CECXG

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CECXG
CECXG structure.png
Systematic (IUPAC) name
2-(1'SR,2'SR,3'SR)-2'-carboxy-3'-ethylcyclopropyl-2-(9-xanthylmethyl)glycine
Clinical data
Legal status ?
Identifiers
ATC code ?
PubChem CID 44329042
ChemSpider 28190823 N
Chemical data
Formula C22H23NO5 
Mol. mass 381.421 g/mol
 N (what is this?)  (verify)

CECXG (3'-ethyl-LY-341,495) is a research drug which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), with reasonable selectivity for mGluR3. While it is some five times less potent than LY-341,495 at mGluR3, it has 38x higher affinity for mGluR3 over mGluR2,[1] making it one of the few ligands available that is able to distinguish between these two closely related receptor subtypes.[2][3][4]


References[edit]

  1. ^ Collado I, Ezquerra J, Mazón A, Pedregal C, Yruretagoyena B, Kingston AE, Tomlinson R, Wright RA, Johnson BG, Schoepp DD (October 1998). "2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors". Bioorganic & Medicinal Chemistry Letters 8 (20): 2849–54. doi:10.1016/S0960-894X(98)00510-1. PMID 9873635. 
  2. ^ Jan Egebjerg, Povl Krogsgaard-Larsen, Arne Schousboe. Glutamate and gaba receptors and transporters: structure, function and pharmacology. pp 171-173. Taylor & Francis, 2002. ISBN 0-7484-0881-9
  3. ^ Sørensen, U. (2003). "Synthesis and Structure–Activity Relationship Studies of Novel 2-Diarylethyl Substituted (2-Carboxycycloprop-1-yl)glycines as High-Affinity Group II Metabotropic Glutamate Receptor Ligands". Bioorganic & Medicinal Chemistry 11: 197–205. doi:10.1016/S0968-0896(02)00387-5.  edit
  4. ^ Ure, J.; Baudry, M.; Perassolo, M. (2006). "Metabotropic glutamate receptors and epilepsy". Journal of the neurological sciences 247 (1): 1–9. doi:10.1016/j.jns.2006.03.018. PMID 16697014.  edit