Mavoglurant
Mavoglurant (AFQ-056) je eksperimentalni kandidat leka za tretman fragilnog X sindroma.[3] On deluje kao antagonist metabotropnog glutamatnog receptora 5 (mGlu5).[4]
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Nazivi | |
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IUPAC naziv
Metil (3aR,4S,7aR)-4-hidroksi-4-[(3-metilfenil)etinil]oktahidro-1H-indol-1-karboksilat
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Drugi nazivi
AFQ056
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Identifikacija | |
3D model (Jmol)
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ChemSpider | |
ECHA InfoCard | 100.219.728 |
UNII | |
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Svojstva | |
C19H23NO3 | |
Molarna masa | 313,40 g·mol−1 |
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa). | |
Reference infokutije | |
Mavoglurant razvija Novartis i trenutno je u fazi III kliničkih ispitivanja.[3][5] U slučaju uspešnog ishoda ispitivanja, on će biti privi lek koji tretira poremećaju umesto simptoma fragilnog X sindroma.[6]
Reference
уреди- ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today. 15 (23-24): 1052—7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.
- ^ Evan E. Bolton; Yanli Wang; Paul A. Thiessen; Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry. 4: 217—241. doi:10.1016/S1574-1400(08)00012-1.
- ^ а б P. Cole (2012). „Mavoglurant”. Drugs of the Future. 37 (1): 7—12. doi:10.1358/dof.2012.37.1.1772147.
- ^ Levenga, J; Hayashi, S; De Vrij, FM; Koekkoek, SK; Van Der Linde, HC; Nieuwenhuizen, I; Song, C; Buijsen, RA; et al. (2011). „AFQ056, a new mGluR5 antagonist for treatment of fragile X syndrome”. Neurobiology of disease. 42 (3): 311—7. PMID 21316452. doi:10.1016/j.nbd.2011.01.022.
- ^ Jacquemont, S.; Curie, A.; Des Portes, V.; Torrioli, M. G.; Berry-Kravis, E.; Hagerman, R. J.; Ramos, F. J.; Cornish, K.; et al. (2011). „Epigenetic Modification of the FMR1 Gene in Fragile X Syndrome is Associated with Differential Response to the mGluR5 Antagonist AFQ056”. Science Translational Medicine. 3 (64): 64ra1. PMID 21209411. doi:10.1126/scitranslmed.3001708.
- ^ „AFQ056 drug improves symptoms in Fragile X patients: Study”. news-medical.net. 9. 1. 2011.