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

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Showing 2421 - 2430 of 8583 results

Norvancomycin is an analog of glycopeptide antibiotic vancomycin. It was first found to be produced by a soil microorganisms such Nocardia orientalis and Amycolatopsis orientalis and recently was found in actinomycete Amycolatopsis orientalis CPCC200066. Norvancomycin can be derived by demethylation at N-terminus of vancomycin. It has significant inhibitory activity against Gram-positive cocci and bacilli. The mode of action of norvancomycin is based on its ability to bind to the cell-wall peptidoglycan of Gram-positive bacteria terminating tripeptide -L-Lys-D-Ala-D-Ala. Similar to vancomycin in terms of antibacterial activity, spectrum and clinical efficacy norvancomycin has more potent antibiotic activity against Staphylococcus aureus and higher affinity for bacteria cell wall analogue DALAA than vancomycin. Norvancomycin has been widely used in China to treat endocarditis, osteomyelitis and other severe infections caused by Staphylococcus aureus (including methicillin-resistant strains). The adverse drug reactions of norvancomycin are like vancomycin, such as nephrotoxicity, ototoxicity, rash and itching. Norvancomycin is not available therapeutically outside of China.
Status:
Possibly Marketed Outside US
Source:
RAJANI
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Timolol maleate (ISTALOL) is a non-selective beta-adrenergic receptor blocking agent. Timolol maleate is a beta1 and beta2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. In its opthalmic form, Timolol maleate, is used to treat open-angle and occasionally secondary glaucoma. Timolol maleate, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Timolol maleate ester is a Timolol maleate specified impurity E [EP]. Timolol impurities are used for ANDA filling/DMF filling and genotoxic study.
(R)-Timolol is the (R)-enantiomer of non-selective Beta antagonist Timolol. (R)-Timolol is a ß-adrenergic blocking agent that binds only to nonspecific sites in the particulate fraction of the heart, lungs, and brain. (R)-Timolol is an antihypertensive agent that increases ocular blood flow and reduces intraocular pressure. (R)-Timolol is one of the impurities in commercial formulation of (S)-Timolol.
Vortioxetine DL-lactate is a lactate salt of vortioxetine and its chemical name is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]-piperazine (RS)-2-hydroxypropanoate. Vortioxetine DL-lactate is manufactured from the milled Vortioxetine hydrobromide via the nonisolated free base. One site is involved in the manufacture of the lactate salt of Vortioxetine. Vortioxetine is an antidepressant for the treatment of major depressive disorder. Unlike the film-coated tablets where a hydrobromide salt of the active substance is used, the oral drops formulation contains vortioxetine DL-lactate as the active substance which shows higher solubility in polar solvents. Vortioxetine is a novel multimodal antidepressant that acts as a serotonin (5-HT)3, 5-HT7, and 5-HT1D receptor antagonist; 5-HT1B receptor partial agonist; 5-HT1A receptor agonist; and 5-HT transporter inhibitor in vitro.
Cotarninium is a uterotonic agent. It increases the tone of smooth muscles of internal organs, particularly the uterus. Indicated for the treatment of uterus subinvolution (after childbirth and abortion), dysfunctional uterine bleeding and bleeding due to fibroids and inflammatory processes. Side effects are nausea, allergic reactions. Contraindications are pregnancy and hypersensitivity to the agent.
Status:
Possibly Marketed Outside US
Source:
Nitroblue tetrazolium (NBT) test
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitroblue Tetrazolium (NBT) is a chromogenic substrate that, like other tetrazolium compounds, can be reduced to produce a colored formazan derivative. Conventionally, a semi-quantitative microscopic NBT assay is used to determine the production of superoxide anion (O2(-)) in various phagocytic cells. This microscopic assay is conducted by counting the cells containing blue NBT formazan deposits, which are formed by reduction of the membrane permeable, water-soluble, yellow-colored, nitroblue tetrazolium (Y-NBT) by O2(-). NBT test, the oldest and most recognized diagnostic test for chronic granulomatous disease (CGD), relies on light microscopy to provide a mostly qualitative determination of phagocyte NADPH oxidase activity: production of blue reduced NBT formazan in normal cells but not in those from patients with CGD. NBT can also be used as a chromogenic activity stain for oxidoreductases in gels or solutions. More commonly NBT is often paired with 5-bromo-4-chloro-3-inolyl phosphate (PCIB) for the colorimetric detection of alkaline phosphatase activity. Alkaline phosphate converts PCIB to a product that reduces NBT to its formazan derivative, resulting in a black-purple precipitate.
Status:
Possibly Marketed Outside US
Source:
Unknown by Buser, H.-R.|Mueller, M.D.|Balmer, M.E.|Poiger, T.|Buerge, I.J.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Enzacamene, (-) [Bicyclo[2.2.1]-heptan-2-one, 1,7,7-trimethyl-3-[(4-methylphenyl)methylene]-, (1S,3E,4R)-] is one of enantiomer of Enzacamene (4-MBC) -- organic sunscreen components, that protects against UV radiation and may therefore help in the prevention of skin cancer. Enzacamene can exist as a cis-(Z)- and trans-(E)-isomer due to the exocyclic carbon-carbon (styrene) double bond. A commercial Enzacamene from a major supplier of UV filters showed the presence of only the (E)-isomer However, it is known that, upon exposure to light, (E)-4-Enzacamene is photochemically isomerized reversably to (Z)-4-Enzacamene. Both (E)- and (Z)-Enzacamene are chiral and thus consist of enantiomers (optical isomers). In a technical material and in a major brand sun lotion, Enzacamene was shown to consist entirely (>99%) of (E)-isomers and to be racemic. Wastewater showed the presence of both (E)- and (Z)-Enzacamene with a clear excess of (E)-isomers (E >Z). Untreated wastewater showed a nearly racemic composition suggesting that most if not all commercial Enzacamene is racemic. Treated wastewater indicated some excess of (R)- or (S)-stereoisomers ikely as a result of some enantioselective (bio)degradation in wastewater treatment plants. Enantiomers may show different biological behavior with respect to uptake, metabolism, and excretion and often differ in toxicity and other biological effects.

Showing 2421 - 2430 of 8583 results