Clorgiline is a monoamine oxidase (MAO) inhibitor. Specifically, it is an irreversible and selective inhibitor of MAO-A. Clorgiline was under investigation for antidepressant and anxiolytic potential but has never been marketed, likely due to efficacy concerns. It continues to see routine use as a molecular probe in biomedical research examining a number of neurological disease and cancer models. In addition to inhibiting the MAO-A receptor, it has also been found to bind to the sigma1 receptor, and with high affinity to the I2 imidazoline receptor.

Benzodepa is an aziridine alkylating agent that cross-links with DNA, causing inhibition of DNA synthesis. It has been studied as a potential treatment for a variety of cancers, most notably bronchiogenic carcinoma.

Temefos (Diphos, Temephos) is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage. Diphos has been used in trials studying the treatment of Plasmodium Falciparum Malaria. Temephos was first registered in the United States in 1965 by American Cyanamid Company for a number of uses including citrus fruits, pet collars, and mosquito control. A Registration Standard was issued in August, 1981. In response to EPA's 1991 Data Call-In, American Cyanamid dropped all uses except the mosquito larvicide use in non-potable waters and requested a low volume minor use waiver for relief from the data requirements associated with that use.

Kifunensine is an immunoactive compound originally produced by Kitasatosporia kifunense, which displays competitive inhibition against immunosuppressive factor in tumor-bearing mice. Kifunensine has also been shown to be a potent inhibitor of the purified glycoprotein processing enzyme, mannosidase I (MAN1), specifically MAN1A1, MAN1A2, MAN1B1 and MAN1C1. Kifunensine inhibits human endoplasmic reticulum α-1,2-mannosidase I and Golgi Class I mannosidases IA, IB and IC with Ki values of 130 and 23 nM, respectively. Enzymes of this class are important factors for the biosynthesis of various types of N-linked oligosaccharide structures. Inhibition of these structures by kifunensine can interfere with cell-to-cell adhesion, targeting of lysosomal hydrolases to lysosomes, and clearance of asialoglycoproteins from the serum. Kifunensine is used to suppress Endoplasmic Reticulum-Associated Degradation (ERAD) via the inhibition of endoplasmic reticulum-associated mannosidase activity. Kifunensine has shown potential for treatment of sarcoglycanopathies and lysosomal storage disorders. Orphan designation (EU/3/11/906) was granted by the European Commission to Généthon, France, for kifunensine for the treatment of beta sarcoglycanopathy, but it was withdrawn later. Kifunensine’s use as a therapeutic is currently being researched in several conditions that benefit from its ability to inhibit mannosidase I.

Allopurinol riboside is a metabolite of allopurinol, a xanthine oxidase inhibitor indicated for the management of patients with leukemia, lymphoma, and solid tumor malignancies who are receiving cancer therapy which causes elevations of serum and urinary uric acid levels and who cannot tolerate oral therapy. Allopurinol riboside is not an inhibitor of xanthine oxidase. Allopurinol riboside is commonly thought to be directly synthesized by purine nucleoside phosphorylase (PNP) in vivo. Allopurinol riboside competitively inhibits the action of PNP on inosine in vitro. Allopurinol riboside potently inhibits growth in vitro of promastigotes of Leishmania species. Patients with American cutaneous leishmaniasis who received allopurinol riboside had clinical improvement. In addition, allopurinol riboside demonstrated some effectivity against Trypanosoma cruzi infections in animals.

3-O-methyldopa (3-OMD) is a metabolite of L-3,4-dihydroxyphenylalanine (L-DOPA), a drug used for the treatment of Parkinson's disease patients. 3-OMD is formed by catechol-O-methyltransferase. 3-OMD may be responsible for the side effects of L-DOPA.

Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia

Sodium tauroglycocholate presents in ENZAR FORTE tablet, together with enzymes: amylase, lipase and protease. ENZAR FORTE is indicated for the treatment of the following digestive symptoms: indigestion/dyspepsia; flatulence; bloating; fullness after eating; heartburn; anorexia; hepatic and pancreatic insufficiency; post-operative digestive upsets and convalescence. Discomfort, flatulence, and abdominal colic may result when the bodies own pancreatic enzymes cannot cope with excessive quantities of food consumed. In such cases, the enzymes present in ENZAR FORTE enhance the digestive processes in a natural way, thereby reducing the amount of undigested food available for fermentation & putrefaction. Amylase enzyme helps in the digestion of starch, lipase is involved in the digestion of lipids, and protease is required for digestion of proteins. The advantage of bile salt i.e. sodium tauroglycocholate for improving absorption of fat & fat-soluble vitamins.

N-Methylspiperone (NMSP) is a derivate of spiperone and high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. In the biodistribution studies in rodents, there was a high accumulation of radioactivity in the liver, lung, and kidneys, whereas the brain radioactivity was not as high N-Methylspiperone is used to study the dopamine and serotonin neurotransmitter systems. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography (PET). [11C] N-Methylspiperone PET is useful for objective monitoring of D2and 5-HT2A receptor occupancy and density in patients being treated with antipsychotic drugs.

Mitragynine is the main active alkaloid constituent of the plant Mitragyna speciosa Korth. Mitragyna speciosa Korth. (M. speciosa), from the Rubiaceae family, is a tropical medicinal plant native to Southeast Asia. In Malaysia, M. speciosa leaves are known as Ketum or Biak, and in Thailand as Kratom. M. speciosa has been historically used in Southeast Asia as a stimulant drug and in its traditional context as a remedy for various symptoms. Pharmacological activities are mainly mediated via opioid receptors as well as neuronal Ca2+ channels, expression of cAMP and CREB protein and via descending monoaminergic system. Mitragynine acted as a partial agonist at mu-opioid receptors, in contrast, at kappa-opioid receptors, mitragynine was a competitive antagonist, similarly, mitragynine acted as an antagonist at delta-mu-opioid receptors, but with very low potency. Experimental studies in animals have now shown that mitragynine has an addictive potential, however, only at higher doses. Human users in countries of frequent use with a traditional context report a rather low daily consumption with only mild side effects. Kratom and mitragynine can be instrumentalized to enhance physical work power and endurance. A major reason for Kratom consumption is its reported efficacy to replace opiates in chronic users. This makes the Kratom plant preparation and also the isolated compound mitragynine interesting options to treat opiate addiction. In August 2016, the US Drug Enforcement Administration announced plans to classify kratom and its mitragynine constituents as Schedule 1 controlled substances.