Dicolinium is a quaternary ammonium derivative that is a ganglion blocking agent, formerly used as an antihypertensive.

D-Fagomine (1,2-dideoxynojirimycin) is a six-membered ring iminocyclitol that was first isolated from seeds of buckwheat (Fagopyrum sculentum Moench, Polygonaceae) and is also present in other plant sources such as mulberry (Morus Alba, Moraceae) leaves and gogi (Lycium chinense) roots. D-fagomine is present in common buckwheat-based foodstuffs in amounts ranging from 1 to 25 mg/kg or mg/L, it is stable during boiling, baking, frying and fermentation, and it is biosynthesised upon sprouting. The estimated total intake of D-fagomine resulting from a diet that includes such foodstuffs would be between 3 and 17 mg per day (mean for both genders; range from P5 to P95). In animal studies D-Fagomine lowers postprandial blood glucose. D-fagomine agglutinated Enterobacteriaceae (Escherichia coli, Salmonella enterica serovar Typhimurium), while it did not show this effect on Bifidobacterium spp. or Lactobacillus spp. D-fagomine significantly inhibited the adhesion of Enterobacteriaceae and promoted the adhesion of Lactobacillus acidophilus to intestinal mucosa. D-Fagomine did not show any effect on bacterial cell viability. D-fagomine may be used as a dietary ingredient or functional food component to reduce the health risks associated with an excessive intake of fast-digestible carbohydrates, or an excess of potentially pathogenic bacteria.

NS-2359, an orally active, triple monoamine reuptake inhibitor that inhibits the reuptake of dopamine, noradrenaline and serotonin, is being developed by Saniona and the Treatment Research Center (TRC) at the University of Pennsylvania for the treatment of Cocaine abuse. NS-2359’s pharmacological profile means that it may be able to reduce cocaine withdrawal symptoms, reduce cocaine craving and reduce cocaine-induced euphoria. Previously NS-2359 was in clinical trials for the treatment of attention-deficit hyperactivity disorder and major depressive disorder, but development was discontinued due to lack of effectiveness.

CYR-101 (MIN-101) is a cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively). MIN-101 also shows binding affinity for a1-adrenergic receptors but low or no affinity for muscarinic, cholinergic, and histaminergic receptors. MIN-101 demonstrated statistically significant efficacy in reducing negative symptoms and good tolerability in stable schizophrenia patients. The drug is in phase II clinical trials for the treatment of Schizophrenia.

[11C]-SCH-442416 was designed and synthesized by scientists at the University of Milano-Bicocca with the intent of development as a PET imaging probe. [11C]-SCH-442416 demonstrates a selective high affinity as an antagonist of the A2A Adenosine Receptor with a Ki of 0.48 nM. [11C]-SCH-442416 has demonstrated the ability to cross the blood-brain barrier and has been used as an imaging agent in a number of animals studies and at least one clinical trial in healthy human volunteers. It should be noted that the non-radio labeled form of SCH-442416 has been investigated in rats for the treatment of addictive behaviors.

Henatinib was developed as a multitargeted tyrosine kinase inhibitor with antitumor activities. Henatinib is an endothelial growth factor receptor type 2 (VEGFR2) antagonist. The drug participated in phase I clinical trial to evaluate the safety and tolerability in patients with advanced solid malignancies, however, the study was terminated. The current development status is unknown.

Buthionine sulfoximine (BSO) is a selective inhibitor of γ-glutamylcysteine synthetase (γ-GCS), the rate-limiting enzyme in glutathione (GSH) synthesis. In cancer cells, glutathione depletion significantly increased cytotoxicity via oxidative stress. In addition, in neuroblastoma cells susceptible to Buthionine sulfoximine treatment, DNA damage and cell apoptosis occurred via ROS production. Buthionine sulfoximine plus melphalan was effective in treatment for patients with recurrent/refractory neuroblastoma. Buthionine sulfoximine may also be used to increase the sensitivity of parasites to oxidative antiparasitic drugs. Buthionine sulfoximine has been shown to increase the efficacy of nifurtimox against T. cruzi and has also been shown to be an effective modulator of GSH-mediated chemoresistance by increasing the in vitro cytotoxicity of alkylating agents and radiation. Buthionine sulfoximine has been tested in animal studies and in human phase I trials for adults with solid tumors, with documented clinical responses in patients with melanoma, ovarian carcinoma and small cell carcinoma of the lung treated with the combination of Buthionine sulfoximine and melphalan.