ITRIGLUMIDE, an anthranilic acid derivative, is a cholecystokinin B receptor antagonist.

Meturedepa (also known as AB-132), an alkylating agent that was developed as an antineoplastic drug. Meturedepa was studied to treat lymphomas and leukemias. The drug also participated in the Eastern clinical drug evaluation program for 233 patients with advanced cancer. Information about the current use of this compound is not available.

Coluracetam (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.

Dazepinil (HRP 543) is a 1,3-benzodiazepine antidepressant, developed by Hoerscht in the early 1980s. In mouse tests, dazepinil inhibited tetrabenazine-induced ptosis and potentiated yohimbine toxicity. In vitro, dazepinil inhibited norepinephrine and serotonin uptake into rat brain synaptosomes and lacked anticholinergic activity.

Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.

Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.

Evenamide (NW-3509) is a blocker of voltage-gated sodium channels. Evenamide modulates sustained repetitive firing, without inducing impairment of normal neuronal excitability. It normalizes glutamate release induced by aberrant sodium channel activity. The potential benefits of the compound have been demonstrated in numerous preclinical models predictive of efficacy in psychiatric diseases, including models of psychosis such as amphetamine-induced hyperactivity, sensorimotor gating and information processing deficits (pre-pulse inhibition impairment induced by different stimuli), mania and depression. Evenamide is being evaluated in a Phase II trial as add-on treatment to 5HT2/D2 blocking antipsychotics in schizophrenic patients.

Dicarbine is an orally active drug approved in Russia under the trade name Карбидин, is used for the treatment patients with schizophrenia and alcoholic psychosis. This drug blocks dopamine receptors in various brain parts, which leads to a reduction in the productive symptoms of psychosis: delusions and hallucinations.

Nonabine is a chromenol structurally related to the cannabinoids which has shown antiemetic efficacy in clinical trials. Nonabine also produced sedative clinical effects, but with an EEG profile which resembled that reportedly caused by cannabinoids. In contrast to cannabinoids, nonabine did not cause changes of mood or perception, suggesting that nonabine lacks the potential for social abuse at antiemetic doses. Nonabine was studied in the 1980s for the prevention of nausea and vomiting associated with cancer chemotherapy.