Levamisole (the trade name Ergamisol), an anthelminthic drug with immunological properties. It also has antitumor activity when administered with 5-fluorouracil in patients with Duke's C colorectal carcinoma; however, this use was discontinued. The mechanism of the antitumor effect is unknown but has been postulated to be related to levamisole's immunomodulatory properties. Levamisole can stimulate antibody formation to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis, chemotaxis and increases motility, adherence, and chemotaxis. Levamisole inhibits alkaline phosphatase and possesses cholinergic activity. The mechanism of action of levamisole as an antiparasitic agent, for example, to treat ascariasis, relates to its agonistic activity to L-subtype nicotinic acetylcholine receptors in nematode muscles. In addition, levamisole was studied for preventing relapses of the steroid-sensitive idiopathic nephrotic syndrome (SSINS). It was shown, that alone or in combination with steroids, the drug can prolong the time to relapse and prevented recurrence during one year of treatment. However, these studies also were also discontinued.

Metacresol (m-cresol or 3-methylphenol) is colorless, yellowish liquid. It is used as a bactericide for control of crown gall and olive knot on certain fruit and nut trees and ornamentals and the genetic/physiological disorder burr knot on apples. Currently, one product is registered which contains both m-cresol and xylenol. Used as disinfectant/bacteriocide/germicide for animal pathogenic bacteria (G- and G+ vegetative) in households, sickrooms, hospitals, veterinary clinics, and veterinary hospitals; on surgical instruments, diagnostic instruments/equipment and on hospital critical rubber/plastic items. Used as an insecticide and miticide on dogs for treatment of lice and fleas. It is also used for making synthetic resins; in photographic developers, explosives. Additionally, m-cresol is chemical intermediate for thymol used in cough/cold medicinals, synthetic pyrethroid insecticides, 3-methyl-6-t-butylphenol, trinitro-m-cresol for explosives, and phenolic resins; disinfectant ingredient; ore flotation agent; solvent. m-Cresol, either pure or mixed with p-cresol, is important in the production of contact herbicides. m-Cresol is also a precursor to the pyrethroid insecticides. Furthermore, many flavor and fragrance compounds, such as (-)-methanol and musk ambrette, are derived from m-cresol. Several important antioxidants including synthetic vitamin E are produced from m-cresol. m-cresol is used as a topical dental antiseptic. m-cresol is an effective antimicrobial preservative and is used at low levels (0.3%) in multi-dose peptide and protein formulations. m-cresol has been shown to cause protein aggregation.

Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TCAs in that it does not appear to block serotonin reuptake. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder (depressive neurosis) and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression. The mechanism of action of maprotiline is not precisely known. It does not act primarily by stimulation of the central nervous system and is not a monoamine oxidase inhibitor. The postulated mechanism of maprotiline is that it acts primarily by potentiation of central adrenergic synapses by blocking reuptake of norepinephrine at nerve endings. This pharmacologic action is thought to be responsible for the drug’s antidepressant and anxiolytic effects. The mean time to peak is 12 hours. The half-life of elimination averages 51 hours.

Phenylalanine is a biologically essential amino acid that acts as a precursor to tyrosine and the catecholamines (epinephrine, norepinephrine, dopamine, and tyramine), and is a constituent of many central nervous system neuropeptides. Normal dietary levels of phenylalanine are approximately 1-2 grams daily. Phenylalanine appears in two forms which are identical mirror images of each other: L-phenylalanine, a nutritional supplement, and D-phenylalanine, an effective painkiller and antidepressant due to its ability to inhibit the breakdown of enkephalins, the brain’s natural pain killers.

Cyclamic acid (Cyclamate) is banned in the United States but it is used in many other Western countries without safety concerns. Cyclamate interacts with the sweet taste receptor subunit T1R3 transmembrane domain. Initially it was recommended for use in treatment of obese patients and by individuals with diabetes but in August 27, 1970 FDA concluded that there was no substantial evidence of effectiveness of cyclamate compounds at any level for treatment of obese patients and individuals with diabetes and therefore prohibited continued sale of cyclamate containing products with drug labeling. cyclamate is the putative carcinogenic agent. Cyclamate was tested in the Maximal Electroshock Seizure model (mice, ip), showing moderate anticonvulsant activity.

Amodiaquine is a medication used to treat malaria, including Plasmodium falciparum malaria when uncomplicated. The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. The side effects of amodiaquine are generally minor to moderate and are similar to those of chloroquine. Rarely liver problems or low blood cell levels may occur. When taken in excess headaches, trouble seeing, seizures, and cardiac arrest may occur. After oral administration amodiaquine hydrochloride is rapidly absorbed,and undergoes rapid and extensive metabolism to desethylamodiaquine which concentrates in red blood cells. It is likely that desethylamodiaquine, not amodiaquine, is responsible for most of the observed antimalarial activity, and that the toxic effects of amodiaquine after oral administration may in part be due to desethylamodiaquine.

Menadione, a drug belong to class of Vitamin K, is prescribed for the treatment of hemorrhage, vitamin K deficiency, moderate to severe forms of hypoprothrombinaemia in adults and children. Menadione is a synthetic form of vitamin K, a lipid-soluble vitamin. Vitamin K is a vital cofactor for the biosynthesis of prothrombin, factor VII, IX, X, protein C and protein S. Menadione supports the functions of osteocalcin. Large doses of menadione have been reported to cause adverse outcomes including hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, neonatal brain or liver damage, or neonatal death in some rare cases.

Quinacrine was initially developed as an anti-malarial drug marketed under the name Atabrine. Also it was approved for the teratment of ascites, however it was wothdrawn for both indication in 1995 and 2003, respectively. The drug is also used for the treatment of giardiasis, lupus, rheumatoid arthritis, refractory pulmonary effusion and pneumothorax, induce female sterilization etc. Proposed mechanisms of action include DNA intercalation interference with RNA transcription and translation, inhibition of succinate oxidation interference with electron transport, inhibition of cholinesterase, and inhibitor of phospholipase.

Adrenalone is a keton form of the natural substrate epinephrine. Adrenalone is evidently formed in vivo by hydrolytic cleavage of the diester by esterases. It is an adrenergic receptor agonist. Adrenalone inhibits the norepinephrine synthesis and dopamine beta oxidase. It is known to have very weak sympathomimetic activity when compared to adrenaline. Adrenalone has the high radioprotective effect. It is a topical nasal decongestant. Adrenalone has hemostatic, sympathomimetic and vasoconstrictor therapeutic functions.

BETANAPHTHOL (or 2-Naphthol) is used as a preservative. It is known, that this compound can cause dermatitis.