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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Kasugamycin, an aminoglycoside antibiotic, potently inhibits both gram-positive and gram-negative bacteria, binds to the 30S subunit of the bacterial ribosome, and suppresses protein synthesis. Kasugamycin was studied in clinical use for urinary tract infections due to Pseudomonas aeruginosa and was investigated its therapeutic effect on respiratory infections due to Pseudomonas aeruginosa. Experiments in vitro showed that kasugamycin did not have any appreciable effect against a variety of bacteria tested. The only exceptions were several species of gram-negative bacteria, against which antibiotics that are more satisfactory already exist. That is why further evaluation of kasugamycin for potential human use as an antipseudomonal was discontinued.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Bisbenzimide ethoxide is a fluorescent nucleic acid stain useful for DNA labeling in fluorescence microscopy and flow cytometry. It appears to bind to AT-rich regions containing at least four such basepairs. Bisbenzimide ethoxide seems to bind relatively poorly to nucleotide sequences containing the alternating step TpA. Bisbenzimide ethoxide induced apoptosis in the HL-60 cells in a time- and dose-dependent manner. Endogenous nuclear topoisomerase I activity in HL-60 cells was inhibited by treatment with Bisbenzimide ethoxide.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
alpha-N-methyl-histamine is a metabolite of histamine that plays an important role in several (patho) physiological processes. alpha-N-methyl-histamine is being a potent agonist of histamine H3 receptor can be used as an effective therapeutic alternative in migraine patients.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Erucic acid is a monounsaturated omega-9 fatty acid found mainly in the Brassica family of plants such as canola, rapeseed, wallflower seed, mustard seed as well as Brussels spouts and broccoli. Erucic acid has many of the same uses as mineral oils but with the advantage that it is more readily biodegradable. Its high tolerance to temperature makes it suitable for transmission oil. Its ability to polymerize and dry means it can be - and is - used as a binder for oil paints. Increased levels of eicosenoic acid (20:ln9) and erucic acid (22:1n9) have been found in the red blood cell membranes of autistic subjects with developmental regression. While studies done on laboratory animals in the early 1970s show that erucic acid appears to have toxic effects on the heart at high enough doses, an association between the consumption of rapeseed oil and increased myocardial lipidosis, or heart disease, has not been established for humans. While there are reports of toxicity from long-term use of Lorenzo's oil (which contains erucic acid and other ingredients), there are no reports of harm to people from dietary consumption of erucic acid. In 2003, Food Standards Australia set a provisional tolerable daily intake (PTDI) for an average adult of about 500 mg/day of erucic acid, extrapolated based on "the level that is associated with increased myocardial lipidosis in nursing pigs."
o-Phenylenediamine is a chemical intermediate used in the synthesis of fungicides, corrosion inhibitors, pigments, and pharmaceuticals. It is also used to remove elemental sulfur in mining ores, and to remove aldehyde color formers in polymeric products. o-Phenylenediamine is also a substrate of enzyme-catalyzed oxidation reactions. 2,3-Diaminophenazine was detected as a product of peroxidase-catalyzed oxidation of o-phenylenediamine dihydrochloride in ELISA procedures. o-Phenylenediamine is a methaemoglobin-producer. Oral administration of o-phenylenediamine led to significantly increased incidences of liver tumors in the rat and mouse.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Sodium aurothiomalate (also known as gold sodium thiomalate) is a gold compound that is used for its immunosuppressive anti-rheumatic effects. It was indicated in the treatment of selected cases of active rheumatoid arthritis—both adult and juvenile type. The greatest benefit occurs in the early active stage. In late stages of the illness when cartilage and bone damage have occurred, gold can only check the progression of rheumatoid arthritis and prevent further structural damage to joints. It cannot repair damage caused by previously active disease. Gold Sodium Thiomalate should be used only as one part of a complete program of therapy; alone it is not a complete treatment. The mode of action is unknown, but was found, that aurothiomalate is able to inhibit Microsomal prostaglandin E synthase-1 (mPGES-1 expression. mPGES-1 is a terminal enzyme in the production of prostaglandin E2 (PGE2) and its expression is upregulated during inflammation. mPGES-1 is considered as a potential drug target for the treatment of arthritis to reduce adverse effects related to the current non-steroidal anti-inflammatory drugs (NSAIDs).
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
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.
Narceine methyl ester and narceine are potent alkaloids which were isolated from Corydalis longipes were found effective in vitro at very low concentration, i.e., 100~500 ppm against spore germination of some test plant pathogenic fungi (Alternaria solani, A. tagetica, Cercospora abelmoschi, Curvularia maculans, Erysiphe cichoracearum, E. pisi, Fusarium udum, Helminthosporium oryzae, H. penniseti, Ustilago cynodontis). George Bell Frankforter was
the first person to isolate narceine (in 1893) during his Ph.D. research for August Hofmann at the University of Berlin. Narceine has a weak morphine-like action, but is not much used in medicine. It may be administered in a pill, as a mild hypnotic and to allay cough; it is less depressant than morphine and does not constipate. Ethylnarceine is a narcotic, analgesic, and antitussive.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
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
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Thiosalicylic acid is an analgesic and anti-inflammatory agent. It is used (in form of sodium salt) to relieve symptoms of acute gout, painful musculoskeletal conditions, osteoarthritis and rheumatic fever. The drug exerts its action by inhibiting prostaglandin synthesis. Thiosalicylic acid usage is associated with the risk of contact dermatitis.