{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Restrict the search for
nonoxynol-9
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Lixazinone selectively inhibits the high-affinity form of cyclic AMP phosphodiesterase (type IV) isolated from human platelets with only weak effects on both the nonspecific and cyclic GMP-sensitive phosphodiesterases. The inhibitor reduces both maximum velocity and substrate affinity of the type IV enzyme. Lixazinone exhibits marked selectively for the platelet high-affinity enzyme. It also has significant inhibitory effects on cardiac membrane-bound phosphodiesterase. Lixazinone may be useful as an agent to increase cardiac output in the treatment of congestive heart failure. It is a potent PDE3 inhibitor. Lixazinone suppresses folic acid-induced proliferation of rat tubular epithelial cells in vivo.
Class (Stereo):
CHEMICAL (RACEMIC)
Tiquinamide (Wy 24081) is a potent inhibitor of gastric secretion and gives good protection in animals against gastric and duodenal erosions induced by stress and chemical stimuli. It reduces basal as well as stimulated acid secretion but has no anticholinergic activity and is only a weak histamine H2 antagonist, since it is substantially more potent in inhibiting basal acid-secretion than the established H2-receptor antagonists, metiamide and burimamide. Since no other pharmacological effect of tiquinamide has been detected in isolated tissues, it seems unlikely that the gastric antisecretory effect of the compound results from a direct action on the peripheral autonomic nervous system. The report from Dr. Szabo on the protective effect of dopamine agonists against duodenal ulceration suggests a possible mechanism of action for tiquinamide.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Tipropidil designed for the treatment of cerebral and peripheral vascular diseases. Tipropidil has been investigated because of its expected antihyperviscosity properties. The increase in plasma free fatty acid levels and decrease in lipolytic response were found to be dependent on the amount of Tipropidil administered. Addition of Tipropidil to the in vitro lipolysis system inhibited norepinephrine- and theophylline-induced fatty acid release in a dose-dependent manner. These results suggest a potent inhibitory action for Tipropidyl on fatty acid mobilization in rat adipose tissue.
Status:
Investigational
Source:
INN:pirandamine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Pirandamine is the potential antidepressant drug. It is a relatively selective inhibitor of the serotonin uptake mechanism and does not exhibit appreciable norepinephrine uptake blocking activity in contrast to the tricyclic antidepressant drugs imipramine and amitriptyline. Pirandamine is equivalent to amitriptyline and greater than imipramine in potency as a serotonin uptake blocker and a potentiator of central serotonin pharmacological actions, and in contrast, does not exhibit appreciable central anticholinergic effects. Pirandamine potentiated the behavioral effects of 5-hydroxytryptophan in mice. Pirandamine, in contrast to desimipramine and imipramine, did not prevent reserpine-induced hypothermia. The (-)-enantiomer of pirandamine retained the activity of the racemate; the (+I-enantiomer was much less effective.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bisnafide (previously known as DMP 840), a bis-naphthalimide derivative that was developed by Bristol-Myers Squibb as a potential anticancer agent. Bisnafide acts as DNA intercalator and topo II inhibitor. This drug participated in phase I clinical trials in pediatric patients with refractory solid tumors. However, further, development has been discontinued.
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.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Alvameline is a partial agonist of the M1 mAChR that also displays M2/M3 antagonist effects. It readily crosses the blood-brain barrier. It has an effect profile that makes it of interest to test its ability to counteract bladder overactivity in humans. Behaviorally, alvameline has been shown to significantly improve Morris water maze (MWM) performance in both young and ageimpaired rats. It failed to improve cognition in patients with mild to moderate Alzheimer's disease.
Status:
Investigational
Source:
NCT00625664: Phase 3 Interventional Completed Urinary Bladder Neoplasms
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
LAROTAXEL is a taxoid with potential antineoplastic activity. It prevents microtubule depolymerization, thereby inhibiting cell proliferation. It displays a broad spectrum of antitumor activity in vitro and in vivo, including activity against P-glycoprotein expressing tumors. LAROTAXEL was in phase III clinical trials for the treatment of breast cancer, pancreatic cancer, and bladder cancer. However, its development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Early explorations of spider and scorpion venoms provided clues for the discovery of new classes of compounds, including delucemine, that act as neuroprotectants in animal models of stroke. This compound targets open NMDA receptor-operated calcium channels and blocks the channel. By blocking these channels, which open in response to the neurotransmitter glutamate, delucemine prevents excessive calcium influx during ischemia. This stabilizes cell chemistry and minimizes cell death. Delucemine attenuated short-term cognitive deficits and histopathological changes associated with traumatic brain injury. Delucemine improved measures of brain tissue edema and ion homeostasis.
Status:
Investigational
Source:
NCT00533377: Phase 2 Interventional Completed Tibial Fractures
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evatanepag (CP-533,536) is a prostaglandin E2 EP2 receptor agonist. It stimulates new bone formation on trabecular, endocortical, and periosteal surfaces and enhances fracture healing. Evatanepag was under development with Pfizer as a bone formation stimulant for therapeutic use in the healing of fractures.
