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Restrict the search for
unoprostone isopropyl
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Cariporide is a selective sodium-hydrogen antiporter inhibitor patented by a pharmaceutical company Hoechst A.-G. for treatment myocardial ischemia-reperfusion injury. The sodium-hydrogen exchanger is an important player in the pathophysiology of myocardial ischemia-reperfusion injury. The accumulation of hydrogen ions in the myocyte cytosol; during ischemia creates a proton gradient that promotes the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in the cytosol, therefore reduce the infarct size. In clinical trials, Cariporide shows a statistically significant decline in myocardial infarction but increases mortality. Due to the increase in mortality, cariporide did not pass clinical trials.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Nexopamil [LU 49938] is the (S)-enantiomer of a phenylalkylamine derivative and has calcium channel blocking and serotonin2 receptor antagonist activity. Nexopamil's significant antifibrillatory effect during both coronary artery occlusion and abrupt reperfusion is reliably tracked by T-wave alternans magnitude. Because the major component of the protection could be reproduced by blockade of the L-type calcium channel with diltiazem, nexopamil's antiarrhythmic action appears to be due mainly to blockade of this channel. Nexopamil's antiplatelet action through blockade of 5-HT2 receptors may confer additional protection against reperfusion arrhythmias. Nexopamil was discontinued in phase 2 for angina pectoris in European Union.
Status:
Investigational
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
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.
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.
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
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
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
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.
