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

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Showing 91 - 100 of 1197 results

Status:
Investigational
Source:
INN:properidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.
Status:
Investigational
Source:
INN:devapamil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

In the early stages of testing was shown that it is about 4 times more potent than gallopamil and 12 times more potent than verapamil in its effects on smooth muscle tone and labeled calcium uptake.
Status:
Investigational
Source:
INN:epervudine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Epervudine (5-isopropyl-2'-deoxyuridine) is an antiviral compound. The antiviral effect of epervudine on herpes viruses (HSV-1 and HSV-2) is based on the sensitivity of virus DNA to nucleases due to epervudine incorporation into the virus DNA and the resulting change in DNA conformation. Virus selectivity is based on virus induced thymidine kinase activity and on HSV induction of polymerase enzymes catalyzing the incorporation. Epervudine (HEVIZOS) ointment is used to treat herpetic skin infections.
Status:
Investigational
Source:
INN:elgodipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Elgodipine (IQB-875, CAS 119413-55-7) is a phenyldihydropyridine derivative acting as a calcium channel antagonist. Elgodipine inhibited both T- and L-type calcium channels in a concentration-dependent manner. Elgodipine was in clinical trials for the treatment of cardiovascular diseases however its development has been discontinued.
Status:
Investigational
Source:
INN:cariporide
Source URL:

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.
Status:
Investigational
Source:
INN:nexopamil
Source URL:

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
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:
INN:capravirine
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.