Cidoxepin is the cis-isomer of the widely prescribed tricyclic compound doxepin. Commercial preparations of the tricyclic anti-depressant doxepin contain 15% of the more active cis-doxepin and 85% of the trans-isomer. Elorac, Inc., a rapidly growing specialty pharmaceutical company focused on the treatment of dermatological disorders, is pleased to announce that it has acquired worldwide rights to the active agent Cidoxepin from Gideon Pharmaceuticals. Cidoxepin appears to be much more potent than doxepin while having less sedative and cholinergic side effects. Elorac plans to develop oral formulations of the drug to treat urticaria and topical formulations for treatment of atopic and contact dermatitis.

Verucerfont (formerly GSK561679), a corticotropin releasing factor (CRF) receptor 1 antagonist, is being developed by GlaxoSmithKline under the license from Neurocrine Biosciences, for the treatment of post-traumatic stress disorder and congenital adrenal hyperplasia (CAH). Verucerfont is a potent, selective CRF1 receptor antagonist (IC50 for CRF1, CRF2, and CRF-BP ~ 6.1, >1000 and >1000 nM, respectively), and is orally available and brain penetrant. Verucerfont is in phase II clinical trials for the treatment of post-traumatic stress disorder or alcoholism. The compound was also in trials for the treatment of classic congenital adrenal hyperplasia (CAH). However, this research has been discontinued. In 2015, orphan drug designation was received in U.S. for the indication.

FEPITRIZOL is a hypnotic agent.

Amphetaminil is chemically an alpha-phenyl-alpha-[(1-methyl-2-phenyl)-ethylamino]-acetonitrile (1), i.e. a derivative of alpha-aminonitrile. It was was developed in the 1970s in Germany and marketed under the brand name Aponeuron. Administration of Aponeuron proved useful in the treatment of children with hyperkinetic syndrome. The subtle and crude motorics improved, symptoms of hyperactivity disappeared and the general school performance of the child improved. Aponeuron was also used in the treatment of disorders of erectile potency, chronic schizophrenia and narcolepsy. In 1974 amphetaminil was included in the class of addictives or habit-forming drugs, although prescription of the drug is not requiring adherence to strict requirements. Nevertheless, it has largely been withdrawn from clinical use.

Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.

Endixaprine (SR 41378 or 3-(4-hydroxy-1-piperidinyl)-6-(2,4-dichlorophenyl)-pyridazine) is a aminopyridazine derivative. Endixaprine is a nonbenzodiazepine compound with a pharmacological profile similar to barbiturates and benzodiazepines. It possesses anticonflict, anticonvulsant, antianxiety and hypnotic activities in rodents.

Lisofylline [1-(5R-hydroxyhexyl)-3,7-dimethylxanthine] is a unique metabolite of pentoxifylline. Lisofylline inhibited the generation of phosphatidic acid and free fatty acids. Lisofylline blocked the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline regulates immune cell function and autoimmune response by inhibition of IL-12 signalling and cytokine production. Lisofylline may have therapeutic value in the prevention of autoimmune disorders, including Type 1 diabetes, autoimmune recurrence following islet transplantation, and in preservation of beta cell functional mass during islet isolation.

Mesocarb (sydnocarb or 3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychomotor stimulant N-alkylated amphetamine derivative. Mesocarb is a selective inhibitor of dopamine uptake, it potently blocks dopamine transporter. It is very likely that mesocarb is being used by drug addicts. Mesocarb is included in the World Anti-Doping Agency’s list of substances and methods that are prohibited in sports. It is used in Russia for the treatment of a variety of neuropsychiatric comorbidities.

Fenaperone exerts tranquilizing and neuroleptic properties.

Mezilamine is a dopamine antagonist, it blocks presynaptic but stimulates postsynaptic alpha-adrenoceptors. Potential antipsychotic drug.