Peratizole is tranquillizer and antihypertensive agent.

Fipamezole is a fluorine substituted imidazole compound with high antagonist specificity for the presynaptic alpha2-adrenoceptor. There were no significant differences between the affinity of Fipamezole for the different subtypes, thus characterizing Fipamezole as a non-subtype–selective alpha2 antagonist. Fipamezole had been in phase III clinical trials for the treatment of dyskinesia associated with Parkinson’s disease. Detected side effects are hypertension, nausea, vomiting, dysgeusia, facial flushing.

AV608, a 4-aminopiperidine derivative, is a selective, specific, long-acting, orally active and potent nonpeptidic antagonist of the NK-1 receptor. AV-608 had been in phase II clinical trials for the treatment of social phobia and overactive bladder (OAB). This compound was originally discovered by Novartis, and then licensed to Areva Pharmaceuticals in October 2003. Addition this drug was in phase I clinical trial for the treatment of Irritable Bowel Syndrome (IBS), this disease is characterized by chronic abdominal pain and frequent comorbid anxiety. The substance P ⁄ neurokinin-1 receptor system is implicated in the regulation of both pain and anxiety, suggesting a potential therapeutic target in IBS. However, the researches on this drug candidate were discontinued in 2010.

2-chloroethyl-3-sarcosinamide-1-nitrosourea (SarCNU) is an alkylating chloroethylnitrosourea with antineoplastic activity. It is a selective cytotoxin that enters cells via the extraneuronal transporter for monoamine transmitters (EMT). Both in vitro and in vivo studies demonstrated that SarCNU was more effective than BCNU against human gliomas. Selectively accumulating in some tumor cells, SarCNU forms covalent linkages with nucleophilic centers in DNA, causing depurination, base pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. SarCNU crosses the blood-brain-tumour-barrier and is taken orally. Phase II trial of SarCNU in malignant glioma revealed unexpected pulmonary toxicity. SarCNU was not FDA approved for orphan indication of malignant glioma.

LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM. Eli Lilly is developing LY 2608204 as an orally administered, once-daily therapy for type 2 diabetes. LY-2608204 is in phase I clinical trials for the treatment of type 2 diabetes.

Chlorpromazine Phenolphthalinate is Phenolphthalinate salt of psychotropic agent Chlorpromazine marketed as Wintermin by Japanese pharmaceutical company Shionogi Inc for treating certain mental or mood disorders. Chlorpromazine is a psychotropic agent indicated for the treatment of schizophrenia and other central nervous system disease

CEP-37440 is a potent ATP-competitive, highly kinase selective, and orally active inhibitor of FAK1 and anaplastic lymphoma kinase (ALK). In addition to a favorable metabolic stability and pharmacokinetic profile preclinically, CEP-37440 is also a brain penetrant. CEP-37440 was able to inhibit the proliferation of certain IBC cells by decreasing the levels of phospho-FAK1 (Tyr 397); none of the cells expressed ALK. Studies using IBC xenograft models showed that CEP-37440 also effectively reduces the growth of the primary tumor xenografts and inhibits the development of brain metastases in mice.

Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. Dihydrexidine was shown to stimulate cyclic AMP synthesis just as well or better than dopamine. It was the first dopamine D1 receptor agonist that had potent antiparkinsonian activity in a primate model of Parkinson's disease. Dihydrexidine produces hypothermia. Dihydrexidine has been shown to alleviate cognitive deficits or enhance cognitive performance in a number of animal models of cognition. It is under investigation for the improving the cognitive and working memory deficits in schizophrenia and schizotypal disorder.

PRX-03140 is a partial agonist of the 5-HT4 receptor that is being developed by EPIX Pharmaceuticals for Alzheimer's disease. In vitro shows potent binding to 5-HT4 receptor and increased cAMP production in human embryonic kidney-293 cells expressing recombinant rat 5-HT(4) receptors. In the clinical trial, PRX-03140 was associated with a statistically significant improvement in the Alzheimer’s Disease Assessment Scale.