angina pectoris.

Reclazepam is a benzodiazepine derivative. Benzodiazepines are primarily used to treat anxiety.

Moxiraprine (also known as CM-30366) is aminopyridazine derivative with antidepressant activity. In preclinical studies Moxiraprine induced stereotyped behaviour and antagonized haloperidol-induced catalepsy in rats, after parenteral and oral administration. In 6-hydroxy dopamine (6-OHDA)-lesioned mice, Moxiraprine induced contralateral rotations and, when injected before 6-OHDA, protected mice against its neurotoxicity. Moxiraprine also provoked contralateral rotations when injected directly into the mouse right striatum. After parenteral injection, Moxiraprine slightly increased motility in mice, at least at low doses. The stereotypies and rotations (after intrastriatal injection) induced by Moxiraprine were antagonized by haloperidol, alpha-methyl-p-tyrosine and reserpine. The effects of Moxiraprine were compared to those of direct and indirect dopamine-like drugs. Bromocriptine induced a behavioural profile, which in most aspects, was qualitatively and quantitatively similar to that of Moxiraprine. Apomorphine was found slightly more potent than Moxiraprine, but in contrast to the latter, apomorphine-induced stereotypies were insensitive to alpha-methyl-p-tyrosine or reserpine. (+)-Amphetamine and nomifensine were less potent than Moxiraprine, and unlike Moxiraprine, induced ipsilateral rotations in 6-OHDA-lesioned mice.

Enilospirone (CERM-3726) is essentially a central stimulant. At low doses (100 mg) it may improve performance and at higher doses it may lead to disturbance of sleep continuity. These effects may not involve DA mechanisms, though changes such as those in REM sleep with chronic ingestion could involve the noradrenergic pathway. The property of the drug, even at low doses, to oppose the deterioration in performance associated with tests of prolonged duration is likely to be due to a mild alerting effect.

Metostilenol was developed as an antidepressant. However, it has never been marketed.

Roxoperone was developed as an anxiolytic agent. Information about the further development of this compound is not available.

Ramciclane is a bicycloheptyloxyethanamine derivative that acts with sedative activity.

Razobazam (Hoe 175) is a benzodiazepine derivative. Benzodiazepines are mainly used for treatment of anxiety. Razobazam improves learning performance in socially deprived rats. A 13% increase in neuronal density in the frontal cortex (associated with complex cognitive functions) of rats treated with razobazam was observed, but no changes in the amygdala (involved in emotion and memory functions). In mice, razobazam also affects retention performance through influences on memory storage and retrieval.

Radequinil (also known as AC-3933 ) is a oxadiazolylnaphthyridinone derivative patented by Dainippon Pharmaceutical Co., Ltd. as an inverse agonist of benzodiazepine receptors useful for the treatment of cognitive disorders including Alzheimer's disease. In preclinical trials, Radequinil enhances acetylcholine release in the rat hippocampus and ameliorates scopolamine-induced memory impairment and age-related cognitive decline in both rats and mice. Unlike the acetylcholinesterase inhibitor donepezil and the benzodiazepine receptor inverse agonist FG-7142, oral administration of Radequinil significantly ameliorated MK-801-induced memory impairment in the Y-maze test and in the object location test. Interestingly, the procognitive effects of Radequinil on MK-801-induced memory impairment were not affected by the benzodiazepine receptor antagonist flumazenil, although this was not the case for the beneficial effects of Radequinil on scopolamine-induced memory deficit. Moreover, the onset of Radequinil ameliorating effect on scopolamine- or MK-801-induced memory impairment was different in the Y-maze test. Unfortunately, in clinical trials, Radequinil failed to demonstrate efficacy and further development was discontinued.

Pirenperone, a quinazoline derivative, is a selective antagonist at serotonin receptor 2A binding sites. The liposoluble compound pirenperone has been studied in a variety of behavioral tests including the sensitive d-lysergic acid diethylamide (LSD) cue discrimination assay, in which it served as a potent LSD-antagonist. Pirenperone also proved to be an effective antagonist of serotonin-mediated behavioral responses including the head twitch response thought to be mediated by serotonin receptors.