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

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Showing 30861 - 30870 of 34777 results

Fostriecin, an antitumor antibiotic produced by Streptomyces pulveraceus, is a strong inhibitor of serine/threonine protein phosphatases type 2A and type 4, and inhibits the catalytic activity of partially purified Topo II (type II topoisomerase) in a non-competitive manner.
Status:
Investigational
Source:
INN:xorphanol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Xorphanol (also known as TR5379M) is a full κ-opioid receptor agonist and is a partial agonist at μ opioid receptor. Clinically, xorphanol was studied as an orally active analgesic that provided effective pain relief but showed low physical dependence liability. Further development of this drug was discontinued.
Status:
Investigational
Source:
INN:cizolirtine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.
Status:
Investigational
Source:
NCT00230074: Phase 2 Interventional Completed Amyotrophic Lateral Sclerosis
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Omigapil (CGP 3466 or TCH346) is a structurally related analog of R-(-)-deprenyl that exhibits virtually no monoamine oxidase type B inhibiting activity but is neuroprotective in the picomolar concentration range. It binds to glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and at subnanomolar concentrations prevent the S-nitrosylation of GAPDH, inhibit GAPDH-Siah binding and prevent the nuclear translocation of GAPDH. Omigapil demonstrated promising potential in the treatment of Parkinson's disease and motoneuron disease in animal models, however, it did not show efficacy in clinical trials. Omigapil is in development for the treatment of congenital muscular dystrophy.
Status:
Investigational
Source:
NCT00259870: Phase 2 Interventional Completed Schizophrenia
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00831103: Phase 2 Interventional Completed Herpes Zoster
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Omaciclovir (previously known as H2G), a cyclic guanosine analog that is structurally similar to acyclovir and was in clinical development for the treatment of herpesvirus infections. This drug acted against varicella-zoster virus (VZV), by the formation of high concentrations of relatively stable H2G-triphosphate, which is a potent inhibitor of the viral DNA polymerases. However, further development of this drug was discontinued.
Status:
Investigational
Source:
INN:pentiapine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pentiapine is a dopamine release inhibitor. It is a tranquiliser. Pentiapine produces a dose-dependent decrease in spontaneous motor activity and blocks the morphineinduced hyperactivity. Moreover, this drug in itself has no effect on place conditioning but blocks the acquisition of morphine-induced conditioned place preference.
Ruboxistaurin is an orally bioavailable, selective, potent inhibitor of protein kinase C β developed for treating diabetic retinopathy. In vitro and in vivo non-clinical models have demonstrated that Ruboxistaurin decreases PKC β activity and ameliorates many of the effects of PKC β on pathologic processes in the retina. Ruboxistaurin prevents the slowing of retinal blood flow that is observed by fluorescein video angiography in the eyes of diabetic rats. It is also reported to cause regression of retinal neovascularization produced by laser-induced major branch vein occlusions in a porcine model. Ruboxistaurin positively affected the diabetes-induced retinal blood flow abnormalities in a Phase Ib study in diabetic patients. Ruboxistaurin is in phase III clinical trials for the treatment of diabetic nephropathy and diabetic macular edema. Eli Lilly had submitted Ruboxistaurin for approval in the US and the EU; however, the company subsequently discontinued development as it was unable to demonstrate sufficient efficacy
Status:
Investigational
Source:
INN:gantacurium chloride [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Gantacurium (GW280430A) is an ultrashort-acting neuromuscular blocking agent with a rapid onset and a wide safety margin, and is one of the most recent neuromuscular blocking agents that have shown potential for clinical application. It is an asymmetric enantiomeric isoquinolinium diester of chlorofumaric acid. The neuromuscular properties of gantacurium (such as spontaneous recovery of a neuromuscular block induced by the compound) were comparable with the depolarizing neuromuscular blocking drug succinylcholine, but without the unwanted side effects of this depolarizing neuromuscular blocking drug. Gantacurium is, due to its unique metabolism, rapidly inactivated by cysteine adduction and alkaline hydrolysis.
Status:
Investigational
Source:
NCT01452373: Phase 3 Interventional Completed Vasomotor Symptoms
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Acolbifene, the active metabolite of EM-800, was identified as a pure antagonist that acts on both activation domains of the ERs. It is in Phase III clinical trials for the prevention of breast cancer and vasomotor symptoms (Hot flush) in postmenopausal women. Most commonly reported adverse events included irregular menses, leg/muscle cramps, diarrhea, and hot flashes. No serious adverse events were reported.

Showing 30861 - 30870 of 34777 results