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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Status:
Investigational
Source:
NCT01911676: Phase 2 Interventional Completed Cognitive Impairments Associated With Schizophrenia
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
PF-03463275 is the novel azabicyclic glycine transporter 1 (GlyT1) inhibitor. Ketamine induced hallucinatory-like behaviors that were not reversed by PF-3463275. In contrast, all doses of PF-3463275 alleviated the deficit in spatial working memory induced by ketamine. PF-03463275 causes changes in electroretinogram (ERG) responses in albino rats. There was dose-dependent reduction in the amplitude of the rat ERG oscillatory potentials (OPs) following single subcutaneous administrations of the PF-03463275. Furthermore, the amplitude of OPs was negatively correlated to the concentration of PF-03463275 in the vitreous humor collected from rats immediately following ERG recordings. A slight increase in the amplitude and latency of the a-wave component of the ERG with PF-03463275 treatment was observed. Since the ERG changes occur in our rodent model with PF-03463275 at exposures comparable with those associated with visual disturbance in the clinic, it was proposed that the visual adverse effects reported in healthy volunteers treated with selective GlyT1 inhibitors may represent a retinal class effect. The dose-related GlyT1 occupancy of PF-03463275 is linear. While PF-03463275 did not show evidence of facilitating N-methyl-D-aspartate receptor function in the ketamine assay, it enhanced neuroplasticity in schizophrenia patients. PF-03463275 had been in phase II clinical trial for the treatment of schizophrenia. However, this development was discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mesabolone is a synthetic anabolic androgen.
Status:
Investigational
Source:
NCT01061970: Phase 2 Interventional Completed Hypogonadism
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fispemifene acts via estrogen receptors and has tissue-selective estrogenic and/or antiestrogenic effects – it has antagonist activity in breast tissue and acts as an estrogen agonist in bone. Due to its low estrogenicity in male rats, it might also be applicable for men. Fispemifene exhibits both antiestrogenic and anti-inflammatory action in the prostate. It could be considered as a new therapeutic option in the treatment and prevention of prostatic inflammation. Fispemifene had been in phase II clinical trials for the oral treatment of hypogonadism.
Class (Stereo):
CHEMICAL (RACEMIC)
FLUCETOREX is a substituted amphetamine with anorectic activity.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLUALAMIDE is an antiemetic agent.
Status:
Investigational
Source:
NCT00003667: Phase 2 Interventional Completed Sarcoma
(1998)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (MIXED)
Naminterol [VAL 479], a phenethanolamine derivative, is a β2 adrenoceptor agonist with bronchodilatory properties. The compound was undergoing phase II clinical trials for asthma in Italy.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ridogrel is a dual action drug used for the prevention of systemic thrombo-embolism and as an adjunctive agent to thrombolytic therapy in acute myocardial infarction. Ridogrel, a combined thromboxane synthase inhibitor, and receptor antagonist is used with streptokinase as an adjunctive therapy to reduce the formation and size of blood clots. Blood clots can cause ischemic cardiac events (heart attacks). Ridogrel has the dual property of inhibiting the synthesis of thromboxane and blocking the receptors of thromboxane/prostaglandin/endoperoxides. It has been shown to accelerate the speed of recanalization and to delay or prevent reocclusion during systemic thrombolysis with tissue plasminogen activator (streptokinase). Ridogrel is a more potent antiplatelet agent than aspirin and might offer an advantage over aspirin as an adjunct to thrombolysis in patients suffering from acute myocardial infarction. While aspirin inhibits cyclooxygenase, the enzyme responsible for producing thromboxane, ridogrel inhibits thromboxane synthesis directly. Ridogrel has been studied primarily as an adjunctive agent to thrombolytic therapy in acute MI (AMI). Despite positive results from initial pilot studies, the largest clinical study, the Ridogrel versus Aspirin Patency Trial (RAPT) failed to demonstrate any advantage with this agent over aspirin. In the study of 907 patients with AMI, there was no difference in the primary endpoint of infarct vessel patency rate between those randomized to ridogrel (72.2%) or aspirin (75.5%). Various mechanisms are likely responsible for the results seen with ridogrel in clinical trials, including potentially ineffective thromboxane receptor inhibition with the concentrations of ridogrel used in human studies. As such, there currently are no clinical indications for preferential use of ridogrel over aspirin.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Licofelone (ML 3000) is a pyrrolizine derivative originally discovered by Merckle GmbH and developed by EuroAllaince with a unique pharmacological profile, which comprises optimal gastrointestinal tolerability and high analgesic and anti-inflammatory activity. These effects are due to balanced and selective inhibition of both cyclo-oxygenase and 5-lipoxygenase. Inhibition of 5-lipoxygenase may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs, which only inhibit cyclooxygenase. Licofelone also has antipyretic and antiaggregatory properties. Clinical and preclinical trials were also undertaken for osteoarthritis, rheumatoid arthritis, asthma, pain and inflammation. However, development for these indications appear to have been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Elsibucol (AGI-1096) is a phenolic intracellular antioxidant with anti-inflammatory and antiproliferative properties. In vitro, elsibucol inhibited the inducible expression of vascular cell adhesion molecule (VCAM)-1, E-selectin, and monocyte chemoattractant protein (MCP)-1 in endothelial cells and tumor necrosis factor (TNF)-alpha and interleukin (IL)-1beta secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells. It also inhibited serum-stimulated proliferation of aortic smooth-muscle cells. In vivo, elsibucol demonstrated anti-inflammatory properties in a murine delayed-type hypersensitivity model. In hypercholesterolemic animals, elsibucol inhibits atherosclerosis and preserves endothelial healing following arterial injury. Elsibucol development for the prevention of transplant rejection has been discontinued.