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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 61 - 70 of 278 results

Schisandrin is a bioactive compound found in Schisandra chinensis. Schisandrin exhibits antioxidant properties and ameliorates ovariectomy-induced memory impairment in rats, and Aβ1-42-induced memory impairment in mice. Schisandrin has an anti-asthmatic effect on OVA-induced airway inflammation in a murine asthma model. The compound inhibits proliferation of breast cancer cell lines at concentrations of 20-100 uM.
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.
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 (ABSOLUTE)



S-17092, a prolyl endopeptidase inhibitor, is in phase I investigations with Servier in France for its potential in cognition disorders. Prolyl endopeptidase is involved in the metabolic breakdown of a number of neuropeptide neurotransmitters in the brain, and so inhibiting the action of the enzyme increases the activity of these neuropeptides. This produces nootropic effects which make S-17092 a promising and novel treatment for neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease.
77-LH-28-1 Oxalate is a salt of 77-LH-28-1. This drug is a potent, selective, bioavailable and brain-penetrant agonist of muscarinic acetylcholine receptor subtype 1. 77-LH-28-1 can increase network oscillations relevant to cognitive processing that would support the potential use of this mechanism in the treatment of cognitive impairment. 77-LH-28-1 exhibited U-shaped dose-effect functions in attenuating cocaine discrimination. 77-LH-28-1, can significantly enhance donepezil-induced gamma oscillations. These data support the notion that it should be possible to find a more efficacious AChE inhibitor or an adjunctive approach, to provide a better therapeutic intervention in Alzheimer's disease.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



BMS-299897 is an orally bioavailable, sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP). BMS-299897 has the potential for treatment of Alzheimer's disease.
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. Tubastatin A is a very selective HDAC6 inhibitor with 100 to over 1000-fold selectivity for HDAC6 over other HDAC classes. Tubastatin A increases the total numbers of mitochondria and restores the number of moving mitochondria in DRG neurons. It reverses the axonal loss in peripheral neurons in the mouse model of Charcot-Marie-Tooth disease. Tubastatin A inhibits the deacetylation of α-tubulin in murine myoblasts.
AZ-1080 (AZD-1080) is an inhibitor of GSK-beta which was developed by AstraZeneca and initially tested in patients with Alzheimer’s disease (phase I). The drug was discontinued for the aforementioned condition, but now it is being investigated as a potential therapy for ovarina cancer and emdometrial carcinoma (basic research).
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



PD-169316 is a selective inhibitor of p38 MAPK. It inhibits p38 MAPK with an IC50 of 89 nM. PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. In an amyloid β (Aβ) rat model of Alzheimer's disease it was demonstrated that caspase-3 and Bax/Bcl-2 ratio, two marks of apoptosis, were significantly decreased in the rats pre-treated with PD169316 intracerebroventricularly.This study suggested the potential neuroprotective role of PD 169316 against the neuronal toxicity induced by Aβ.