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

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Showing 2201 - 2210 of 2596 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Magnesium bromate is a white crystalline compound, insoluble in alcohol, soluble in water. Contact may cause irritation to skin, eyes, and mucous membranes. May be toxic by ingestion, inhalation and skin absorption. It is used as an analytical reagent. Has found little usage in Industry because there are better oxidizing agents available.
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.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

SR-57227A is a potent and selective agonist at the 5HT3 receptor, with high selectivity over other serotonin receptor subtypes and good blood-brain barrier penetration. SR-57227A had affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes in vitro. SR 57227A stimulated the uptake of [14C]guanidinium into NG 108-15 cells in the presence of substance P and contracted the isolated guinea-pig ileum, effects that were antagonized by the 5-H 3 receptor antagonist tropisetron. The agonist effect of SR 57227A was also observed in vivo, as the compound elicited the Bezold-Jarisch reflex in anesthetized rats, an effect that was blocked by tropisetron.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Disodium phenyl phosphate is a monophenyl ester of phosphoric acid. It is used as tool compound to study the efficacy of phosphatases. Hydrolysis of phenyl phosphate by milk phosphatases was used to used to indicate whether milk has been adequately pasteurized or whether it has been contaminated with raw milk after pasteurization. Phenyl phosphate was also used as a molecular fragment for fragment-based drug discovery of Src SH2.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

N-acetylmuramic acid (MurNAc) is a bacterial cell wall component. Peptidoglycan, also called murein, is a polymer that consists of long glycan chains that are cross-linked via flexible peptide bridges to form a strong but elastic structure that protects the underlying protoplast from lysing due to the high internal osmotic pressure. The peptidoglycan is the only cell wall polymer common to both gram-negative and gram-positive bacteria. The glycan chain is built up of alternating, β-1,4-linked N-acetylglucosamine (GlcNAc) and N-acetylmuramic acid (MurNAc) subunits. The chemistry of the glycan chains varies only slightly between different bacteria.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

(1,1'-Biphenyl)-3,3',4,4'-tetramine (3,3'-Diaminobenzidine, DAB) is an organic benzidine derivative, that used as a precursor to polybenzimidazoles. As its water-soluble tetrahydrochloride, (1,1'-Biphenyl)-3,3',4,4'-tetramine has been used in immunohistochemical staining of nucleic acids and proteins. Diaminobenzidine is oxidized by hydrogen peroxide in the presence of hemoglobin to give a dark-brown color. This color change is used to detect fingerprints in blood. The solubility of (1,1'-Biphenyl)-3,3',4,4'-tetramin in water allows for adaptability compared to other detection solutions which use toxic solvents. In research, this reaction is used to stain cells that were prepared with hydrogen peroxidase enzyme, following common immunocytochemistry protocols. Relevant to Alzheimer's disease, Aβ protein amyloid plaques are targeted by a primary antibody, and subsequently by a secondary antibody, which is conjugated to a peroxidase enzyme. This will bind (1,1'-Biphenyl)-3,3',4,4'-tetramine as a substrate and oxidize it, producing an easily observable brown color. Plaques can then be quantified for further evaluation.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Epiquinidine is an alkaloid derived from the bark of the cinchona tree. The most abundant constituents of the Cinchona barks are two pairs of erythro diastereoisomers: quinineand quinidine, which are active antimalarials. Their threo epimers, epiquinine and epiquinidine, are practically inactive. Compared to quinine and quinidine, the 9-epimers had significantly reduced hemozoin inhibition efficiency and did not affect pH-dependent aggregation of ferriprotoporphyrin IX (FPIX) heme. Magnetic susceptibility measurements showed that the 9-epimers perturb FPIX monomer-dimer equilibrium in favor of monomer, and UV-visible (VIS) titrations showed that Epiquinine and Epiquinidine bind monomer with similar affinity relative to quinine and quinidine. However, unique ring proton shifts in the presence of zinc(II) protoporphyrin IX (ZnPIX) indicate that binding of the 9-epimers to monomeric heme is via a distinct geometry.
Methoxetamine (abbreviated as MXE) is a novel psychoactive substance that is emerging on the Internet and induces dissociative effects and acute toxicity. MXE acts behaviourally as a typical dissociative anesthetic with stimulant and anxiogenic effects at lower doses, sedative/anesthetic effects at higher doses, and as a disruptor of sensorimotor gating. Its pharmacological effects have not yet been adequately investigated, but recently published articles shown, that MXE differentially affected motor activity, behavior and emotional states in rats, depending on the dose tested. Methoxetamine acts mainly as N-methyl-D-aspartate (NMDA) receptor antagonist and a serotonin reuptake inhibitor.
Guanosine 3′,5′-cyclic monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate (GTP). Cyclic GMP is a cellular regulatory agent that acts as a second messenger. Its levels increase in response to a variety of signals (acetylcholine, insulin, oxytocin). cGMP is involved in the regulation of kinases G. cGMP binds to sites on the regulatory units of protein kinase G (PKG) and activates the catalytic units, enabling them to phosphorylate their substrates. cGMP is a common regulator of ion channel conductance, glycogenolysis, and cellular apoptosis. It also relaxes smooth muscle tissues. In blood vessels, relaxation of vascular smooth muscles lead to vasodilation and increased blood flow. cGMP is a secondary messenger in phototransduction in the eye. In the photoreceptors of the mammalian eye, the presence of light activates cGMP phosphodiesterase 5 (PDE5), which degrades cGMP. The sodium ion channels in photoreceptors are cGMP-gated, so degradation of cGMP causes sodium channels to close, which leads to the hyperpolarization of the photoreceptor's plasma membrane and ultimately to visual information being sent to the brain. Mutations in the cGMP phosphodiesterase cause defects in cGMP metabolism leading to retinal disease. Inhibition of cGMP degrading PDE5 by its selective inhibitor sildenafil induced migraine without aura in 10 of 12 migraine patients and in healthy subjects.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

There is no information, related to the pharmacological application of D-gulonic acid. But is known, that it is a component of the herb Centella asiatica, and can form a complexes with tungsten(VI) and molybdenum(VI), in aqueous solutions. In addition, was studied how D-gulonic acid could serve as a immobilization support for mushroom tyrosinase.

Showing 2201 - 2210 of 2596 results