U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 8571 - 8580 of 8601 results

Kainic acid (kainate) is a natural marine acid present in some seaweed. Kainic acid is a potent neuroexcitatory amino acid that acts by activating receptors for glutamate, the principal excitatory neurotransmitter in the central nervous system. Kainic acid is commonly injected into laboratory animal models to study the effects of experimental ablation. Kainic acid is a direct agonist of the glutamic kainate receptors and large doses of concentrated solutions produce immediate neuronal death by overstimulating neurons to death. Such damage and death of neurons is referred to as an excitotoxic lesion. Thus, in large, concentrated doses kainic acid can be considered a neurotoxin, and in small doses of dilute solution kainic acid will chemically stimulate neurons. Kainic acid is utilised in primary neuronal cell cultures and acute brain slice preparations [5] to study of the physiological effect of excitotoxicity and assess the neuroprotective capabilities of potential therapeutics. Kainic acid is a potent central nervous system excitant that is used in epilepsy research to induce seizures in experimental animals, at a typical dose of 10–30 mg/kg in mice. In addition to inducing seizures, kainic acid is excitotoxic and epileptogenic. Kainic acid induces seizures via activation of kainate receptors containing the GluK2 subunit and also through activation of AMPA receptors, for which it serves as a partial agonist.
Status:
Possibly Marketed Outside US
Source:
Japan:Minodronic Acid Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Minodronic acid (RECALBON®, Bonoteo®), a third-generation bisphosphonate, was approved in Japan for the oral treatment of osteoporosis. This drug increases the bone mineral density and the strength by inhibiting osteoclastic bone resorption. Nitrogen-containing bisphosphonates, such as minodronic acid (RECALBON®, Bonoteo®) induce osteoclast apoptosis by inhibiting farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Inhibition of FPPS in osteoclasts prevents the biosynthesis of isoprenoid lipids that are required for the prenylation of small GTPase signaling proteins necessary for osteoclast function. Similarly, nitrogen-containing bisphosphonates have been shown to inhibit farnesyl pyrophosphate/geranyl pyrophosphate synthase activity.
Status:
Possibly Marketed Outside US
Source:
NCT01990807: Phase 4 Interventional Unknown status Childhood Acute Lymphoblastic Leukemia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Disodium iminodiacetate is a salt of iminodiacetic acid (IDA). The iminodiacetate anion can act as a tridentate ligand to form a metal complex with two, fused, five-membered chelate rings. Iminodiacetic acid is used to diagnose problems of the liver, gallbladder and bile ducts in an imaging procedure, called as hepatobiliary iminodiacetic acid (HIDA) scan. A nuclear medicine scanner tracks the flow of the tracer from the liver into the gallbladder and small intestine and creates computer images. In addition, iminodiacetate is a part of the iminodiacetate-modified poly-L-lysine dendrimer (IMPLD), a fluorescent bone-imaging agent. IMPLD is used in the diagnosis of bone tumors, or to be used for the delivery of chemotherapy drugs or therapeutic agents. Bones differ from other body tissues in their unique calcium mineral composition, which consists mainly of hydroxyapatite (HA). IDA functionalization could be used as a general approach to bone targeting by increasing affinity for HA, enabling the transport of other molecules or particles to bones.
Status:
Possibly Marketed Outside US
Source:
Canada:SODIUM HEXAFLUOROSILICATE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ammonium hexafluorosilicate is a white crystalline solid. Corrodes aluminum. Used as a disinfectant, in etching glass, metal casting, and electroplating. Ammonium hexafluorosilicate is useful for the treatment of dentin hypersensitivity, since ammonium hexafluorosilicate induced calcium phosphate precipitation from the saliva; therefore, it has a continuous effect on dentin tubules occlusion under a simulated oral environment. Ammonium hexafluorosilicate has been applied to arrest caries without discoloration. The major use of sodium hexafluorosilicate and fluorosilicic acid is as fluoridation agents for drinking water. Sodium hexafluorosilicate has also been used for caries control as part of asilicophosphate cement, an acidic gel in combination with monocalcium phosphate monohydrate,and a two-solution fluoride mouth rinse. Both chemicals are also used as a chemical intermediate (raw material) for aluminum trifluoride, cryolite (Na3AlF6), silicon tetrafluoride,and other fluorosilicates and have found applications in commercial laundry. Other applications for sodium hexafluorosilicate include its use in enamels/enamel frits for china and porcelain, in opalescent glass, metallurgy (aluminum and beryllium), glue, ore flotation, leather and wood preservatives, and in insecticides and rodenticides. It has been used in the manufacture of pure silicon, as a gelling agent in the production of molded latex foam, and as afluorinating agent in organic synthesis to convert organodichlorophosphorus compounds to the corresponding organodifluorophosphorus compound. In veterinary practice, external applicationof sodium hexafluorosilicate combats lice and mosquitoes on cattle, sheep, swine, and poultry, and oral administration combats roundworms and possibly whipworms in swine and prevents dental caries in rats. Apparently, all pesticidal products had their registrations cancelled or they were discontinued by the early 1990s
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Bucloxic acid, a nonsteroidal anti-inflammatory agent, which was studied to treat the chronic glomerular nephropathy.

