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

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Showing 1211 - 1220 of 4002 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dihydrocoumarin is a concentrated aromatic and flavor ingredient which may be used in flavor and fragrance compounds according to legal and IFRA or FEMA GRAS/FDA guidelines. Dihydrocoumarin is a common compound found in sweet clover that has been studied as a disruptor of epigenetic processes in cells. Epigenetic processes control gene expression within a cell and are highly influenced by environmental factors. Epigenomic disruptions change which genes are expressed and to what extent and are not linked to DNA mutations. Dihydrocoumarin has been shown to inhibit the sirtuin deacetylase family, specifically Sir2, SIRT1, and SIRT2.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tribromoethanol is a popular injectable anesthetic agent commonly used for embryo-transfer surgery for the generation of transgenic mice and sometimes rats. In humans and animals, Tribromoethanol produces a generalized CNS depression, including both the respiratory and cardiovascular centers. It undergoes conjugation with glucuronic acid during metabolism in the liver, followed by excretion in the urine as TBE glucuronate. Tribromoethanol causes rapid and deep anesthesia followed by rapid and full postoperative recovery, but the margin of safety between anesthetic and the lethal dose is narrow. Depression of respiration and circulation, together with its general unpredictability, eventually discouraged its use. Although Tribromoethanol solutions are often referred to as Avertin, this is a misnomer. Avertin was the trade name for Winthrop Laboratories’ proprietary Tribromoethanol formulation, which is no longer available. Marketing of pharmaceutical-grade Tribromoethanol took place under several proprietary names, including Avertin, Bromethol, Ethobrom, and Narkolan, each as a 66.7% (w/w) solution of Tribromoethanol in tertiary-amyl alcohol, wherein each milliliter contained 1 g of Tribromoethanol. Although pharmaceutical-grade TBE has not been commercially available or routinely used for human or veterinary anesthesia for several years, the agent has received widespread acceptance for use in the various manipulations required for the production of genetically engineered mice and rats. Tribromoethanol is an attractive anesthetic choice for many researchers because it is easy and inexpensive to make in the laboratory from readily available reagents, requires no special equipment for its administration, and is not subject to federal or state drug enforcement agency storage or accountability regulations. More importantly, the i.p. injection of TBE results in the simple and rapid induction of short-term surgical anesthesia sufficient for the vasectomy, embryo transfer, and tail amputation for Southern blot analysis—all necessary elements in the production of genetically engineered animals.
ABT-491 is highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist, developed by Abbott Laboratories for allergic rhinitis treatment. ABT-491 is a potent antagonist of responses linked to the PAF receptor at the cellular level, especially platelets and neutrophils. ABT-491 was also effective in blocking platelet activation in blood, indicating that the presence of high concentrations of protein and other serum factors slightly alters the ability of ABT-491 to interact with PAF receptor. ABT-491 effectively antagonizes PAF-induced platelet and neutrophil responses at submicromolar concentrations in vitro and exhibits in vivo efficacy in alleviating PAF-mediated inflammatory and pathological processes in various animals, including guinea pigs, mice, and rats, via either i.v., i.p. or p.o. routes.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



L-365,260 is an antagonist of gastrin and brain CCK-B receptor. In vivo, oral administration of L-365,260 antagonized gastrin-stimulated acid secretion. L-365,260 is used as a tool compound to investigate gastrin and brain CCK-B and their role in psysiology and disease. In a double-blind placebo-controlled study L-365,260 did not augment the analgesic effect of morphine in subjects with chronic neuropathic pain. Preclinical studies demonstrated modes activity of L-365,260 in models of anxiety and ulcers.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

CE-178,253 benzenesulfonate is a CB1 antagonist discovered by Pfizer medicinal chemists. In vitro, CE-178,253 exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.33 nM) and functional assays (Ki = 0.07 nM). CE-178,253 has low affinity (Ki > 10,000 nM) for human CB2 receptors. In vivo, CE-178,253 exhibits concentration-dependent anorectic activity in both fast-induced re-feeding and spontaneous nocturnal feeding FI models. In two preclinical models of obesity, CE-178,253 dose-dependently promotes weight loss in diet-induced obese rats and mice.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



4'-Chlordiazepam or Ro5-4864 (7-chloro-5- (4-chlorophenyl)-1,3-dihydro-1-methyl-2-H-1,4-benzodiazepine-2)) is a ligand of peripheral-type benzodiazepine receptor (translocator protein or Tspo). It exerts neurosteroidogenic activity. 4'- chlordiazepam is sedative, convulsant and anxiogenic in rodents.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Tecnazene, also known as 2,3,5,6-tetrachloro-1-nitrobenzene or tcnb, is a member of the class of compounds known as nitrobenzenes. Tecnazene is a dual acting pesticide. It is used as a plant growth regulator to suppress sprouts on potatoes during storage and as a fungicide to prevent dry rot on the tubers. Human exposure is primarily through ingestion of food residues, with an Acceptable Daily Intake level of 0.01 mg/kg of body weight according to FAO/WHO guidelines. Tecnazene is commercially available as granules and as dispersible dust formulations.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Fensulfothion is an organophosphate insecticide/nematicide. Fensulfothion is highly toxic to man and other non-target terrestrial and aquatic organisms from acute oral and dermal routes of exposure. Fensulfothion is registered for use as preplant or at-planting soil application to tobacco and various fruits and vegetables. Postplant topical applications are permitted in addition to the at-planting application on corn, peanuts, and rutabagas. Topical application is also permitted on commercial and ornamental turf. Fensulfothion is an organophosphate insecticide/nematicide that kills primarily by contact action, but also provides some systemic control of insects attacking the foliage of treated plants. The mode of action is by phosphorylating the acetylcholinesterase enzyme of tissues, allowing accumulation of acetylcholine at nerve junctions, with subsequent blocking effects upon the central nervous system.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Didiavalo (premethadone) is a methadone analog and precursor. Didiavalo possesses analgetic properties with the effective dose in rats 30 times higher than the analgesic dose of morphine.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Methidathion is an organophosphate insecticide and acaricide (U.S. EPA, 1988). Methidathion and its oxygen analog produce their toxic reaction primarily through their inhibition of cholinesterase (ChE) enzymes, including acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Methidathion is used to control a variety of insects and mites in many crops such as fruits, vegetables, tobacco, alfalfa and sunflowers. Methidathion is also used in greenhouses and on rose cultures. It is especially useful against scale insects.

Showing 1211 - 1220 of 4002 results