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

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Showing 1941 - 1950 of 2596 results

Mevastatin (compactin or ML-236B) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This drug induces apoptosis and arrest of cancer cells in G1 phase. Therapeutic effects of mevastatin on serum level of lipoproteins and unbiquinone-10 in patients with familial hypercholesterolemia were investigated. However, that study was discontinued. In addition, mevastatin was investigated for the treatment of melanoma. It was suggested, that mevastatin was unlikely to prevent melanoma at standard doses. However, higher doses could have a role to play in adjuvant therapy by inhibiting growth and invasion of melanoma cells. Also was revealed, that mevastatin increased histone deacetylase inhibitor, LBH589-induced cell death in triple-negative breast cancer (TNBC) cells.
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
INN:selfotel [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



(+)-selfotel ((+)-CGS-19755) is an enantiomer of selfotel, a competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptors. The inhibition of NMDA-evoked ACh release from rat striatal slices is stereospecific, with the (+)-enantiomer less potent than the (-)-enantiomer.
Status:
Investigational
Source:
NCT04083339: Phase 3 Interventional Active, not recruiting Diabetic Cardiomyopathies
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Aldose reductase-IN-1 is an inhibitor of aldose reductase
Status:
Investigational
Source:
INN:dextiopronin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

There is a few information about DEXTIOPRONIN. It is an R isomer of N-(2-Mercaptopropionyl)-glycine (MPG), a synthetic aminothiol antioxidant, that is used in the treatment of cystinuria, rheumatoid arthritis, liver and skin disorders.
Mevastatin (compactin or ML-236B) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This drug induces apoptosis and arrest of cancer cells in G1 phase. Therapeutic effects of mevastatin on serum level of lipoproteins and unbiquinone-10 in patients with familial hypercholesterolemia were investigated. However, that study was discontinued. In addition, mevastatin was investigated for the treatment of melanoma. It was suggested, that mevastatin was unlikely to prevent melanoma at standard doses. However, higher doses could have a role to play in adjuvant therapy by inhibiting growth and invasion of melanoma cells. Also was revealed, that mevastatin increased histone deacetylase inhibitor, LBH589-induced cell death in triple-negative breast cancer (TNBC) cells.
Status:
Investigational
Source:
INN:dexlofexidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dexlofexidine is an isomer “+“ of lofexidine, which is agonist of alpha 2-adrenoceptor, but in 10 times less potent than the other isomer, levlofexidine.
Status:
Investigational
Source:
INN:propoxate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Propoxate (R7464) is a potent anesthetic agent in cold-blooded vertebrates, which has never been marked and has never been used on humans.
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
NCT00942656: Not Applicable Interventional Completed Cardiovascular Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Rumenic acid is the major conjugated linoleic acid (CLA), probably because of successive desaturation and chain elongation and can be considered as the principal dietary form. In experiments on rodents was shown that rumenic acid possessed the protective effect against colitis, which was associated with the activation of the Nrf2 pathway.

Showing 1941 - 1950 of 2596 results