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CECXG

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
CECXG
Identifiers
  • 2-(1'SR,2'SR,3'SR)-2'-carboxy-3'-ethylcyclopropyl-2-(9-xanthylmethyl)glycine
CAS Number
PubChemCID
ChemSpider
Chemical and physical data
FormulaC22H23NO5
Molar mass381.428 g·mol−1
3D model (JSmol)
  • c4cccc2c4Oc3ccccc3C2CC(N)(C(O)=O)C1C(C(=O)O)C1CC
  • 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 ☒N
  • Key:NBAKIHCDPVZWRB-KQLBNOIASA-N ☒N
 ☒NcheckY (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 thanLY-341,495 at mGluR3, it has 38x higher affinity formGluR3 overmGluR2,[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, 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.
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
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