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

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Showing 51 - 60 of 232 results

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.
3-Methoxytyramine (3-MT) is a human trace amine that occurs as a metabolite of the neurotransmitter dopamine. It has been shown to act as an agonist of human TAAR1, and an inhibitor of mitochondrial respiration. 3-MT has garnered research interest for its potential links and implications to Parkinson's disease and other Neurological disorders.
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.
Bay 65-1942 free base (Bay 65-1942) is a selective inhibitor of IKKβ with IC50 value of 10 uM and Ki value of 2 nM. Bay 65-1942 has been reported to provide cardioprotection through specific suppression of NF-κB signaling. It also afforded potent neuroprotection against LPS-induced neurodegeneration through selective inhibition of NF-kappaB activation and may be of potential benefit in the treatment of PD.
P7C3 is a chemical compound belongs to a class of proneurogenic compounds that are potential nicotinamide phosphoribosyltransferase (NAMPT) activators, and might shed light on future drug development in neurogenesis restoration. This compound protects newborn neurons in the dentate gyrus by mitigating cell death. Also enhances learning and memory in aged rats. In addition on animal models was shown, that P7C3 is sufficient to restore the neurogenic deficits observed in the Ts65Dn mouse model of Down Syndrome, and also was discovered, that P7C3 might provide a basis for the discovery and optimization of pharmacologic agents for the treatment of amyotrophic lateral sclerosis (ALS) and for the treatment of patients with Parkinson disease (PD).
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



GSK 0660 is a selective PPARdelta antagonist. The compound reduced psoriasis-like changes in a preclinical model and demonstrated neuroprotection in an in vitro model of Parkinson’s disease. When given alone GSK 0660 exhibits inverse agonist effects.
Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia
AS601245 (1,3-benzothiazol-2-yl (2-{[2-(3-pyridinyl) ethyl] amino}-4 pyrimidinyl) acetonitrile) is a potent and selective JNK inhibitor developed by Applied Research Systems ARS Holding as promising neuroprotective agent. In vitro AS601245 is a potent and cell permeable ATP competitive JNK inhibitor, which has been shown to inhibit the JNK signaling pathway, promotes cell survival after cerebral ischemia. AS601245 and clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells. AS601245 is a new potent adenosine triphosphate-competitive JNK inhibitor, provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia and is also neuroprotective in rats after focal cerebral ischemia. The ischemia-induced phospho-c-Jun expression is attenuated by AS601245, providing a mechanism through which AS601245 blocks the loss of neuronal cells.
SKF83959 is a benzodiazepine derivative which acts as an agonist of D1 receptor. Activation of D1 receptors by SKF83959 fails to stimulate adenylyl cyclase and inhibits the stimulation of adenylyl cyclase induced by dopamine but stimulates phosphatidylinositol 4,5-biphosphate hydrolysis in membranes of frontal cortex. SKF83959 was identified as a specific agonist for the heteromer D1/D2 complex. SKF83959 elicit anti-parkinsonism effects in monkeys and rodents. In lower concentrations, SKF83959 inhibits serotonin, norepinephrine and dopamine transporters and is an allosteric regulator of sigma 1 receptor. The compound has demonstrated activity in a preclinical model of depression.
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.