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

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Showing 421 - 430 of 13408 results

Status:
Investigational
Source:
INN:mesocarb [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Mesocarb (sydnocarb or 3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychomotor stimulant N-alkylated amphetamine derivative. Mesocarb is a selective inhibitor of dopamine uptake, it potently blocks dopamine transporter. It is very likely that mesocarb is being used by drug addicts. Mesocarb is included in the World Anti-Doping Agency’s list of substances and methods that are prohibited in sports. It is used in Russia for the treatment of a variety of neuropsychiatric comorbidities.
Status:
Investigational
Source:
INN:nepicastat
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.
Status:
Investigational
Source:
INN:fluorescein lisicol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluorescein Lisicol (NRL972) is a fluorescent-labelled bile acid analog that is used as an investigational marker for liver function, specifically hepatic biliary transporter function. Fluorescein Lisicol has been used in trials investigating the pharmacokinetics of hepatic cirrhosis, viral hepatitis, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.
Status:
Investigational
Source:
INN:brasofensine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

NeuroSearch was developing brasofensine (or NS 2214), an oral dopamine reuptake inhibitor for the treatment of Parkinson's disease. Brasofensine successfully passed phase II clinical trial in patients with Parkinson's disease, The drug was safe and well tolerated. However, NeuroSearch discontinued the development of the drug because of the cis-anti isomerization of the 2α-methyloxime group of brasofensine in favor of NS 2230.
Status:
Investigational
Source:
INN:cefetrizole
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefetrizole is aminocephalosporanic acid derivative with broad antibacterial activity against penicillin-resistant strains patented by Spanish pharmaceutical company Ferrer Internacional S. A.
Status:
Investigational
Source:
INN:cefazaflur
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefazaflur (INN) is a semisynthetic first-generation cephalosporin antibiotic patented by Smithkline Corp. For treatment of bacterial infections.
Status:
Investigational
Source:
INN:cefclidine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefclidin is a fourth-generation cephalosporin antibiotic effective against a clinical strain of Citrobacter freundii. The affinity of cefclidin for the β-lactamase isolated from these mutants was lower than that of ceftazidime, and the kinetic parameters of enzymatic hydrolysis showed that cefclidin was hydrolyzed more slowly at a low concentration than was ceftazidime. It is suggested that the high activity of cefclidin against strains derepressed for β-lactamase plays a major role in the absence of emergence of resistant mutants.
Taselisib (GDC-0032) is an highly selective small-molecule inhibitor of phosphatidylinositol 3-kinase (PI3K) p110-α isoform (PIK3CA). Taselisib is designed to bind to the ATP-binding pocket of PIK3CA to potentially prevent subsequent downstream signaling. Taselisib caused a strong differential growth inhibition in carcinoma cells harbored oncogenic PIK3CA mutations. In preclinical studies, taselisib induced growth inhibition in PIK3CA-mutant xenograft mouse models. Genentech (a Roche subsidiary) is developing taselib primarily for the treatment of solid tumours.
Status:
Investigational
Source:
INN:camobucol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Camobucol is a novel, orally active, phenolic antioxidant and anti-inflammatory compound with antirheumatic properties. Camobucol exhibited potent antioxidant activity toward lipid peroxides in vitro and displayed enhanced cellular uptake relative to a structurally related drug, probucol. This resulted in potent inhibition of cellular levels of reactive oxygen species in multiple cell types. Camobucol selectively inhibited tumor necrosis factor (TNF)-alpha-inducible levels of the redox-sensitive genes, vascular cell adhesion molecule-1 and monocyte chemoattractant protein-1, with less inhibition of E-selectin, and no effect on intracellular adhesion molecule-1 expression in endothelial cells. In addition, Camobucol inhibited cytokine-induced levels of monocyte chemoattractant protein-1, interleukin (IL)-6, and IL-8 from endothelial cells and human fibroblast-like synoviocytes as well as lipopolysaccharide-induced release of TNF-alpha, IL-1beta, and IL-6 from human peripheral blood mononuclear cells. Camobucol did not inhibit TNF-alpha-induced nuclear translocation of nuclear factor of the kappa-enhancer in B cells (NF-kappaB), suggesting that the mechanism of action is independent of this redox-sensitive transcription factor.
Status:
Investigational
Source:
INN:propetandrol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Propetandrol is a pregnanediol derivative patented by Schering A.-G. as long-acting anabolic androgen. Propetandrol is potent in the prevention of tissue calcification and skeletal lesions.