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

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Showing 391 - 400 of 993 results

Oroxylin A is a flavonoid compound, one of the main components extracted from Scutellariae radix. It possess a broad spectrum of pharmacological effects, especially anti-cancer, anti-inflammatory and neuroprotective activity. Oroxylin A inactivated HIF1α and reprogrammed fatty acid metabolism of HCT116 cells, decreasing intracellular fatty acid level and enhancing fatty acid oxidation. Oroxylin A improves attention-deficit hyperactivity disorder-like behaviors in spontaneously hypertensive rats via enhancement of dopamine neurotransmission and not modulation of GABA pathway as previously reported. Importantly, the present study indicates the potential therapeutic value of oroxylin A in the treatment of attention-deficit hyperactivity disorder. Both in vitro and in vivo study showed that oroxylin A possesses low toxicity, but the field was just limited in cancer research.
Canadine (tetrahydroberberine,THB) is an isoquinoline alkaloid (5,8,13,13a-tetrahydro-9,10-dimethoxy-6H-benzo[g]-1,3-benzodioxolo[5,6-a]quinolizine) from Corydalis tuber, it has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (i.e., 5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4). Canadine enhances gastrointestinal motor function. THB, with D(2) receptor antagonist and 5-HT(1A) receptor agonist properties, has significant potential as a therapeutic for treatment of functional dyspepsia. THB is a potent inhibitor of platelet aggregation in vitro and in vivo and is a promising antithrombotic drug.
Alpha-ergocryptine is a component of the ergotoxine complex; it is the main ergot alkaloid of Japanese & South American wid grasses. Alpha-ergocryptine is an agonist at the D2 dopamine receptor. Alpha-ergocryptine effectively decreases intraocular pressure in the alpha-chymotrypsin-induced model of ocular hypertension.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

P-88-8991, (-)- is a metabolite of Iloperidone. It has functional affinity for noradrenergic, dopaminergic and serotoninergic receptors. Humans produce only one enantiomer stereospecifically following administration of Iloperidone. Preclinical studies revealed that P-88-8991, (-)- might be useful for the treatment of psychotic disorders such as schizophrenia and bipolar disorders.
P-88-8991, (+)- is a metabolite of Iloperidone. It has functional affinity for noradrenergic, dopaminergic and serotoninergic receptors. Humans produce only one enantiomer stereospecifically following administration of Iloperidone. Preclinical studies revealed that P-88-8991, (+)- might be useful for the treatment of psychotic disorders such as schizophrenia and bipolar disorders.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Saikosaponin A is a triterpene saponin found in Bupleurum that exhibits anti-inflammatory, analgesic, neuromodulatory, anticancer, and immunosuppressive activities. Saikosaponin A decreases production of TNF-α, IL-1β, and IL-2 and increases mechanical withdrawal thresholds and thermal withdrawal thresholds in animal models of chronic constructive injury. Saikosaponin A also decreases self-administration of cocaine and morphine. In colon carcinoma cells, saikosaponin A causes activation of caspases 2, 3, 8, and 9 and PARP, induces apoptosis, and decreases expression of Bcl-2 and XIAP. Additionally, this compound inhibits the proliferation and activation of ConA-treated T cells, inducing G0/G1 phase cell cycle arrest and decreasing expression of TNF-α, IL-2, and IFN-γ.