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CECXG

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Chemical compound Pharmaceutical compound
CECXG
Identifiers
IUPAC name
  • 2-(1'SR,2'SR,3'SR)-2'-carboxy-3'-ethylcyclopropyl-2-(9-xanthylmethyl)glycine
PubChem CID
ChemSpider
Chemical and physical data
FormulaC22H23NO5
Molar mass381.428 g·mol
3D model (JSmol)
SMILES
  • c4cccc2c4Oc3ccccc3C2CC(N)(C(O)=O)C1C(C(=O)O)C1CC
InChI
  • InChI=1S/C22H23NO5/c1-2-12-18(20(24)25)19(12)22(23,21(26)27)11-15-13-7-3-5-9-16(13)28-17-10-6-4-8-14(15)17/h3-10,12,15,18-19H,2,11,23H2,1H3,(H,24,25)(H,26,27)/t12-,18+,19+,22+/m1/s1
  • Key:NBAKIHCDPVZWRB-KQLBNOIASA-N
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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, making it one of the few ligands available that is able to distinguish between these two closely related receptor subtypes.

References

  1. Collado I, Ezquerra J, Mazón A, Pedregal C, Yruretagoyena B, Kingston AE, et al. (October 1998). "2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors". Bioorganic & Medicinal Chemistry Letters. 8 (20): 2849–2854. doi:10.1016/S0960-894X(98)00510-1. PMID 9873635.
  2. Schoepp DD, Jane DE, Monn JA (2002). "Pharmacology of metabotropic glutamate receptors". In Egebjerg J, Krogsgaard-Larsen P, Schousboe A (eds.). Glutamate and GABA receptors and transporters: structure, function and pharmacology. Taylor & Francis. pp. 171–173. ISBN 0-7484-0881-9.
  3. Sørensen US, Bleisch TJ, Kingston AE, Wright RA, Johnson BG, Schoepp DD, Ornstein PL (January 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 (2): 197–205. doi:10.1016/S0968-0896(02)00387-5. PMID 12470714.
  4. Ure J, Baudry M, Perassolo M (August 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. S2CID 22777207.
Metabotropic glutamate receptor modulators
Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
mGluR6Tooltip Metabotropic glutamate receptor 6
mGluR7Tooltip Metabotropic glutamate receptor 7
mGluR8Tooltip Metabotropic glutamate receptor 8
See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators
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