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Restrict the search for
amphotericin b
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Decloxizine (UCB-1402; NSC289116) is a histamine 1 receptor antagonist. Decloxizine is a broncholyticum.
Status:
Investigational
Source:
NCT01314014: Phase 2 Interventional Completed Follicular Lymphoma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Imexon (INN, trade name Amplimexon) is a substance that is being studied in the treatment of some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. Imexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm. Nuvenzepine substantially shares the antimuscarinic properties of pirenzepine but it is also endowed with a (weak) H1-blocking action. Nuvenzepine is selective for M1 receptors (pA2 = 6.63-7.74). Nuvenzepine, administered intraduodenally, displayed a long-lasting and dose-dependent inhibition of neostigmine-induced intestinal motility in anaesthetized cats. On ileal motor activity, the compound showed a potency 10 times greater than that of pirenzepine, and, although to a lesser extent, it was also active, unlike pirenzepine, on colonic stimulated motility. In conscious cats, nuvenzepine inhibited pentagastrin-stimulated gastric acid secretion resulting 25-30 times more potent than pirenzepine.
Status:
Investigational
Source:
INN:dimethylthiambutene [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Dimethylthiambutene is the synthetic narcotic analgesic agent. It has analgesic effect similar to those of meperidine. The (+)-enantiomer of dimethylthiambutene is more active than the (-)-isomer. Dimethylthiambutene clinically compared with meperidine (pethidine), but maintains the dependence-producing capability of morphine. It has had illicit use in Japan in the past. Dimethylthiambutene is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.
Status:
Investigational
Source:
NCT01155531: Phase 1 Interventional Completed Obesity
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Telenzepine is a selective muscarinic M1 receptor antagonist that was studied for selective inhibition of gastric acid secretion. Telenzepine was used in clinical trials in patients with acute duodenal ulcer, where was found that once daily administration of 3 mg in the evening must be regarded as the optimal dosage regimen of telenzepine. However, the preregistration for peptic ulcer in Germany was discontinued. In addition, the drug was studied in patients with nocturnal asthma. It was shown that telenzepine via the oral route at a dose of up to 5 mg was not effective in preventing nocturnal asthma.
Status:
Investigational
Source:
NCT00483704: Phase 3 Interventional Completed Migraines
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Telcagepant (MK-0974) is a calcitonin gene-related peptide receptor antagonist. Merck & Co was developing telcagepant for the treatment of pain. Telcagepant is an extremely potent CGRP antagonist with a Ki = 0.77 (0.07 nM). Telcagepant showed efficacy against acute migraines; however, different patient populations may show more beneficial effects with telcagepant versus triptans. In the acute treatment of migraine, Telcagepant was found to have equal potency to rizatriptan and zolmitriptan in two Phase III clinical trials. Merck & Co has now terminated development of the drug.
Status:
Investigational
Source:
JAN:CILOSTAMIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cilostamide (also known as OPC 3689) is a selective inhibitor of type III phosphodiesterases: PDE3A and PDE3B, which inhibits thrombin-induced platelet aggregation. Elevating intracellular cAMP has been shown to inhibit platelet function. cAMP interferes with platelet-activating signals, which leads to aggregation inhibition, but the precise mechanism is unclear. It is known, that inhibition of Akt phosphorylation leads to inhibition of phosphorylation of glycogen synthase kinase 3-beta (GSK-3beta), which is an effector of Akt. However, cAMP-elevating agents’ stimulated GSK-3beta phosphorylation at Ser9. The cAMP-elevating agent cilostamide did not directly affect the enzyme activity of PI3-kinase, and thus it has two effects on PI3K signaling: inhibition of Akt phosphorylation independent of PKA. And stimulation of GSK-3beta phosphorylation dependent on PKA.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Clorotepine (aka octoclothepin or octoclothepine) is an antipsychotic from the tricyclic group derived from perathiepin. It was originally developed in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis. Clorotepine has a high affinity for the dopamine (D1, D2, D3, D4), receptors the serotonin 5-HT (2A, 2B, 2C, 6, 7) receptors, the alpha-adrenergic receptors (1A, 1B, 1D), and the histamine H1 receptors. In most instances, it acts as an antagonist (or inverse agonist). Clorotepine will also block the reuptake of norepinephrine by inhibiting the norepinephrine transporter.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Zaprinast is (M&B 22,948; 2-o-propoxy-phenyl-8-azapurin-6-one) is a selective inhibitor of cyclic GMP (cGMP)-dependent phosphodiesterases, with vasodilation activity in a variety of species and tissues. The potency of zaprinast as a vasorelaxant varies with the species, the tissue, and the presence and absence of endothelium. Zaprinast apparently loses all or most of its vasorelaxant capacity when arteries have been denuded of the endothelial cell layer. Alternatively, the vasorelaxant effects of zaprinast can be attenuated using methylene blue, an inhibitor of soluble guanylate cyclase and hemoglobin inhibitor of nitric oxide synthesis. Therefore, zaprinast-induced relaxations appear to be endothelium-dependent. In human platelets zaprinast, at a dose of 10 mkM, caused a modest (20%) inhibition of aggregation as well as a small increase in cGMP content. In anesthetized rats, zaprinast dose-dependently lowered mean arterial blood pressure (MAP), an effect that correlated well with increased levels of plasma cGMP. Zaprinast decreased mean arterial pressure, the reduction being inversely related to zaprinast concentration. Zaprinast had no effect on heart rate, but increased cardiac output, urinary output, urinary sodium excretion, as well as renal blood flow. Oral administration of zaprinast to spontaneously hypertensive rats at a dose of 200 mg/kg/day normalized blood pressure. In normotensive rats, however, no changes in blood pressure were observed with the same treatment. In an initial placebo-controlled, double-blind crossover trial, 10 mg of zaprinast was effective in reducing exercise-, but not histamine-induced bronchoconstriction in adult asthmatics. However, in a similar study with asthmatic children, zaprinast was ineffective in preventing exercise-induced bronchoconstriction. Since then the clinical development of zaprinast has been discontinued.
Status:
Investigational
Source:
NCT00230074: Phase 2 Interventional Completed Amyotrophic Lateral Sclerosis
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Omigapil (CGP 3466 or TCH346) is a structurally related analog of R-(-)-deprenyl that exhibits virtually no monoamine oxidase type B inhibiting activity but is neuroprotective in the picomolar concentration range. It binds to glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and at subnanomolar concentrations prevent the S-nitrosylation of GAPDH, inhibit GAPDH-Siah binding and prevent the nuclear translocation of GAPDH. Omigapil demonstrated promising potential in the treatment of Parkinson's disease and motoneuron disease in animal models, however, it did not show efficacy in clinical trials. Omigapil is in development for the treatment of congenital muscular dystrophy.
