PQ401 is a diaryl urea compound and a potent inhibitor of autophosphorylation of the IGF-1 receptor. It has been investigated in preclinical studies as a potential cancer treatment in a number of cell models; most notably for breast cancer. It was also studied in mouse models as a possible treatment of diabetic neuropathies, although it showed less promise here.

Epicatechin-5-Sulfate is a metabolite of epicatechin. It is patented for inclusion in food formulations intended for weight loss, and treatment of diabetes.

Destomycin A is an aminoglycoside antibiotic and is reported to have antibacterial and anthelmintic activity. It has an antibacterial effect on Gram-positive bacteria, Gram-negative bacteria, and fungi. The mode of action of destomycin A is the inhibition of polypeptide synthesis in cells of Escherichia coli and stimulation of adenylate cyclase in several animal tissues. Destomycin A is added to feed for pigs and chickens to prevent parasitic infection of Ascaris suum (the mechanism of action involves inhibition of vitelline coat formation of the parasite eggs.)

Polygodial is a sesquiterpene dialdehyde isolated from the leaves of certain peppers and related plants, that exhibits anti-inflammatory, antiallergic, antinociceptive, anticancer, antifungal and antimicrobial activities. Polygodial’s primary antifungal action is as a nonionic surfactant, disrupting the lipid-protein interface of integral proteins nonspecifically, denaturing their functional conformation. It is also likely that Polygodial permeates by passive diffusion across the plasma membrane, and once inside the cells may react with a variety of intracellular compounds. Polygodial is a component of the “hot taste” in peppery spices of traditional Japanese cuisine.

GBR-12935 (1-{2-benzhydryloxyethyl}-4-(3-phenylpropyl)piperazine) is a potent and selective inhibitor of dopamine transporter. Gist-Brocades originally initiated studies of GBR-12935 for the treatment of cocaine dependence. Tritium-labeled GBR-12935 may be used in radioligand binding studies. GBR-12935 is considered to be the metabolite of vanoxerine, another piperazine dopamine uptake inhibitor.

Songorine is a diterpenoid alkaloid which can be isolated from the genus Aconitum. Songorin has demonstrated anti-inflammatory, anti-anxiolytic and the ability to promote wound healing. The Anti-anxiolytic properties appear to be linked to the agonistic activity of the Dopamine D2 receptor as shown in rat hippocampal slices. The wound healing effect is the result of songorine's ability to stimulate the development of mesenchymal progenitor cells, although the exact mechanism of action remains unclear.

Corynanthine is one of the two diastereomers of yohimbine (the other is alpha-yohimbine). Corynanthine is an antagonist of the alpha-1, alpha-2A and alpha-2C adrenergic receptors showing greater selectivity for the alpha-1 adrenergic receptor. Corynanthine was tested as the active ingredient of eye drops in a small clinical trial for Ocular hypertension where formulations of 2% and 5% demonstrated relief of symptoms.

Magnesium adipate is a magnesium salt. It was reported that treatment with a preparation containing magnesium adipate and magnesium nicotinate (in tablet or ampule form for i.v. or i.m. administration) has been useful in the treatment of patients with coronary, cerebral and peripheral atherosclerosis.

SCH-23390 is a potent and selective antagonist of the dopamine-1 and dopamine-5 receptors (Ki = 0.2 and 0.3 nM respectively). It was found to prevent death from d-amphetamine overdose in rats and has also been investigated as a potential treatment for Parkinson's Disease and Bipolar Disorder. A single clinical trial was conducted in healthy humans where SCH-23390 induced akathisia (motor restlessness). Preclinical and clinical trials as therapeutic have been discontinued due to side-effects and lack of efficacy. However, it should be noted that a C11 radiolabeled version of the compound has been synthesized and used as a PET imaging probe for the study of Parkinson's Disease and Huntington's Disease.

BW 245C is a DP receptor agonist. Systemic administration of BW 245C to healthy volunteers lead to inhibition of platelet aggregation responses to ADP. BW245C was found to be effective in reducing human intraocular pressure, but its clinical usefulness as anti-glaucoma drugs is limited by the extraocular side effects.