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Restrict the search for
m nalidixic acid
to a specific field?
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
Class (Stereo):
CHEMICAL (RACEMIC)
Clomoxir (POCA, B 807-27) is a potent inhibitor of mitochondrial fatty acid oxidation at the stage of carnitine palmitoyltransferase I (CPT-I). It acts by the tight binding of POCA-CoA to this enzyme. The compound demonstrated hypoketonaemic and hypoglycaemic activities in fasted normal and diabetic rats.
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:
JAN:RITOBEGRON ETHYL HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.
Class (Stereo):
CHEMICAL (RACEMIC)
Moxadolen is tricyclo-[5.2.1.0.2.6endo]decenone derivative. Moxadolen pharmacokinetics were investigated after oral application in male Wistar rats. The compound is extensively absorbed and mainly renally eliminated. Within 60 h, 63% of the activity is recovered in urine and feces. After 12 h 27% of the activity is eliminated (application in polyethylene glycol). The highest total concentration of the activity in the plasma is found after 2 h, the highest of the unchanged drug is found after 1 h. The half-life is 2.9 h.
Class (Stereo):
CHEMICAL (RACEMIC)
Miroprofen, an imidazopyridine derivative, possesses anti-inflammatory properties. It was shown that this compound could be effective in suppressing pain responses and acute inflammation accompanied by increased vascular permeability. Analgesic effect of this compound was studied in post-extraction pain. However, information about the current study of this agent is not available.
Class (Stereo):
CHEMICAL (MIXED)
Micinicate, a vasodilator was developed as a spasmolytic agent. Information about the current use of this compound is not available.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Brecanavir (previously known as VX-385), a HIV aspartyl protease inhibitor was developed for the treatment of HIV. The inhibition of HIV viral proteinase enzyme prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Brecanavir reached Phase II development. However, GlaxoSmithKline announced to discontinue development brecanavir. Because of the inability to develop a viable oral dosage formulation capable of delivering the desired brecanavir levels in patients with multi-drug resistant HIV.
Class (Stereo):
CHEMICAL (UNKNOWN)
Deprostil is prostaglandin E analog. The drug exhibits a prolonged inhibition of basal gastric acid secretion. Deprostil is the orally active anti-ulcer agent. It is a racemate with four possible optical isomers. Like deprostil the (nat)- and (epi)-isomers appear to be potentially useful therapeutic agents for the treatment of hypergastrlc acid secretion and peptic ulcers.
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.
