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

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Showing 11 - 20 of 206 results

Status:
Investigational
Source:
NCT02745730: Not Applicable Interventional Completed Pleasure
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


D-Psicose (akaD-allulose) is a low energy monosaccharide found throughout nature in small quantities. t is a c-3 epimer of D-fructose and has 50% the sweetness of sucrose. Possible health benefits include improved insulin resistance, antioxidant enhancement and formation, and hypoglycemic controls. The use US-FDA lists psicose as generally recognized as safe (GRAS) and has approved its use as a food additive in a wide variety of products. Psicose is not generally metabolized and does not raise blood sugar levels above baseline after consumption. In addition, to use as a low-calorie sweetener, psicose has also been formally investigated as a dietary supplement to control obesity and pre-diabetic insulin insensitivities. Furthermore, D-psicose has shown the ability to inhibit the proliferation of ovarian cancer cells in vitro.
Sodium taurodeoxycholate is a bile salt-related, anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. It is formed by the conjugation of ursodeoxycholic acid (UDCA) with taurine. Sodium taurodeoxycholate and ursodeoxycholic acid are major constituents of black bear bile, which has been used in traditional Chinese medicine for thousands of years. Bear bile was historically employed to treat a number of diseases including jaundice, summer diarrhea, abdominal pain due to hepatobiliary diseases and gastric malfunction, biliary ascariasis, infectious skin diseases, the common cold, intestinal worms, and inflammation of the throat. Sodium taurodeoxycholate has been shown to inhibit apoptosis by modulating mitochondrial membrane perturbation and pore formation, B cell lymphoma 2 (Bcl-2)-associated protein X (BAX) translocation, cytochrome c release, and caspase activation. Sodium taurodeoxycholate inhibits amyloid beta (Ab)-induced apoptosis and attenuates the endoplasmic reticulum (ER) stress, which are thought to be key components of the pathological process in certain diseases. In clinical studies, Sodium taurodeoxycholate is shown to be very safe with oral administration of 1500 mg/day for up to 6 months. In a more recent clinical study, a dose of 1750 mg/day for up to 4 weeks was well tolerated in healthy obese persons. One of the major adverse effects of Sodium taurodeoxycholate is diarrhea. Based on the related information from ursodeoxycholic acid, other gastrointestinal side effects are possible including abdominal pain, flatulence, nausea, dyspepsia, and anorexia.
Status:
Investigational
Source:
NCT01811303: Not Applicable Interventional Completed Reduction of Post-prandial Glycaemic Response
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



D-Fagomine (1,2-dideoxynojirimycin) is a six-membered ring iminocyclitol that was first isolated from seeds of buckwheat (Fagopyrum sculentum Moench, Polygonaceae) and is also present in other plant sources such as mulberry (Morus Alba, Moraceae) leaves and gogi (Lycium chinense) roots. D-fagomine is present in common buckwheat-based foodstuffs in amounts ranging from 1 to 25 mg/kg or mg/L, it is stable during boiling, baking, frying and fermentation, and it is biosynthesised upon sprouting. The estimated total intake of D-fagomine resulting from a diet that includes such foodstuffs would be between 3 and 17 mg per day (mean for both genders; range from P5 to P95). In animal studies D-Fagomine lowers postprandial blood glucose. D-fagomine agglutinated Enterobacteriaceae (Escherichia coli, Salmonella enterica serovar Typhimurium), while it did not show this effect on Bifidobacterium spp. or Lactobacillus spp. D-fagomine significantly inhibited the adhesion of Enterobacteriaceae and promoted the adhesion of Lactobacillus acidophilus to intestinal mucosa. D-Fagomine did not show any effect on bacterial cell viability. D-fagomine may be used as a dietary ingredient or functional food component to reduce the health risks associated with an excessive intake of fast-digestible carbohydrates, or an excess of potentially pathogenic bacteria.
Status:
Investigational
Source:
NCT01217905: Phase 1 Interventional Completed Type 2 Diabetes
(2010)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



