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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00094003: Phase 1 Interventional Completed Liver Neoplasms
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Acefurtiamine is a vitamin B1 analog. It is as an analgesic.
Status:
Investigational
Source:
NCT00966914: Phase 3 Interventional Completed Non-small Cell Lung Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Dimesna is a prodrug of mesna (dimer of mesna). Dimesna is reduced to mesna in the kidneys. Dimesna does not prevent cellular damage by metabolites of ifosfamide and cyclophosphamide in the renal tubular cell line LLC-PK1. Dimesna is a mucolytic agent used to alleviate toxic side effects of antitumor drugs. The organic acid transporter OAT4 on the luminal side of the proximal renal tubule facilitates the reabsorption of dimesna, and therefore its reduction to mesna, whereas the multidrug and toxin extrusion protein MATE1, the multidrug resistance protein MRP2, and P glycoprotein facilitate the efflux of mesna and/or dimesna back into the lumen; dimesna may also be excreted unchanged by MRP4. It has therefore been suggested that polymorphism of these renal transport proteins or transporter-mediated drug-drug interactions may reduce the efficacy of mesna and dimesna.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oxfenicine is a CPT-1b-specific inhibitor. It must be transaminated to its active form, 4-hydroxyphenyl-glyoxylate, which is competitive with carnitine, preventing the formation of acylcarnitine. Because CPT-1b shows the highest sensitivity to 4-hydroxyphenyl-glyoxylate, inhibition of fatty acid oxidation by oxfenicine takes place selectively in those tissues that express this CPT isoform. It may be effective for treating noninsulin-dependent diabetes mellitus which is characterized by elevated fatty acid levels and obesity. In 1980 it was also tested in preclinical models of angina pectoris and ischemia.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Furacrinic acid (also known as GP 48 674) was studied as a diuretic agent and participated in clinical trials. However, information about the further development of this drug is not available.
Class (Stereo):
CHEMICAL (ACHIRAL)
Pirmagrel is the selective thromboxane synthetase inhibitor. The compound was well tolerated by all subjects without evidence of any adverse reactions. Serum thromboxane B2 levels (the stable metabolic product of thromboxane A2) were significantly reduced after administration of the compound, with the maximal effect of a 99 per cent reduction occurring at 0.5 and 1 hour after administration. Bleeding times showed a slight increase 2 hours after administration of the compound. Pirmagrel was able to completely prevent the increase in serum thromboxane B2 following allergen challenge in asthmatic patients; while it caused a very small reduction in the early response to allergen, there was no effect on the late response or on airway hyperresponsiveness. Pirmagrel was developed for the treatment of ischemic heart disorders and thrombosis. However, this development was discontinued.
Status:
Investigational
Source:
USAN:SODIUM ARSENATE AS 74 [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Sodium arsenate as-74 (As74) has been the principal positron-emitting scanning agent. As74 as a commercial preparation for parenteral adminitration was made available towards the end of 1956. From March 1957 all studies were made with sodium arsenate rather than sodium arsenite. Sodium arsenate as-74 was used in the diagnosis of suvatentorial brain tumours. Traces of the element were found in all body tissues, and assays of injected As74 recovered in brain tumours showed highest values in meningiomas, followed, in order, by gliolastomas, metastatic carcinomas and astrocytomas.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Meteneprost (9-deoxo-16, 16-dimethyl-9-methylene PGE2) is a prostaglandin E2 analog. It exerts uterine-stimulating potency: meteneprost is able to both stimulate uterine contractions and dilate the cervical canal. It was studied as an abortifacient in early pregnancy.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
GV 150526A (gavestinel) is an investigational drug for a neuroprotective therapy of acute ischemic stroke within 6 hours of symptom onset. It is a potent and selective non-competitive antagonist at the glycine site of the N-methyl-D-aspartate receptor (NMDA) which reduces infarct volume in experimental stroke models. Gavestinel acts at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex with nanomolar affinity (pKi = 8.5), coupled with high glutamate receptor selectivity. Gavestinel displays higher than 1000-fold selectivity over NMDA, AMPA and kainate binding sites and is orally bioavailable and active in vivo. GV 150526A inhibited convulsions induced by NMDA in mice, when administered by both IV and po routes (ED50 = 0.06 and 6 mg/kg, respectively). The safety and efficacy of GV150526 were studied in two phase III randomized placebo-controlled clinical trials of acute ischemic stroke patients within 6 h from onset [The Glycine Antagonist in Neuroprotection (GAIN) International and GAIN Americas Trials] sponsored by GlaxoSmithKline. The results of these trials suggested that gavestinel was not of substantial benefit or harm to patients with primary intracerebral hemorrhage.
