Pipramadol is an analgesic agent. Pipramadol exhibits not only antinociceptive but also central and peripheral antiserotonin properties.

Lorcinadol is an analgesic agent.

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.

Renanolone is a synthetic neuroactive C21 5β-H steroid. It was never used in a clinical setting. The thermogenic and inflammatory responses induced by renanolone were reported to be similar to responses induced generally by appropriate administration of neutral steroid pyrogens in humans.

Penirolol is a beta-adrenergic blocking agent that was studied as an antihypertensive agent. Information about the further development of this drug is not available.

Tolboxane is an alpha-adrenergic blocking drug. It is a product of arachidonic acid oxidation. Tolboxane is a tranquilizer. It influences atherosclerosis pathogenesis.

Vofopitant (previously known as GR205171), a tetrazole-derivative, was developed as a neurokinin1 receptor antagonist. Vofopitant was studied in clinical trials phase II for the treatment of primary insomnia and posttraumatic stress disorder. However, these studies were discontinued due to lack of effectiveness. In addition, vofopitant participated in phase I for patients with bipolar disorder. However, this study was terminated because of the slow recruitment; trial unlikely to reach completion.