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

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Showing 491 - 500 of 4351 results

Status:
Investigational
Source:
INN:rosaramicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rosamaricin is a macrolide antibiotic similar to erythromycin. This compound is more effective against Gram-negative bacteria than erythromycin, especially in the prostate where rosamaricin was shown to be more concentrated than erythromycin in dogs. Rosamaricin has antibiotic activity against Neisseria gonorrhoeae, Chlamydia trachomatis, Ureaplasma urealyticum and Mycoplasma hominis. When the drug was compared with penicillin G in the treatment of pneumococcal meningitis in rabbits it was found to be less effective than penicillin G, as measured by bacterial clearance from cerebrospinal fluid and by treatment outcome. No information on the current use of this compound is available.
Status:
Investigational
Source:
INN:lorpiprazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lorpiprazole (brand name Normarex) is a marketed anxiolytic drug of the phenylpiperazine group. It has been described as a serotonin antagonist and reuptake inhibitor (SARI) in the same group as trazodone, nefazodone, and etoperidone.
Status:
Investigational
Source:
INN:bedoradrine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.
Status:
Investigational
Source:
INN:etonitazene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Etonitazene is a potent and selective mu-opioid agonist. It was developed in CIBA. Administration of etonitazene may induce respiratory depression, and therefor etonitazene is not used in humans. Etonitazene is explicitly listed as an illegal drug under UN convention and is illegal throughout the world.
Status:
Investigational
Source:
INN:fenobam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fenobam is a selective and potent metabotropic glutamate (mGlu)5 receptor antagonist with inverse agonist activity. Fenobam was previously investigated as an anxiolytic in a number of phase II studies in the early 1980s. These studies revealed a mixed picture of anxiolytic efficacy, with double blind, placebo controlled trials variously reporting the compound as active or inactive. This discrepancy was not easily reconciled based on patient numbers, dose level, duration of treatment, or outcome measures. The positive effects seen in animal models of fragile X syndrome (FXS) treated with fenobam or other mGluR5 antagonists, the apparent lack of clinically significant adverse effects, and the potential beneficial clinical effects seen in this pilot trial support further study of the compound in adults with FXS.
Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.
Status:
Investigational
Source:
INN:ciclazindol [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Ciclazindol is an indole derivative and monoamine uptake inhibitor patented by pharmaceutical company John Wyeth and Brother Ltd. as an antidepressant. Besides that, Ciclazindol is effective anorectic agent, inducing weight loss in rats and man. Ciclazindol was shown to inhibit ATP-sensitive K+ (K(ATP)) channel currents and stimulate insulin secretion from CRI-G1 insulin-secreting cells. The inhibition of KATP channel currents by ciclazindol is unaffected by the removal of intracellular Mg2+ ions and after trypsinization of the cytoplasmic surface of excised patches, treatments known to abolish sulphonylurea sensitivity.
Status:
Investigational
Source:
INN:ciprefadol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ciprefadol is an opioid analgesic drug. It binds with a high affinity to mu (Ki 4.2 nM) and kappa (Ki 2.5 nM) opioid receptors. In vivo, ciprefadol displays mixed antagonist/agonist activity in the mouse writhing and the rat tail heat tests: in low doses, the compound inhibits the analgesic effect of morphine, while at higher doses it displays analgesic effect. Chronic administration of ciprefadol to rhesus monkeys produced a marked physical dependence more severe than that of morphine, and its effect was consistent with what would be expected of a potent, long-lasting morphine-like agonist.
Status:
Investigational
Source:
INN:naxaprostene
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naxaprostene (CG 4305) is a prostacyclin analogue, which causes concentration dependent inhibition of thrombocyte function. Naxaprostene is more selective for IP receptors and tends towards partial agonism. Naxaprostene prevented thrombotic arterial occlusion in rabbits.
Status:
Investigational
Source:
INN:butilfenin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Butilfenin is N-substituted iminodiacetic acid derivative that was studied as tridentate ligand to form a technetium-99m complex.