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

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Showing 971 - 980 of 13268 results

Status:
Investigational
Source:
INN:linetastine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Linetastine has anti-inflammatory and anticarcinogenic effects. It is a potent inhibitor of 5-lipoxygenase. It also inhibits histamine release and epidermal cyclooxygenase activity. It also markedly inhibited TPA-stimulated leukotriene B4 formation, but inhibited formation of prostaglandin E2, a cyclooxygenase product, only slightly. This suggested that neither cyclooxygenase inhibition nor antihistaminic activity were essential to the anti-inflammatory action of linetastine. The anti-inflammatory effect of oral linetastine is probably due to 5-lipoxygenase inhibition. Oral administration of linetastine almost completely suppressed Cyp1a1 mRNA levels in mouse epidermis induced by a topical application of 3-methylcholanthrene or benzo[a]pyrene to mouse skin. Oral administration of linetastine inhibited DMBA-caused skin tumor initiation at least in part by inhibiting Cyp1a1 mRNA induction and epidermal aryl hydrocarbon hydroxylase activity. Linetastine had been in phase II clinical trial for the treatment of allergic rhinitis. However, this study was discontinued.
Status:
Investigational
Source:
INN:octastine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octasine is an antihistamine agent that has never been marketed.
Status:
Investigational
Source:
INN:diarbarone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diarbarone is the anticoagulant.
Status:
Investigational
Source:
INN:devapamil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

In the early stages of testing was shown that it is about 4 times more potent than gallopamil and 12 times more potent than verapamil in its effects on smooth muscle tone and labeled calcium uptake.
Status:
Investigational
Source:
INN:dexefaroxan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Dexefaroxan is a selective alpha 2-adrenergic receptor antagonist. Вexefaroxan improved TgCRND8 (protein-transgenic mouse model of Alzheimer's disease) behavioral phenotypes and increased BDNF mRNA expression without affecting amyloid-β peptide levels. Dexefaroxan treatment also enhanced the number and complexity of the dendritic arborizations of polysialated neural cell adhesion molecule-positive neurons. The trophic effects of dexefaroxan on newborn cells might involve an increase in brain-derived neurotrophic factor, which was upregulated in afferent noradrenergic fiber projection areas and in neurons in the granule cell layer. By promoting the survival of new endogenously formed neurons, dexefaroxan treatment represents a potential therapeutic strategy for maintaining adult neurogenesis in neurodegenerative conditions, such as Alzheimer's disease, that affect the hippocampus. Dexefaroxan increases neuron survival in the olfactory bulb of the adult rat in vivo, putatively as a result of reducing the apoptotic fate of telencephalic stem cell progenies.
Status:
Investigational
Source:
INN:elgodipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Elgodipine (IQB-875, CAS 119413-55-7) is a phenyldihydropyridine derivative acting as a calcium channel antagonist. Elgodipine inhibited both T- and L-type calcium channels in a concentration-dependent manner. Elgodipine was in clinical trials for the treatment of cardiovascular diseases however its development has been discontinued.
Status:
Investigational
Source:
INN:dipiproverine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dipiproverine is the spasmolytic agent. It was used as anticholinergic drug.
Status:
Investigational
Source:
INN:fenetradil
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

FENETRADIL is a coronary dilator.
Status:
Investigational
Source:
INN:thiotetrabarbital
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Thiotetrabarbital is a thiobarbituric acid derivative patented by "Centre national de la recherche scientifique" as a short-acting anesthetic agent useful in veterinary medicine.
Status:
Investigational
Source:
NCT00460278: Phase 1 Interventional Suspended Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

XL418 is a dual protein kinase B (Akt) and ribosomal protein S6 Kinase (p70 S6K) inhibitor that also acts as an ATP-pocket binder with potential antineoplastic activity. XL418 was involved in phase I clinical trial in patients with solid tumors, however, in Dec 2007, this study was discontinued, due to low drug exposure.