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Status:
Investigational
Source:
NCT02660112: Phase 2 Interventional Completed Friedreich's Ataxia
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(+)-Epicatechin or ent-Epicatechin is one of the 4 catechin diastereoisomers. (+)-Epicatechin has been isolated from various species of Palmae. It is occurred in the leaves or fruit of six palm species. In addition, it was isolated from Dryas octopetala and guarana seeds. It resists to the microbial transformation by endophytic fungi isolated from a tea plant.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mevastatin (compactin or ML-236B) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This drug induces apoptosis and arrest of cancer cells in G1 phase. Therapeutic effects of mevastatin on serum level of lipoproteins and unbiquinone-10 in patients with familial hypercholesterolemia were investigated. However, that study was discontinued. In addition, mevastatin was investigated for the treatment of melanoma. It was suggested, that mevastatin was unlikely to prevent melanoma at standard doses. However, higher doses could have a role to play in adjuvant therapy by inhibiting growth and invasion of melanoma cells. Also was revealed, that mevastatin increased histone deacetylase inhibitor, LBH589-induced cell death in triple-negative breast cancer (TNBC) cells.
Status:
Investigational
Source:
NCT02128971: Phase 2 Interventional Unknown status Anemia
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ferric glycinate is an iron chelate (Patent N 249.049/96 University of
Buenos Aires-SANCOR C.U.L., Argentina) that is produced
and used industrially in fluid milk fortification by
a dairy products company in Argentina.
Status:
Investigational
Source:
NCT01460420: Phase 1/Phase 2 Interventional Completed Hematologic Malignancies
(2011)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
(±)-quinuclidinyl benzilate (3-quinuclidinyl benzilate), is a specific muscarinic cholinergic receptor antagonist. It binds potently but reversibly to the muscarinic cholinergic receptors of mammalian brain and peripheral tissues. 3-quinuclidinyl benzilate was invented by Hoffmann-La Roche Inc in 1951, while investigating antispasmodic agents resembling tropine for the treatment of gastrointestinal conditions. In the 1960s 3-quinuclidinyl benzilate, was developed and weaponized as a new chemical agent for battlefield use as a psychochemical. Assigned the NATO code BZ it is classified as a hallucinogenic chemical warfare agent that affects both the peripheral and central nervous systems (CNS). It is one of the most potent anticholinergic psychomimetics known, with only small doses necessary to produce incapacitation. The primary route of absorption is through the respiratory system but absorption also can occur through the skin or gastrointestinal tract. BZ is odorless and is usually disseminated as an aerosol. Data regarding the health effects of BZ in humans following inhalation exposure are limited to military application studies. Pharmacologic activity of 3-quinuclidinyl benzilate is similar to other anticholinergic drugs (eg, atropine) but with a much longer duration of action. It was shown that I[3H]-3-quinuclidinyl benzilate accumulated in various brain regions after intravenous injection. The specific binding of [3-3H]3-quinuclidinyl-benzilate and [125I]3-quinuclidinyl-(3-iodo-4-hydroxy-benzilate) to rat brain subcellular fractions is parallel in myelin, synaptic plasma membrane and mitochondrial fractions with a 3-4-fold enrichment observed in synaptic plasma membrane over crude mitochondrial fractions. These findings suggested the use of 3-quinuclidinyl benzilate as a binding probe useful in assaying low levels of muscarinic receptor in tissue culture and other biological sources including labeling the receptor in vivo for autoradiographic studies. M2 muscarinic acetylcholine receptor (M2 receptor), essential for the physiologic control of cardiovascular function through activation of G protein-coupled inwardly-rectifying potassium channels, was shown to bind 3-quinuclidinyl benzilate with high affinity in vitro.
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
NCT03966833: Not Applicable Interventional Completed Mental Depression
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Isopropyl β-D-1-thiogalactopyranoside (IPTG) is a molecular biology reagent that induces β-galactosidase activity in many bacteria. This compound is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon, and it is therefore used to induce protein expression where the gene is under the control of the lac operator. Like allolactose, IPTG binds to the lac repressor and releases the tetrameric repressor from the lac operator in an allosteric manner, thereby allowing the transcription of genes in the lac operon, such as the gene coding for beta-galactosidase, a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. But unlike allolactose, the sulfur atom creates a chemical bond which is non-hydrolyzable by the cell, preventing the cell from metabolizing or degrading the inducer.
Status:
Investigational
Source:
NCT01530893: Not Applicable Interventional Completed Cardiovascular Disease Risk Reduction
(2012)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Flavanone is the basic chemical skeleton for the class of compounds known as Flavanoids. Flavonoids are naturally occurring secondary plant metabolites. They are mainly found in cereals and herbs. In the western diet, the estimated daily intake of flavonoids is in the range of 20 -50 mg per day. Flavonoids as a class generally have effects on CYP (P450) activity, and therefore may affect drug metabolisms.
Status:
Investigational
Source:
NCT03301454: Phase 2 Interventional Unknown status Esophageal Cancer, Squamous Cell
(2018)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Imazethapyr is an imidazole compound used as a selective herbicide. It is applied preplant incorporated, preemergence, at cracking, and postemergence. The compound controls weeds by reducing the levels of three branched-chain aliphatic amino acids, isoleucine, leucine and valine, through the inhibition of aceto-hydroxyacid synthase, an enzyme common to the biosynthetic pathway for these amino acids. This inhibition causes a disruption in protein synthesis which, in turn, leads to an interference in DNA synthesis and cell growth. The compound is used to control grasses and broadleaved weeds including barnyardgrass, crabgrass, cocklebur, panicums, pigweeds, nightshade, mustard, smartweed, velvetleaf, jimsonweed, foxtails, seedling johnsongrass, lambsquarters, morningglory and others. Tolerant crops include soybeans, peanuts, dry and edible beans, peas, alfalfa and imidazolinone resistant/tolerant corn. Additional research is being conducted on other leguminous crops. Acetolactate synthase inhibition is the primary mechanism of action of imazethapyr (IM).
Status:
Investigational
Source:
NCT01666587: Not Applicable Interventional Completed Ischemic Reperfusion Injury
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(R)-Ibuprofen, a nonsteroidal anti-inflammatory, is the less active enantiomer of ibuprofen. (S)-enantiomer of ibuprofen has the desired therapeutic effect (160 times more active than its (R)-enantiomer) in the in vitro inhibition of prostaglandin synthesis, while the (R)- ibuprofen is inactive. The accumulation of (R)- ibuprofen can cause serious side effects to the human body such as gastrointestinal pain and production of “hybrid” triglycerides between (R)- ibuprofen and Coenzyme A, which disrupt normal lipid metabolism and membrane function. The R(-)-isomer is almost inactive in inhibiting COX-2.
Status:
Investigational
Source:
NCT03262792: Not Applicable Interventional Completed Knee Osteoarthritis
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Neoandrographolide, one of the principal diterpene lactones, isolated from a medicinal herb Andrographis paniculata Nees. Andrographis paniculata (Burm. f.) Wall. ex Nees (Acanthaceae), also known as “kalmegh” in India, is a widely distributed plant in Asia. In many traditional formulations, the aerial parts have been used as anti-inflammatory and antipyretic drugs for the treatment of a variety of chronic and infectious diseases. Neoandrographolide possesses significant anti-inflammatory effects, which implies that it would be one of the major contributing components to participate in the anti-inflammatory effect of A. paniculata. and a potential candidate for further clinical trial.