LY-404,039

Izvor: Wikipedia
LY-404,039
(IUPAC) ime
(-)-(1R,4S,5S,6S)-4-amino-2-sulfonilbiciklo[3.1.0]heksan-4,6-dikarboksilna kiselina
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 9834591
Hemijski podaci
Formula C7H9NO6S 
Mol. masa 235,214 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

LY-404,039 je lek koji se koristi u naučnim istraživanjima kao selektivni agonist metabotropnih glutamatnih receptora grupe II podtipova mGluR2 i mGluR3.[3] Istraživanja su pokazala da ima znatan afinitet (Ki = 8.2±1nM) za D2 receptor iz čega sledi mogući mehanizam dejstva.[4] On ima anksiolitičko i antipsihotičko dejstvo u životinjskim studijama, ali ne uzrokuje sedaciju.[5]

Reference[uredi - уреди]

  1. 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. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. 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. 
  3. Rorick-Kehn LM, Johnson BG, Burkey JL, Wright RA, Calligaro DO, Marek GJ, Nisenbaum ES, Catlow JT, Kingston AE, Giera DD, Herin MF, Monn JA, McKinzie DL, Schoepp DD (April 2007). "Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039)". The Journal of Pharmacology and Experimental Therapeutics 321 (1): 308–17. doi:10.1124/jpet.106.110809. PMID 17204749. 
  4. Philip Seeman, Hong-Chang Gua (2009). "Glutamate Agonist LY404,039 for Treating Schizophrenia Has Affinity for the Dopamine D2 High Receptor". SYNAPSE: 935–939. doi:10.1002/syn.20704. 
  5. Rorick-Kehn LM, Johnson BG, Knitowski KM, Salhoff CR, Witkin JM, Perry KW, Griffey KI, Tizzano JP, Monn JA, McKinzie DL, Schoepp DD (July 2007). "In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders". Psychopharmacology 193 (1): 121–36. doi:10.1007/s00213-007-0758-3. PMID 17384937. 

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