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Class (Stereo):
CHEMICAL (RACEMIC)
Manozodil is a vasodilator agent.
Status:
Investigational
Source:
NCT00304525: Phase 1/Phase 2 Interventional Completed Metastatic Melanoma
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CHIR-265 (RAF265) is a potent selective orally active small molecule Raf-kinase inhibitor with anti‐angiogenic activity through inhibition of vascular endothelial growth factor type 2 (VEGFR‐2) in preclinical models. CHIR-265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. Raf kinase inhibition by CHIR-265 in mutant B-Raf melanoma cell lines causes cell cycle arrest and induces apoptosis, mimicking the effect of Raf RNAi in these cells. CHIR-265 also potently inhibits the phosphorylation of VEGFR2 and proliferation of VEGF-stimulated hMVEC.
Class (Stereo):
CHEMICAL (ACHIRAL)
Maroxepin is a tetracyclic compound antagonizing activity of dopamine receptors. Maroxepin has a potent central nervous action and a strong sedative potential. Maroxepin exerts both antipsychotic and antidepressant properties.
Class (Stereo):
CHEMICAL (ACHIRAL)
Mepramidil (PF-26) is a coronary vasodilator.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Mepiroxol is pyridine-oxide derivative with some antimicrobial activity.
Class (Stereo):
CHEMICAL (ACHIRAL)
Linetastine has anti-inflammatory and anticarcinogenic effects. It is a potent inhibitor of 5-lipoxygenase. It also inhibits histamine release and epidermal cyclooxygenase activity. It also markedly inhibited TPA-stimulated leukotriene B4 formation, but inhibited formation of prostaglandin E2, a cyclooxygenase product, only slightly. This suggested that neither cyclooxygenase inhibition nor antihistaminic activity were essential to the anti-inflammatory action of linetastine. The anti-inflammatory effect of oral linetastine is probably due to 5-lipoxygenase inhibition. Oral administration of linetastine almost completely suppressed Cyp1a1 mRNA levels in mouse epidermis induced by a topical application of 3-methylcholanthrene or benzo[a]pyrene to mouse skin. Oral administration of linetastine inhibited DMBA-caused skin tumor initiation at least in part by inhibiting Cyp1a1 mRNA induction and epidermal aryl hydrocarbon hydroxylase activity. Linetastine had been in phase II clinical trial for the treatment of allergic rhinitis. However, this study was discontinued.
Status:
Investigational
Source:
INN:phenampromide [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Phenampromide is an opioid analgesic, which is considered to be structurally similar to isomethadone. Phenampromide belongs to the ampromide family of drugs, which also include propiram and diampromide. According to the literature, (R)-phenampromide has greater analgesic potency than its (S)-enantiomer. Synthetic narcotic analgesic phenampromide is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.
Status:
Investigational
Source:
NCT00055510: Phase 2/Phase 3 Interventional Completed Graft Occlusion, Vascular
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Seglitide (previously known as L363,586 or MK-678), a cyclic, hexapeptide analog of somatostatin-14, is a somatostatin receptor 2 (SSTR2) agonist. This compound was studied in Alzheimer's disease. Besides, it possessed inhibitory actions on rat growth hormone (GH) release and thus could have a role in the treatment of acromegaly. Intravenous and intranasal administration of seglitide to diabetic subjects was effective in reducing both fasting and postprandial hyperglycemia. Thus, this compound could be useful in the control of unstable diabetes. In addition, preclinical studies have shown that seglitide had potential as a treatment for diabetic retinopathy and macular degeneration. However, the further studied of this compound were discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Odapipam is a benzazepine with high affinity and selectivity for D1-dopamine receptors. Labeled with C-11, it has been used as a PET radiotracer to visualize D1 receptors both in striatal and extrastriatal areas, such as the prefrontal cortex. Odapipam inhibits dopamine D1 receptor binding in vitro with low nanomolar to picomolar dissociation constants. The affinity of [11C]NNC 756 for D1 receptors is 0.18 nM. Odapipam was tested in phase I of clinical trials for the treatment of psychotic disorders, but failed.