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

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Showing 31 - 40 of 13993 results

Status:
Investigational
Source:
INN:traboxopine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Traboxopine (EGYT-2509) revealed specific dopamine-antagonistic activity with potentially minimal undesirable side effects. EGYT-2509 behaved as a dopamine receptor antagonist in all functional in vitro biochemical-pharmacological tests (striatal adenylate cyclase, striatal dopamine release, prolactin release from pituitary). The drug exhibited a marked preference for adenylate cyclase-coupled (D1) dopamine receptors, followed by the 3H-spiperone displacing potency at striatal receptors. Traboxopine exerts pharmacological and biochemical effects that seem to be partially similar to those of traditional neuroleptics, except for some undesirable side effects (e.g. cataleptogenic, influencing prolactin level). Traboxopine proved to be diversely influential on the dopaminergic components of the integration of sympathetic output and somato-autonomic reflexes. The apomorphine-induced stereotypy was potentiated by lower, and antagonized by higher doses of EGYT-2509. The in vitro potency of EGYT-2509 to block dopamine-mediated inhibition of prolactin release was weaker by three orders of magnitude than that of haloperidol.
Status:
Investigational
Source:
INN:octapinol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Octapinol, a substance with a low antibacterial activity that was studied to use in gingivitis and in stomatitis. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:nonapyrimine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nonapyrimine is an anticonvulsant, vasodilator.
Status:
Investigational
Source:
INN:raxofelast
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Raxofelast (IRFI 016) is a hydrophilic vitamin E-like antioxidant, that was developed to maximize the antioxidant potency of phenols related to vitamin E. It has been investigated as a mucoactive drug, a type of drug that is used for treatment of respiratory diseases. Also, in diabetic mice, raxofelast was shown to improve wound healing to a level close to that seen in healthy mice, and in another study it improved clinical outcomes in experimental burn wounds. In a rat model of myocardial damage, raxofelast was found to be a useful drug to reduce heart attacks. This compound has good bioavailability and physicochemical properties. No clinical trials have been conducted.
Status:
Investigational
Source:
INN:lucartamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lucartamide is an antisecretory and antiulcer agent.
Status:
Investigational
Source:
INN:libecillide
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Libecillide is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin. A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined libecillide-penicillin treatment. A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients. The overall tolerance of libecillide in allergic patients has been very good. Nevertheless, the major obstacle to a wider general use of libecillide at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin.
Status:
Investigational
Source:
INN:bisbendazole
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Bisbendazole was developed as an anthelmintic agent.
Status:
Investigational
Source:
INN:trecadrine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trecadrine is a beta3-adrenergic agonist. Trecadrine could have normalized the oxygen consumption by the liver, in which other metabolic pathways could be involved. The administration of Trecadrine produced a statistically significant decrease in glucose levels, which is not related to changes in insulin levels. Trecadrine administration to animals significantly inhibited galactose intestinal absorption, which was independently confirmed by additional in-vitro studies and decreased disaccharidase activities. Trecadrine enhance glucose storage in liver, probably through a non-insulin dependent mechanism of action. Trecadrine administration may have a therapeutic potential in disorders associated with hypertriglyceridemia such as obesity and some types of hyperlipidaemias. Trecadrine shows a potent hypoglycaemic effect in the alloxan-induced model of diabetes in rats by decreasing hepatic glucose output and improving muscle glucose uptake.
Status:
Investigational
Source:
INN:saterinone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Saterinone, a dual-action drug combines both alpha-1 blocking vasodilatory property and phosphodiesterase III (PDE III) inhibition--mediated inotropism. PDE III inhibitors are well established in the acute intravenous treatment of patients with decompensated chronic congestive heart failure. Saterinone was demonstrated to be a safe and potent drug on short-term application without major changes in myocardial oxygen consumption. Saterinone was studied in phase II trials in Germany for the treatment of heart failure. However, the development of this drug has been discontinued.
Status:
Investigational
Source:
INN:lixumistat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)