Class (Stereo):
CHEMICAL (RACEMIC)

Targets:


Iophendylate (Pantopaque (in USA) or Myodil, formerly manufactures by Glaxo Laboratories (London,UK) was commonly used from the 1940s until the late 1980s for myelography, cisternography, and ventriculography; the use of oil-based contrast agents such as Myodil has been discontinued, and images of intradural oil-based contrast are rarely encountered at present. In 1942 Van Wagenen (a neurosurgical colleague of Warrens, at the University of Rochester) identified Iophendylate as causing chemical meningitis in 30 patients where "space-displacing masses within the spinal canal were suspected". Iophendylate has been shown to be both a radiographic and magnetic resonance (MR) contrast agent in patients with suspected cord abnormalities who underwent MR examination following myelography. The iophendylate appears as a linear band of high signal intensity along the dependent portion of the spinal canal on MR images obtained with a repetition time of 500 msec and an echo time of 30 msec. Recently was published report, where depicted a unique case of posteriorly located subdural trapped Myodil, about three decades after myelography. The clinical picture of that case highlighted that such a complication didn’t carry the risk of arachnoiditis and could remain silent for several decades. Although Iophendylate is not used for evaluation of spinal disease anymore in the modern diagnostic era, its former use and its intrathecal persistence makes its recognition in MR imaging important. That case emphasized the necessity of awareness about these rare features which continue to present even decades after abandonment of oil-based myelography.
Status:
Possibly Marketed Outside US
Source:
Canada:CAMPHORICUM ACIDUM
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Camphoric acid is a product of oxidation of camphor, naturally occurring in rosemary. In the early twentieth century, camphoric acid was used in the night-sweats of phthisis and was also employed in solution as a local antiseptic to the nose, throat, and bladder. Camphoric acid was found to induce the expression of glutamate receptors NMDAR1, GluR3/4, and mGluR8.
Status:
Possibly Marketed Outside US
Source:
Zevtera by Avir Pharma Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ceftobiprole is a fifth-generation cephalosporin antibiotic. It was discovered by Basilea Pharmaceutica and was developed by Johnson & Johnson Pharmaceutical Research and Development. The drug is demonstrates activity against clinically important gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicilliin-resistant Staphylococcus pneumoniae, and Enterococcus faecalis. The drug also has demonstrated activity against gram-negative bacteria including Citrobacter spp., Escherichia coli, Enterobacter spp., Klebsiella spp., Serratia marcescens, and Pseudomonas aeruginosa. The drug has gained regulatory authorization from European states for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).
Alpha-ketoglutarate (AKG), an endogenous intermediary metabolite in the Krebs cycle, is a molecule involved in multiple metabolic and cellular pathways. As an intermediate of the tricarboxylic acid cycle, AKG is essential for the oxidation of fatty acids, amino acids, and glucose. Extracellular AKG is a significant source of energy for cells of the gastrointestinal tract. As a precursor for the synthesis of glutamate and glutamine in multiple tissues (including liver, skeletal muscle, heart, brain, and white adipose tissue), AKG bridges carbohydrate and nitrogen metabolism for both conservation of amino acids and ammonia detoxification. Additionally, emerging evidence shows that AKG is a regulator of gene expression and cell signaling pathways (including the mammalian target of rapamycin and AMPactivated protein kinase). Thus, AKG is an attractive dietary supplement in animal and human nutrition to improve cellular energy status, immunity, and health.AKG can decrease protein catabolism and increase protein synthesis to enhance bone tissue formation in the skeletal muscles and can be used in clinical applications. In addition to these health benefits, a recent study has shown that AKG can extend the lifespan of adult Caenorhabditis elegans by inhibiting ATP synthase and TOR. Orally, AKG is used for kidney disease, gastrointestinal disorders, bacterial overgrowth, intestinal toxemia, liver dysfunction, and chronic candidiasis. It is also used for improving peak athletic performance, improving amino acid metabolism in hemodialysis patients, and cataracts. Intravenously, AKG is used for preventing ischemic injury during heart surgery, improving renal blood flow after heart surgery, and preventing muscle protein depletion after surgery or trauma.
Status:
Withdrawn

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Pangamic acid (6-O-(dimethylaminoacetyl)-D-gluconic acid) has been detected 1938 and described as a natural, universally occurring substance with multiple biological and medical functions. In this respect pangamic acid has been worldwide on the market since decades as a drug stimulating cellular respiration. In addition to the natural pangamic acid, diisopropylammonium dichloroacetate (DIPA), a synthetic product not found in biological material, is on the market requesting similar biological functions. Pangamic acid is the name given to a product originally claimed to contain D-gluconodimethyl aminoacetic acid, which was obtained from apricot kernels and later from rice bran. It is also referred to as vitamin B15, but pangamic acid is not generally recognized as a vitamin. Despite serious safety concerns, pangamic acid is used for improving exercise endurance; treating asthma and related diseases, skin conditions including eczema, lung problems, painful nerve and joint conditions, cancer, and arthritis; improving the oxygenation of the heart, brain, and other vital organs; and “detoxifying” the body. It is also used for treating alcoholism, hangovers, and fatigue; protecting against urban air pollutants; extending cell life; strengthening the immune system; lowering bloodcholesterol levels; and assisting in hormone regulation. Since there is no standard identity for the chemicals in pangamic acid, how it might work is unknown. Although pangamic acid is also called vitamin B15, there is no research that shows it is required by the body, as the term “vitamin” would suggest. The United States Food and Drug Administration has recommended seizing any chemicals advertised as pangamic acid and restraining the importation and interstate shipment of pangamic acid on the grounds that pangamic acid and pangamic acid products are unsafe for use and have no known nutritional properties

Showing 8571 - 8580 of 8601 results