Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.

Hexacyclonic Acid (aka gevilon) has been clinically demonstrated to produce hypolipidemic effects. It has been investigated as a treatment for coronary heart disease, and hypertensive disease with severe lipid metabolic disturbances. Gevilon has been found to have a hypolipidemic effect in reducing the levels of total cholesterol, beta-cholesterol, triglycerides, increasing alpha-cholesterol levels and normalizing the atherogenicity coefficient; especially in patients with Type IIb dyslipoproteinemia.

Tropapride is dopamine D2 receptor antagonist, which potential high antipsychotic activity has been clearly shown in biochemical and pharmacological tests.

Basimglurant is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties that are corroborated by its functional magnetic imaging profile as well as anxiolytic-like and antinociceptive features. In electroencephalography recordings, basimglurant shows wake-promoting effects followed by increased delta power during subsequent non-rapid eye movement sleep. Basimglurant has favorable drug-like properties, a differentiated molecular mechanism of action, and antidepressant-like features that suggest the possibility of also addressing important comorbidities of MDD including anxiety and pain as well as daytime sleepiness and apathy or lethargy. Basimglurant is being under development by Roche for the treatment of treatment-resistant depression (as an adjunct). It is in phase II clinical trials for this indication.

Valtrate is a principle compound isolated from Valeriana jatamansi Jones, which is a Traditional Chinese Medicine used to treat various mood disorders. Valtrate at a high dose has been found to have sedative properties by inhibiting spontaneous motion and increasing the sleeping number induced by pentobarbital sodium in mice. In rats valtrate exhibits anxiolytic-like profiles in the elevated plus maze test and the open field test. Valtrate attenuated HPA axis activity by reducing the corticosterone level. Valtrate also possesses anti-breast cancer activities via cell cycle arrest, apoptosis, and inhibition of cell migration, thus supporting valtrate as a potential antitumor agent.

Cintriamide is a tranquilizer. It possessed anxiolytic properties. 3,4,5-Trimethoxybenzaldehyde can be used as an intermediate in the synthesis of cintriamide.

Pagoclone is an anxiolytic agent from the cyclopyrrolone family, related to better-known drugs such as the sleeping medication zopiclone. It binds with the roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either a α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing a α3 subunit. Pagoclone produces anxiolytic effects with little sedative or amnestic actions at low doses.

Nerispirdine, an acetylcholine release enhancer and a K+/Na+ use-dependent channel blocker, was in clinical development with sanofi-aventis for the treatment of multiple sclerosis. Nerispirdine is not proconvulsant. It can inhibit axonal K(+) channels and this mechanism may underlie the ability of the drug to enhance neuronal conduction. Nerispirdine can also inhibit neuronal Na(+) channels, a mechanism that may explain why nerispirdine lacks proconvulsant activity.

Pridopidine is an experimental drug candidate belonging to a class of agents known as dopidines, which act as dopaminergic stabilizers in the central nervous system. As a dopamine stabilizer, pridopidine is thought to reduce the effects of dopamine when there’s too much and increase its effects when there’s too little. Pridopidine, therefore, plays two opposing roles in the brain, which stabilize dopamine levels. In this way, pridopidine is thought to help the brain reestablish a normal balance of neurotransmitters, and thus regain control over motion. Pridopidine intended to treat Huntington’s disease movement symptoms. Pridopidine was well tolerated and had an adverse event profile similar to a placebo.

Fluperlapine is dibenzazepine chemically and pharmacologically similar to clozapine. Fluperlapine had no cataleptogenic effect and did not inhibit the apomorphine- and d-amphetamine-induced stereotypes. Fluperlapine is fairly effective neuroleptic drug with a fast-acting antipsychotic affect. The effects in movement disorders imply that fluperlapine is less liable than traditional neuroleptics to induce acute extrapyramidal side effects and tardive dyskinesia and is particularly beneficial in the treatment of patients vulnerable to neurological side-effects. It was demonstrated efficacy in the treatment of a variety of medical conditions including schizophrenia, psychosis associated with Parkinson's disease and dystonia. It has the capacity for producing life-threatening agranulocytosis.