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

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Showing 941 - 950 of 12521 results

Status:
Investigational
Source:
INN:irolapride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

IROLAPRIDE is an antiemetic agent.
Status:
Investigational
Source:
INN:droloxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Status:
Investigational
Source:
INN:etacepride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Etacepride is a neuroleptic and antiemetic agent.
Status:
Investigational
Source:
INN:lodazecar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lodazecar is a benzodiazepine derivative, which does not bind to the brain benzodiazepine receptor. The drug shares some similarity in tertiary structure with the cholesterol molecule. Oral administration of lodazecar in the cholesterol-fed rat is associated with significant changes in plasma lipoproteins and in key enzymes controlling hepatic cholesterol metabolism. In human the treatment reduced both the fractional and the absolute cholesterol absorption and increased fecal neutral sterol excretion by about 50%, serum plant sterol levels were reduced, most probably because of diminished sterol absorption. Biliary cholesterol secretion was unchanged.
Status:
Investigational
Source:
INN:coumazoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Coumazoline is a vasoconstrictor developed as a nasal decongestant by a French corporation Labez. Intravenous administration of the compound to dogs lead to a marked and prolonged drop in the temperature of the gingival mucosa. In rats, coumazoline caused slowing of the dye diffusion on the surface of the skin. The compound did not influence the ciliary motility, as was measured on an isolated guinea pig trachea.
Status:
Investigational
Source:
INN:bervastatin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Bervastatin (also known as LS 2904), a synthetic HMG-CoA reductase inhibitor that was developed for the treatment of hyperlipidemia. However, information about further development is not available.
Status:
Investigational
Source:
INN:benzethidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Benzethidine an opioid analgesic that was forbidden for use.
Status:
Investigational
Source:
INN:binospirone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Binospirone (MDL-73,005-EF) acts as a potent, highly selective 5-HT1A ligand: as an antagonist at postsynaptic 5-HT1A receptors and also acts as a highly efficacious partial agonist at somatodendritic autoreceptors. Experiments on rodents have shown, that it also possesses anxiolytic properties.
Status:
Investigational
Source:
INN:isosulpride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

ISOSULPRIDE, a benzamide derivative, is an atypical neuroleptic.
Status:
Investigational
Source:
INN:panidazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Panidazole, an antiprotozoal agent that was studied in patients for the treatment of intestinal amoebiasis and vaginal trichomoniasis. However, information about the further development of this drug is not available.