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

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Showing 781 - 790 of 4002 results

Chrysophanic acid (Chrysophanol) is a member of the anthraquinone family abundant in rhubarb, a widely used herb for obesity treatment in Traditional Korean Medicine. Chrysophanol has been shown to induce cell death in different types of cancer cells. Chrysophanol inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K. Chrysophanol also effectively suppresses breast cancer cell proliferation and facilitates chemosentivity through modulation of the NF-κB signaling pathway. A treatment of chrysophanol could reduce significantly the clinical signs and the levels of inflammatory mediators in a colitis model caused by DSS treatment. The anti-inflammatory activities of chrysophanol could be attributed, at least in part, to the inhibition of proinflammatory cytokine production (TNF-α and IL-6), COX-2, and iNOS protein expression. These effects of chrysophanol are caused by the inhibition of LPS-induced NF-κB activation, IκB-α degradation, and caspase-1 activation. These results provide experimental evidence showing that chrysophanol might prove useful in the treatment of inflammatory diseases.
5-(2-Aminopropyl)benzofuran (5-APB) is an empathogenic psychoactive compound of the substituted benzofuran, substituted amphetamine and substituted phenethylamine classes. 5-(2-Aminopropyl)benzofuran is a serotonin–norepinephrine–dopamine reuptake inhibitor and serotonin–norepinephrine–dopamine releasing agent. The toxicity and long-term health effects of recreational 5-APB use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown/ 5-(2-Aminopropyl)benzofuran 's high affinity for the 5-HT2b receptor makes it likely that 5-APB would be cardiotoxic with long-term use, as seen in other 5-HT2B agonists such as fenfluramine and MDMA.
LM11A-31 is a small, nonpeptide, monomeric ligand of p75 neutrophin receptor (p75NTR). The compound promotes neuron survival in vitro. PharmatrophiX is developing a modified version of LM11A-31 (LM11A 31 BHS) for the oral treatment of Alzheimer's disease.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

U-92016A is a psychoactive drug and research chemical used in scientific studies. U-92016A acts as a potent, high efficacy, and selective 5-HT1A receptor full agonist with a long duration of action.
FK-960 [N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate], a novel putative anti-dementia drug of piperazine derivative, ameliorates memory deficits in a variety of animal models of dementia in rats and monkeys, and also augments long-term potentiation (LTP) in the mossy fiber-CA3 pathway in guinea-pig hippocampal slices. FK-960 acts as Serotonin modulator. FK-960 had been in phase II clinical trials by Fujisawa Pharmaceutical (now Astellas) for the treatment of Alzheimer's disease (AD). However this study was suspended. In 2003 Phase-II for Alzheimer's disease in USA was discontinued and in Jul 2004 - Phase-II for Cognition disorders in Europe.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



JNJ-40418677 is an inhibitor of gamma-secretase. JNJ-40418677 selectively reduced amyloid β 42 secretion in human neuroblastoma cells and rat primary neurones, but it did not inhibit Notch processing or formation of other amyloid precursor protein cleavage products. Oral treatment of non-transgenic mice with JNJ-40418677 resulted in an excellent brain penetration of the compound and a dose- and time-dependent decrease of brain amyloid β 42 levels. Chronic treatment of Tg2576 mice (a mouse model of Alzheimer's disease) with JNJ-40418677 reduced brain amyloid β levels, the area occupied by plaques and plaque number in a dose-dependent manner compared with transgenic vehicle-treated mice.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



CP 226269 is a selective dopamine D4 agonist. This compound was developed by Pfizer for Neuroscience research. CP226269 showed a significant enhancement in the 5-trial inhibitory avoidance model.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



RAC BHFF is the potent and selective GABAB receptor positive allosteric modulator that increases the potency and efficacy of GABA. Exhibits anxiolytic and anticonvulsant activity in vivo and is orally active. RAC BHFF reduces alcohol’s reinforcing properties in alcohol-preferring rats and adds further support to the hypothesis that the positive allosteric modulators of the GABAB receptor may constitute a novel class of agents with therapeutic potential for alcohol dependence.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Nobiletin is a flavanoid isolatable from citrus peels. It has demonstrated anti-cancer properties in several in vitro cell models and garnered interest as a potential treatment for the motor and cognitive symptoms of Parkinson's disease. However, investigation of this compound has not moved beyond animal studies.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



N-(4-(2-Methoxyphenoxy)-phenyl-N-(2,2,2-trifluoroethylsulfonyl)-pyrid-3-ylmethylamine (LY487379) is a selective positive allosteric modulator at metabotropic glutamate subtype 2 receptors (mGluR2). The compound exerts antipsychotic and anxiolytic actions.