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

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Showing 1081 - 1090 of 4002 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Dibutyl oxalate is used in the manufacture of lubricants is biologically toxic causing neurological degradation characterized by ataxia and stupor. Sufficient dosing of dibutyl oxalate induces oxalate retinopathy, an experimental model of "flecked retina". In this model, the retinal flecks are the result of an intracellular accumulation of calcium oxalate in the RPE cells.
Strychnine-N-oxide is the major metabolite of Strychnine. Strychnine, the major alkaloid present in $trychnos:nuxypmicagseeds has been reported to stimulate the entire central nervous system with preference for the spinal cord. It is a powerful convulsant and because of this property, it is an important pharmacological tool as it plays a unique role as an inhibitor of post synaptic inhibitory impulses. It is useful to study inhibitory transmitter and receptor types. However, because of its extreme toxicity, strychnine does not have any therapeutic application in the Western system of medicine. Strychnine-N-oxide is less toxic and less convulsive than strychnine itself. However, strychnine N-oxide is not being used as a therapeutic agent now probably because of the threat of convulsions at higher doses. Strychnine-N-oxide is a muscarinic allosteric agent.
P-88-8991, (+)- is a metabolite of Iloperidone. It has functional affinity for noradrenergic, dopaminergic and serotoninergic receptors. Humans produce only one enantiomer stereospecifically following administration of Iloperidone. Preclinical studies revealed that P-88-8991, (+)- might be useful for the treatment of psychotic disorders such as schizophrenia and bipolar disorders.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tribufos is an organophosphate defoliant used for cotton crops. It is specifically used to defoliate cotton in preparation for machine harvesting. Tribufos inhibits CB1 in vivo, without cholinergic poisoning signs, by 50% at 50 mg/kg intraperitoneally with a recovery half-time of 3-4 days, indicating covalent derivatization.
MK-912 is non-specific alpha-2 adrenergic receptor antagonist, with high affinity for the alpha-2-A, alpha-2B, and alpha-2C variants. Originally developed by Merk & Co, it has been investigated for potential therapeutic properties for the treatment of depression and diabetes. MK-912 is also regularly used as a molecular probe in biomedical studies seeking information about alpha-2 adrenergic receptors.
Saikosaponin A is a triterpene saponin found in Bupleurum that exhibits anti-inflammatory, analgesic, neuromodulatory, anticancer, and immunosuppressive activities. Saikosaponin A decreases production of TNF-α, IL-1β, and IL-2 and increases mechanical withdrawal thresholds and thermal withdrawal thresholds in animal models of chronic constructive injury. Saikosaponin A also decreases self-administration of cocaine and morphine. In colon carcinoma cells, saikosaponin A causes activation of caspases 2, 3, 8, and 9 and PARP, induces apoptosis, and decreases expression of Bcl-2 and XIAP. Additionally, this compound inhibits the proliferation and activation of ConA-treated T cells, inducing G0/G1 phase cell cycle arrest and decreasing expression of TNF-α, IL-2, and IFN-γ.
Estragole (ES) is a natural constituent of a number of plants (e.g. tarragon, sweet basil and sweet fennel) and their essential oils have been widely used in foodstuffs as flavouring agents. Estragole ES was given GRAS Generally Recognized As Safe status by the Flavor and Extract Manufacturer’s Association FEMA, 1965 and is approved by the Food and Drug Administration for food use 21 CFR code of Federal Regulation 121.1164 . Several studies with oral, i.p. or s.c. administration to CD-1 and B6C3F1 mice have shown the carcinogenicity of ES. In vivo and in vitro experimental assays have shown that EST has sedative, anticonvulsant, antioxidant, antimicrobial, and anesthetic activity.
The selective serotonin reuptake inhibitor fluoxetine consists of equal amounts of R and S stereoisomers (antidepressant Prozac (racemic fluoxetine). Binding to the transporter confirmed selectivity of R- and S-fluoxetine for the 5-HT transporter versus the dopamine (DA) and norepinephrine (NE) human transporters. In addition, receptor binding studies demonstrated significant affinity of R-fluoxetine, but not S-fluoxetine, for human 5-HT(2A) and 5-HT(2C) receptor subtypes. R-fluoxetine acts as an antagonist at 5-HT(2A) and 5-HT(2C) receptors. The attempt to develop a single-enantiomer formulation of fluoxetine for the treatment of depression was unsuccessful. Eli Lilly has terminated its licensing and development agreement with Marlborough, Mass.-based Sepracor for (R)-fluoxetine, the single-isomer version of Lilly's antidepressant Prozac.R-enantiomer of fluoxetine, at its highest administered dose, led to statistically significant prolongation of cardiac repolarization in phase II studies; the studies were subsequently stopped.
Status:
Other

Class (Stereo):
CHEMICAL (MIXED)


Conditions:

Triadimenol is a triazole-type fungicide that is identified as weak estrogen receptor agonist. Triadimenol is a systemic fungicide with protective, curative and eradicant action. Absorbed by the roots and leaves, with ready translocation in young growing tissues, but less ready translocation in older, woody tissues. Triadimenolis used for controlling of powdery mildews, rusts and Rhynchosporium in cereals, and, when applied as a seed treatment, control of bunt, smuts, Typhula spp., seedling blight, leaf stripe, net blotch and other cereal diseases. Also used on vegetables, ornamentals, coffee, hops, vines, fruit, tobacco, sugar cane, bananas and other crops, mainly against powdery mildews, rusts and various leaf spot diseases.
Mesaconitine is a diterpene alkaloid, from the plants of the Aconitum genus, Ranunculaceae. Mesaconitine is a centrally acting analgesic without affinity to opioid receptors. It has been reported that the antinociception is due to an interaction with the noradrenergic system. As a neurotoxic, it opens the TTX-sensitive Na+ channels in the heart and other tissues and induces arrhythmia. The activity of Mesaconitine, which is a chemical analog of Aconitine, on TTX sensitive Na+ channels in the heart and other tissues is stronger than that of Aconitine. The duration of its neurotoxic effect is shorter. It possesses an hypotensive activity. The hypotensive action is not inhibited by an adrenergic b-blocker but abolished with muscarinic blocker. It may be partially mediated by a muscarinic mechanism. Mesaconitine binds with high affinity to the open state of the voltage-sensitive sodium channels at site 2, thereby causing a persistent activation of the sodium channels, which become refractory to excitation.

Showing 1081 - 1090 of 4002 results