Talaglumetad (also known as LY-544344) is a bicyclohexane derivative patented by Eli Lilly and Company as modulators of metabotropic glutamate receptor. Talaglumetad acts as a prodrug of Eglumegad, a selective agonist of metabotropic glutamate receptors (mGluR2/3) and metabolized to release active compound by both human jejunal homogenates and rat liver homogenates. In experiments on mice, Talaglumetad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment.

Ciclotizolam is triazolothienodiazepines derivative useful as anticonvulsants, muscle relaxants, anxiolytics, anti-tension agents, and appetite stimulators for mammals.

Enpiprazole is a heterocyclic three-ringed pyrazolylalkyl piperazine derivative. Enpiprazole has a cataleptic action very similar to that of neuroleptics, and its effect on muscle relaxation is comparable with that of diazepam. Enpiprazole exerts anxiolytic properties in animals.

Carperone is a fluorobutyrophenone compound which in animal studies has showed calming or tranquilizing effects resembling those of haloperidol, trifluperidol, and other antipsychotic drugs

Revospirone (BAY VQ 7813) is a pyrimidinylpiperazine derivative that acts as partial agonist at 5-HT1A receptors. Head shakes were reported after administration of revospirone in pigs, and once daily administration for 3-5 days led to a reduction in this head shake response. No behavioral alterations were observed. This compound was never marketed

Nonaperone, a butyrophenone, is a neuroleptic agent. It is antipsychotic in schizophrenics at doses which do not elicit extrapyridal side effects.

Tracazolate (ICI 136,753), a pyrazolopyridine, is a non-benzodiazepine with anxiolytic-like activity in animal models. It is known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. Its intrinsic efficacy, potentiation, or inhibition is determined by the nature of the third subunit (gamma1-3, delta, or epsilon) within the GABA(A) receptor complex.

Primaperone is substituted amino ketone patented by Science-Union et Cie.-Societe Francaise de Recherche Medicale as hypotensive and tranquilizing agents. Primaperone acts as serotonin receptor antagonis and demonstrate activity in behavioral despair test

Diazepinomicin is a structurally novel farnesylated dibenzodiazepinone discovered through DECIPHER technology, Thallion's proprietary drug discovery platform. A small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types, inducing cell cycle arrest and apoptosis in PBR-expressing cells. The compound was shown to have a broad cytotoxic activity in the low micromolar range, when tested in the NCI 60 cell line panel. Diazepinomicin can cross the blood-brain barrier. Diazepinomicin is in phase II clinical trials for the treatment of Telomeric 22q13 Monosomy Syndrome and phase I for the treatment of Fragile X syndrome.

Isoindoline pazinaclone (also known as DN-2327), a partial agonist at GABAA benzodiazepine receptors, produced anxiolytic, taming and anti-convulsive effects. This neuropsychiatric drug was involved in phase II clinical trial for patients with generalized anxiety disorder. However, this study was discontinued.