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Restrict the search for
unoprostone isopropyl
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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.
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.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
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.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Volpristin is an antibiotic. Information about the current use of this agent is not available.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Famprofazone, a nonsteroidal anti-inflammatory agent, is found in a multi-ingredient medication (Gewodin) used for pain relief. It is available over-the-counter in Taiwan. Famprofazone transforms to methamphetamine (MA) and amphetamine (AM) following administration, which is responsible for the side effects of the drug. For example, famprofazone user might be interpreted as an illicit MA abuser in Taiwan because the user's urine tested positive for MA.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Namirotene [CBS-211A] is a retinoic acid analogue which was undergoing phase II trials with Chauvin in France as 0.02% eye drops for corneal ulcer. It was discontinued later. Namirotene is a synthetic analogue of retinoic acid with differentiation inducing and potential antineoplastic activities. Like other retinoic acid agents, namirotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. When it was associated with 1 alpha,25(OH)2D3, CBS-211A strongly potentiated the 1 alpha,25(OH)2D3-induced inhibition of U937 cell proliferation and caused a dramatic increase in their differentiation toward monocytes/macrophages. The co-inducing effect of CBS-211A was restricted to U937 cells. Our data suggest that CBS-211A may have therapeutic implications in the treatment of certain kinds of myelomonocytic leukemia. CBS-211A also provides an interesting tool to understand the mechanisms involved in the differentiation of myelomonocytic cells.
