Repositioning Candidate Details
| Candidate ID: | R1302 |
| Source ID: | DB09338 |
| Source Type: | experimental |
| Compound Type: | small molecule |
| Compound Name: | Mersalyl |
| Synonyms: | Mersal |
| Molecular Formula: | C13H17HgNO6 |
| SMILES: | COC(CNC(=O)C1=CC=CC=C1OCC(O)=O)C[Hg]O |
| Structure: |
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| DrugBank Description: | Mersalyl is the sodium salt form of mersalyl acid, a mercurial diuretic. It is an outdated drug, and its approval has been discontinued by the FDA. Mersalyl acid is currently replaced by less toxic non-mercury containing diuretics . The sodium salt of a mercury-containing derivative of salicylamide, was formerly used (often in combination with theophylline) to treat edema, due to its powerful diuretic properties . Interestingly, it has been found to have antiviral properties in mice . |
| CAS Number: | 486-67-9 |
| Molecular Weight: | 483.87 |
| DrugBank Indication: | Elevated blood pressure, edema . |
| DrugBank Pharmacology: | Mersalyl acid is an organomercuric compound. It is used as a diuretic. Mercury is a heavy, silvery d-block metal and one of six elements that are liquid at or near room temperature and pressure. It is a naturally occuring substance, and combines with other elements such as chlorine, sulfur, or oxygen to form inorganic mercury compounds (salts). Mercury also combines with carbon to make organic mercury compounds . |
| DrugBank MoA: | Mersalyl is a mercurial diuretic which acts on the renal tubules, increasing the excretion of sodium and chloride, in approximately equal amounts, and of water . As a result, blood pressure and edema is markedly decreased. High-affinity binding of the divalent mercuric ion to thiol or sulfhydryl groups of proteins is believed to be the major mechanism for the activity of mercury. Through alterations in intracellular thiol status, mercury can promote oxidative stress, lipid peroxidation, mitochondrial dysfunction, and changes in heme metabolism. Mercury is known to bind to microsomal and mitochondrial enzymes, resulting in cell injury and death. For example, mercury is known to inhibit aquaporins, halting water flow across the cell membrane. It also inhibits the protein LCK, which causes decreased T-cell signaling and immune system depression. Mercury is also believed to inhibit neuronal excitability by acting on the postsynaptic neuronal membrane. It also affects the nervous system by inhibiting protein kinase C and alkaline phosphatase, which impairs brain microvascular formation and function, as well as alters the blood-brain barrier. Organic mercury exhibits developmental effects by binding to tubulin, which prevents microtubule assembly and causes mitotic inhibition. In addition, mercury produces an autoimmune response, likely by modification of major histocompatibility complex (MHC) class II molecules, self-peptides, T-cell receptors, or cell-surface adhesion molecules . |
| Targets: | Alkaline phosphatase, tissue-nonspecific isozyme antagonist; Aquaporin-1; Monocarboxylate transporter 1 antagonist |
| Inclusion Criteria: | Therapeutic strategy associated |
