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

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Showing 101 - 110 of 1320 results

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

Class (Stereo):
CHEMICAL (RACEMIC)

Emopamil is a phenylalkylamine calcium antagonist. Emopamil has optically active stereoisomers. Emopamil enhanced the postischemic restoration of high-energy phosphate levels. The racemic mixture and the (-)-enantiomer of emopamil caused similar metabolic changes while (+)-enantiomer of emopamil proved to be ineffective. Emopamil is able to reverse multi-drug resistance in human KB cell lines. No differences in reversing potency were observed between emopamil (R)-isomers, (L)-isomers and the racemic form. There is a pharmacological relationship between sigma1-binding site and the mammalian sterol C8-C7 isomerase which is identical with the emopamil binding protein.
Status:
Investigational
Source:
INN:dazolicine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dazolicine is an anti-arrhythmic compound, developed by the German company Roechlingsche Eisen & Stahl. In patients with various types of arrhythmia, after i.v. injection the drug proved to have very strong antiarrhythmic potency and rather a low incidence of side effects. After oral treatment, ectopic beats were eliminated in only 4 of 10 patients.
Status:
Investigational
Source:
NCT00052117: Phase 2 Interventional Completed HIV Infections
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Capravirine (S-1153, AG1549) is a 1,2,4,5-tetrasubstituted imidazole derivative patented by pharmaceutical company Shionogi as specific inhibitors of HIV-​1 reverse transcriptase. However, safety and efficacy studies showed that Capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb.
Status:
Investigational
Source:
INN:dicirenone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dicirenone is an aldosterone antagonist. It is used as a hypotensive agent. Dicirenone inhibited the effects of aldosterone on urinary K(+):Na(+) ratios and the binding of [(3)H]aldosterone to renal cytoplasmic and nuclear receptors. Dicirenone blocked the action of aldosterone on Na-K ATPase. Cytoplasmic binding of [(3)H]aldosterone and dicirenone was similar in magnitude and involved the same set of sites. It had no effect on adrenal steroidogenesis.
Status:
Investigational
Source:
INN:inicarone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Inicarone is benzofuryl derivative with potent antifibrinolytic activity.
Status:
Investigational
Source:
NCT00002357: Phase 2 Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Talviraline (HBY 097) was developed as a nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (NNRTI) for the treatment of HIV Infections. Talviraline participated in a phase II clinical trial. It was found that the drug caused pronounced acute suppression of HIV-1 replication both in combination with zidovudine and alone. However, further development of the drug has been discontinued.
Status:
Investigational
Source:
INN:mivotilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mivotilate is an orally active hepatoprotective agent for the treatment of liver cirrhosis and hepatitis-B infection. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. The low oral bioavailability of Mivotilate in rats could be primarily attributed to poor absorption and considerable hepatic and gastrointestinal first-pass effects. The thermal reversible microemulsion system of YH439 greatly enhances the bioavailability of YH439 after oral administration. Mivotilate prevents mutagenesis caused by agents such as benzopyrene and reduces skin tumours induced by these agents.
Status:
Investigational
Source:
INN:befiperide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Befiperide, a non-dopaminolytic serotonin 1 receptor agonist, was a neuroleptic for psychotic disorders. However, further studies for this drug were discontinued.
Status:
Investigational
Source:
INN:lemildipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.
Status:
Investigational
Source:
INN:volpristin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Volpristin is an antibiotic. Information about the current use of this agent is not available.