AZD-7687 is a potent inhibitor of Diacylglycerol O-acyltransferase 1 (DGAT1) which was developed by AstraZeneca for the treatment obesity and type 2 diabetes mellitus. AZD-7687 reached phase I of clinical trials, but was discontinued by unknown reasons.
Cobalt protoporphyrin (CoPP) is a potent HO-1 inducer and generally known to be an antioxidant in various cell types. CoPP has been shown to downregulate various cytochrome P450 isoforms, and various mechanisms of action have been attributed to its ability to induced HO- 1. It has also been used to promote endogenous carbon dioxide (CO) generation and protect against myocardial infarction in vivo. CoPP also participated in regulating the inflammatory response in CNS which mainly suppressed inflammatory component. It has been demonstrated that CoPP reduced LPS/Interleukin 13 (IL-13)-induced microglial death.
Status:
Investigational
Source:
INN:ibrolipim [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lipoprotein lipase (LPL) is a rate-limiting enzyme that hydrolyzes circulating triglyceride-rich lipoproteins such as very low-density lipoproteins and chylomicrons. Otsuka Pharmaceutical Factory, Inc. synthesized the LPL activator NO-1886 (ibrolipim, [4-(4-bromo-2-cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl ester, CAS 133208-93-2). NO-1886 increased LPL mRNA and LPL activity in adipose tissue, myocardium and skeletal muscle, resulting in an elevation of postheparin plasma LPL activity and LPL mass. It was discovered, that this agent has a potentially beneficial for the treatment of hypertriglyceridemia, hypo-HDL cholesterolemia, and protection from atherosclerosis. In addition, this agent may be used in the treatment of obesity and obesity-linked health problems in postmenopausal women.
Status:
Investigational
Source:
NCT00092872: Phase 3 Interventional Completed Obesity
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MK-0557, trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro [6 azaisobenzofuran-1(3H),10-cyclohexane]-40-carboxamide, is an orally available Neuropeptide Y (NPY5) receptor antagonist. MK-0557 was studied in the clinical trials for the treatment of obesity, however, MK-0557 did not significantly increase the weight loss efficacy. MK-0557 safety and effectiveness were studied in a trial for the treatment of cognitive impairment in patients with schizophrenia. It seems MK-0557 development was discontinued.
DOV 216,303 [(+/-)-1-(3, 4-dichlorophenyl)-3-azabicyclo-[3.1.0] hexane hydrochloride] is the prototype of a class of compounds referred to as "triple" reuptake inhibitors. DOV 216,303 were licensed from Wyeth in 1998. This compound inhibits the reuptake of norepinephrine (NE), serotonin (5-HT), and dopamine (DA), the three neurotransmitters most closely linked to major depressive disorder. In August 2004, DOV entered into a development and commercialization partnership for the triple reuptake inhibitors (DOV 21,947 and DOV 216,303) with Merck for depression.
Status:
Investigational
Source:
NCT00358930: Phase 2 Interventional Completed Head and Neck Neoplasms
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lapachone (aka beta-Lapachone) is an ortho naphthoquinone, originally isolated from a tree whose extract has been used medicinally for centuries. It has garnered interest as a potential therapeutic or lead compound against a number of disease conditions including cancers, and blindness due to retinopathy of prematurity. It is lethal to a number of cancer cell types at micromolar concentrations, and it is capable of enhancing the efficacy of radiation therapies against cultured cells. A number of clinical trials have been conducted.
Status:
Investigational
Source:
INN:metamfepramone [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) was synthesized by various routes in the 1930s and 1940s and clinically evaluated as anorectic as well as a treatment of hypotension and symptoms of the common cold. It was widely used for the treatment of the common cold or hypotonic conditions. Due to its stimulating properties and its rapid metabolism resulting in major degradation products such as methylpseudoephedrine and methcathinone, it has been considered relevant for doping controls by the World Anti-Doping Agency (WADA). Metamfepramone was marketed as an appetite suppressant, but was made illegal in 2006.

Showing 11 - 20 of 206 results