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Restrict the search for
vitamin a
to a specific field?
Class (Stereo):
CHEMICAL (RACEMIC)
Batanopride, previously known as BMY-25801, a 5-hydroxytryptamine 3 receptor antagonist, was studied against emesis for cancer patients that were treated by chemotherapy procedure. Batanopride had the dose-limiting side effects including hypotension and long QT syndrome that is why any further experiments for its medical application were discontinued.
Status:
Investigational
Source:
INN:benzaprinoxide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 and is of potential interest in the treatment of psoriasis and other diseases characterized by accelerated cell growth and T lymphocyte activation, which was studied in the clinical trial. KH1060 also prevents type I diabetes in the preclinical investigation without significant effects on calcium or bone metabolism. In addition also was shown that neuroblastoma (NB) cell lines were more susceptible to growth inhibition by KH1060, suggesting its possible use in NB to potentiate the action of retinoids, which are in clinical use for this disease. The underlying biochemical reasons for the increased biological activity of KH1060 are unknown, but it can include 1) metabolic considerations in addition to explanations based upon 2) enhanced stability of KH1060-liganded transcriptional complexes.
Status:
Investigational
Source:
INN:fenmetozole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Fenmetozole is an alpha-2 adrenergic receptor antagonist which was developed for the treatment of schizophrenic and/or depressed patients, however never reached the market. It was also shown that the drug may reduce symptoms of minimal brain dysfunction in children and antagonize the effect of barbiturates and ethanol.
Status:
Investigational
Source:
NCT02251197: Phase 2 Interventional Completed Stroke
(2001)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Clobenetine is benzomorphan derivative developed by Boehringer-Ingelheim. Clobenetine acts as a sodium channel blocker and displaces radioligand from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes with IC50 of 49 nM. The IC50 value for the inactivated Na(+) channels was much lower than for Na(+) channels in the resting state. In animal models, clobenetine reduced lesion size in mice and rats when administered 5 min after permanent focal cerebral ischemia at doses that did not impair motor coordination. Clobenetine produced significant analgesic and anti-hyperalgesic effects in the rat model of arthritis, induced by complete Freund's adjuvant. In the early 2000s, the compound was investigated in phase II clinical trial for the treatment of thromboembolic stroke, but no results were reported.
Status:
Investigational
Source:
NCT01362400: Phase 2 Interventional Completed Non Small Cell Lung Cancer
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.
Status:
Investigational
Source:
INN:ciaftalan zinc [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ciaftalan Zinc (also known as Zinc(II)-phthalocyanine) is phthalocyanine and photosensitizers which showed a high activity in photodynamic therapy studies on a variety of animal tumors. Ciaftalan Zinc belongs to second generation photosensitizers that have a more intense long wavelength absorption and greater extinction coefficient compare to the first generation. The greater the extinction coefficient value associated with greater efficacy, smaller drug dosage required to induce a cytotoxic response and diminished risk of provoking systemic toxic reactions. The long absorption wavelength correlates with higher penetration depth and it is, therefore, Ciaftalan Zinc causes deep tumor necrosis in animal models. Currently, Tetra-triethyleneoxysulfonyl substituted Ciaftalan Zinc derivatives are studied as novel photodynamic therapy of cancer.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.
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 (ACHIRAL)
Butanserin is the potent and selective alpha 1-adrenoceptor antagonist.
