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

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Showing 181 - 190 of 1447 results

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 (ACHIRAL)

Targets:


MK6-83 is an activator of TRPML and its F408Δ and F465L mutants. MK6-83 restores endolysosomal trafficking and zinc homeostasis in lysosomes of mucolipidosis type IV (MLIV) mutant fibroblasts.
Status:
Other

Class (Stereo):
CHEMICAL (EPIMERIC)


Conditions:

Nicotine-1'-N-oxide (NNO) is an oxidation product of nicotine. Flavin-containing monooxygenase is responsible for the oxygen transfer. Nicotine N'- oxide is a primary metabolite of nicotine, although only about 4-7% of nicotine absorbed by smokers is metabolized via this route. It appears that NNO is not further metabolized to any significant extent, except by reduction back to nicotine, which may lead to recycling of nicotine in the body.
Andrograpanin is a component of Andrographis paniculata, a traditional Chinese medicine (TCM) that has been effectively used for treatment of infection, inflammation, cold, fever, and diarrhea in China. Andrograpanin inhibited productions of NO and pro-inflammatory cytokines through down-regulating iNOS and pro-inflammatory cytokines gene expression levels. Further studies suggested that down-regulation of p38 mitogen-activated protein kinase (MAPKs) signaling pathways were involved in the anti-inflammatory activities of andrograpanin. This study provided evidences that andrograpanin might be useful as a potential anti-inflammatory leading compound for inflammatory drug development. Andrograpanin has the potential to modulate the chemokine pathway and the effect of andrograpanin might contribute to the anti-infectious function of A. paniculata.
GYKI-472611 is a non-competitive AMPA antagonist receptor. Also, GYKI-47261 was considered as a potent CYP2E1 inducer. In vivo, it displays broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-472611 developed by IVAX Drug Research Institute Ltd. for treatment of epilepsy and parkinsonism.