Valrocemide is an anticonvulsant agent which was under development by Teva and Acorda as a potential therapeutic for the treatment of epilepsy. Valrocemide is an N-valproyl derivative of GABAand glycine. It was found that 1 mM of valrocemide could drastically inhibit human brain crude homogenate MIP synthase activity. Furthermore, the mechanism of the effect of valrocemide was studied and results showed that valrocemide reduced the enzyme activity by an apparent competitive mode of inhibition. In October 2003, a phase II trial using valrocemide as an adjunct therapy in refractory epilepsy patients had been completed and phase III trials were being planned. Valrocemide was also being investigated for potential utility in the treatment of bipolar disorder and neuropathic pain. This compound was originally discovered by Yissum Research and Development Company of the Hebrew University of Jerusalem, then licensed and developed by Teva in collaboration with Acorda in 2003, then licensed to Shire the worldwide development, production and marketing rights in 2006. However, the development of Valrocemide was discontinued by Shire in 2009.

Piriqualone is the noncompetitive AMPA receptors antagonist. It was developed as an anticonvulsant, hypnotic and muscle relaxant agent.

Pitenodil is a vasodilator.

Posizolid (AZD2563 or AZD5847) is an oxazolidinone, identified from an antibiotic research programme which aimed to synthesise agents that inhibited all Gram-positive bacteria, including multiresistant strains likely to be encountered clinically. Oxazolidinones bind to the 50S ribosomal subunit and inhibit the initiation phase of translation. Posizolid had been in phase II clinical trials for the treatment of tuberculosis. However, this study was discontinued.

Prazitone (also known as AGN-511) is a barbiturate derivative patented by Aspro-Nicholas Ltd. as a non-sedating anxiolytic and antidepressant

Umespirone [KC 9172, KC 7218] is a serotonin 1A receptor agonist that was undergoing phase I clinical trials with Solvay in the Netherlands as a potential treatment for anxiety and psychotic disorders. Umespirone prevented the behavioural consequences of withdrawal from diazepam. Umespirone also had an anxiolytic profile of action in the tests of rat social interaction and in the marmoset exposed to a human threat. Umespirone reduced the hyperactivity induced by the infusion of dopamine into the nucleus accumbens of rat. In radioligand binding assays umespirone demonstrated nanomolar affinity for the alpha 1-adrenoceptor and the 5-HT1A and dopamine D2 receptors.

Turosteride [FCE 26073] is a selective 5α-reductase inhibitor being developed by Pharmacia Corporation. Turosteride inhibits human and rat prostatic 5 alpha-reductases with IC50 values of 55 and 53 nM, respectively. It was in phase II clinical trials in Italy for the treatment of benign prostatic hyperplasia.

Valofane is an atypical barbiturate. It is a tautomer (and prodrug) of proxibarbal Valofane is a neurotropic drug. It has sedative and hypnotic action.

Vedaclidine [LY 297802, NNC 101053, NNC 111053, butylthio[2.2.2]], a quinuclidine, is a muscarinic receptor agonist being developed by Novo Nordisk and Eli Lilly as an analgesic drug. Vedaclidine is a muscarinic receptor ligand which is equiefficacious to morphine in producing antinociception. In vitro, Vedaclidine had high affinity for muscarinic receptors in brain homogenates, but had substantially less or no affinity for several other neurotransmiter receptors and uptake sites. Its pharmacological profile suggests that it may have clinical utility in the management of pain as an alternative to opioids.

Vanyldisulfamide is an anti-infective sulfonamide drug.