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LY-404,039
Systematic (IUPAC) name
(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid
Identifiers
CAS number  ?
ATC code  ?
PubChem 9834591
Chemical data
Formula C 7H9NO6S 
Mol. mass 235.214 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

LY-404,039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3.[1] It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation.[2] Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.[3][4][5]

LY-214,0023

See also

References

  1. ^ 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.  
  2. ^ 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.  
  3. ^ Patil ST, Zhang L, Martenyi F, Lowe SL, Jackson KA, Andreev BV, Avedisova AS, Bardenstein LM, Gurovich IY, Morozova MA, Mosolov SN, Neznanov NG, Reznik AM, Smulevich AB, Tochilov VA, Johnson BG, Monn JA, Schoepp DD (September 2007). "Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial". Nature Medicine 13 (9): 1102–7. doi:10.1038/nm1632. PMID 17767166.  
  4. ^ Lebois EP (2008). "Neither typical nor atypical: LY404039 provides proof of concept that selective targeting of mGluR2/3 receptors is a valid mechanism for obtaining antipsychotic efficacy". Current Topics in Medicinal Chemistry 8 (16): 1480–1. PMID 19006848.  
  5. ^ Fraley ME (June 2009). "Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia". Expert Opinion on Therapeutic Patents. doi:10.1517/13543770903045009. PMID 19552508.  
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