VU 0361737 - CAS 1161205-04-4
Catalog number: 1161205-04-4
Category: Inhibitor
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Molecular Formula:
C13H11ClN2O2
Molecular Weight:
262.693
COA:
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Targets:
mGluR
Description:
VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displaying weak activity at mGlu5 and mGlu8 receptors, and being inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
Synonyms:
VU 0361737, VU-0361737, VU0361737
MSDS:
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InChIKey:
ARYUXFNGXHNNDM-UHFFFAOYSA-N
InChI:
InChI=1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17)
Canonical SMILES:
COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl
1.Evaluation of the antimicrobial properties of different parts of Citrus aurantifolia (lime fruit) as used locally.
Aibinu I;Adenipekun T;Adelowotan T;Ogunsanya T;Odugbemi T Afr J Tradit Complement Altern Med. 2006 Nov 13;4(2):185-90.
We investigated the potency of Citrus aurantifolia (Lime fruit), against pathogens, in the different forms in which this fruit plant is used locally (juice of the fruit, burnt rind of the fruit commonly known as "epa-ijebu" in the Yoruba dialect) and the oil obtained from steam distillation of the fruit. The antimicrobial activity of "epa-ijebu" in different solvents was also compared. The solvents include palm-wine (a local alcoholic drink tapped from palm trees), Seaman's Schnapps 40% alcoholic drink, water, ethanol and fermented water from 3 days soaked milled maize known as "ekan-ogi" or "omidun" in the Yoruba dialect. Antimicrobial activity was carried out by the agar well diffusion. The clinical isolates used included Anaerobic facultative bacteria, namely: Staphylococcus aureus ATCC 25213, Staphylococcus aureus, Salmonella paratyphi, Shigella flexnerii, Streptococcus faecalis, Citrobacter spp, Serratia spp, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli ATCC 25922, and Escherichia coli; Fungi such as Aspergillus niger and Candida albicans; and Anaerobes which includes Bacteroides spp, Porphyromonas spp, and Clostridium spp. Crude extracts of all solvents used varied in zones of inhibition.
2.A study of placental umbilical cord whole blood transfusion in 72 patients with anemia and emaciation in the background of cancer.
Bhattacharya N Eur J Gynaecol Oncol. 2006;27(2):155-61.
In the under-resourced world, transfusion to advanced oncological patients involves two major problems, i.e., (a) transfusion transmitted disease, and (b) infrastructural deficiency. Many hospitals cannot cope with the specialized requirements of immunocompromised cancer victims, for instance, leucoreduction, selective apheresis, irradiation of the blood, viral inactivation of the blood by solvent and/or detergent treatment or photochemical inactivation using psoralen or long wavelength ultraviolet light and cytomegalovirus safe blood. The exorbitant cost of red blood cell (RBC) substitutes like hemoglobin-based oxygen carriers or perflurocarbon emulsions, liposome encapsulated hemoglobin, is simply unacceptable for an average oncological patient in the developing world. Moreover, it should be underscored that none of the total blood functions are replaced by any available so-called blood substitute, the primary function of which is oxygen delivery and volume expansion only. A more accurate term should be red cell substitute. Cord blood, because of its rich mix of fetal and adult hemoglobin, platelet and white blood cell (WBC) count, and plasma filled with cytokine and growth factors--as well as its hypoantigenic nature and altered metabolic profile--has all the potential of a real and safe alternative to adult blood during emergencies or any etiology of blood loss.
3.The neuroprotective effects of orthosteric agonists of group II and III mGluRs in primary neuronal cell cultures are dependent on developmental stage.
Jantas D;Gręda A;Gołda S;Korostyński M;Lasoń W Neuropharmacology. 2016 Dec;111:195-211. doi: 10.1016/j.neuropharm.2016.09.003. Epub 2016 Sep 4.
Activation of metabotropic glutamate receptors (mGluRs) modulates neuronal excitability. Here, we evaluated the neuroprotective potential of four structurally diverse activators of group II and III mGluRs: an orthosteric agonist of group II (LY354740), an orthosteric agonist of group III (ACPT-I), an allosteric agonist of mGluR7 (AMN082) and a positive allosteric modulator (PAM) of mGluR4 (VU0361737). Neurotoxicity was induced by the pro-apoptotic agents: staurosporine (St) and doxorubicin (Dox) or the excitotoxic factor glutamate (Glu). The effects were analyzed in primary hippocampal (HIP) and cerebellar granule cell (CGC) cultures at two developmental stages, at 7 and 12 days in vitro (DIV). The data reveal a general neuroprotective effect of group II and III mGluR activators against the St- and Glu- but not Dox-induced cell damage. We found that neuroprotective effects of group II and III mGluR orthosteric agonists (LY354740 and ACPT-I) were higher at 12 DIV when compared to 7 DIV cells. In contrast, the efficiency of allosteric mGluR agents (AMN082 and VU0361737) did not differ between 7 and 12 DIV in both, St and Glu models of neuronal cell damage. Interestingly, the protective effects of activators of group II and III mGluRs were blocked by relevant antagonists only against Glu-induced neurotoxicity.
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CAS 1161205-04-4 VU 0361737

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