2-Carboxy-2-Phenylethyl 1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1h-Indole-3-Acetate (Tropesin, VUFB-12018) is indometacin prodrug with potent anti-inflammatory efficacy and advantageous therapeutic properties. In experiments in vivo in rats, after oral administration of a Tropesin dose of 50 mg/kg, esterolysis was observed between 2-3, with a peak level of liberated indometacin between 10-13 h after ingestion. Tropesin was administered orally to rats and dogs in the daily therapeutic dose, triple the dose and ten times the dose for 3 months. After the highest dosage, in isolated cases, some dogs were found to have superficial erosions of the gastric mucosa and dystrophic lesions of renal tubules without biochemical correlations. Indometacin, administered in parallel doses, caused severe lesions of the gastrointestinal tract with melaena and subsequent anemia, as well as severe degenerative changes in renal tubules, in all dosage groups. From the toxicological aspect, Tropesin is substantially more acceptable than indomethacin. The anti-inflammatory and anti-arthritic activities of Tropesin in comparison with indomethacin, were studied in various models of both acute and chronic inflammatory reactions. Both compounds exhibited significant therapeutic activities without substantial quantitative differences.

AMD8664 (1-pyridin-2-yl-N-[4-(1,4,7-triazacyclotetradecan-4- ylmethyl)benzyl]methanamine) is an antagonist of CXCR4 receptor. It has therapeutic potential in the treatment of HIV. AMD8664 is an effective suppressor of choroidal neovascularization.

N-Ethyl-3-piperidyl benzilate (JB-318) is an anticholinergic drug. It is a potent hallucinogenic agent. JB-318 is a psychotomimetic, it has an antitremor action in patients with Parkinson disease.

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.