CECXG

CECXG
Identifiers
	IUPAC name 2-(1'SR,2'SR,3'SR)-2'-carboxy-3'-ethylcyclopropyl-2-(9-xanthylmethyl)glycine;
PubChem CID	44329042;
ChemSpider	28190823 ;
Chemical and physical data
Formula	C22H23NO5
Molar mass	381.428 g·mol−1
3D model (JSmol)	Interactive image;
	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 ;
	(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 (mGluR_2/3), 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

^ 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.
^ 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.
^ 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.
^ 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.

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[pmid9873635-1] 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.

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