Ensiklopedia Dunia

Technopedia Center

Faculty of Engineering and Computer Science
S1 Informatics S1 Information Systems S1 Information Technology S1 Computer Engineering S1 Electrical Engineering S1 Civil Engineering

faculty of Economics and Business
S1 Management S1 Accountancy

Faculty of Letters and Educational Sciences
S1 English literature S1 English language education S1 Mathematics education S1 Sports Education

CECXG - Wikipedia

From Wikipedia, the free encyclopedia

CECXG
Identifiers

IUPAC name 2-(1'SR,2'SR,3'SR)-2'-carboxy-3'-ethylcyclopropyl-2-(9-xanthylmethyl)glycine
PubChem CID	44329042
ChemSpider	28190823^N
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^N Key:NBAKIHCDPVZWRB-KQLBNOIASA-N^N
^NY (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.

Metabotropic glutamate receptor modulators

Group I

mGluR₁Tooltip Metabotropic glutamate receptor 1	Agonists: ACPD DHPG Glutamate Ibotenic acid Quisqualic acid Ro01-6128 Ro67-4853 Ro67-7476 VU-71 Theanine Antagonists: BAY 36-7620 CPCCOEt Cyclothiazide LY-367,385 LY-456,236 MCPG NPS-2390
mGluR₅Tooltip Metabotropic glutamate receptor 5	Agonists: ACPD ADX-47273 CDPPB CHPG DFB DHPG Glutamate Ibotenic acid Quisqualic acid VU-1545; Positive allosteric modulators: LSN2463359 Antagonists: CTEP DMeOB LY-344,545 Mavoglurant MCPG NPS-2390 Remeglurant SIB-1757 SIB-1893; Negative allosteric modulators: AZD9272 Basimglurant Dipraglurant Fenobam GRN-529 MPEP MTEP Raseglurant

Group II

mGluR₂

Agonists: BINA
CBiPES
DCG-IV
Eglumegad
Glutamate
Ibotenic acid
LY-379,268
LY-404,039 (pomaglumetad)
LY-487,379
LY-566,332
MGS-0028
Pomaglumetad methionil (LY-2140023)
Talaglumetad; Positive allosteric modulators: JNJ-40411813 (ADX-71149)

Antagonists: APICA
CECXG
EGLU
HYDIA
LY-307,452
LY-341,495
MCPG
MGS-0039
PCCG-4; Negative allosteric modulators: Decoglurant
RO4491533

mGluR₃

Antagonists: APICA
CECXG
EGLU
HYDIA
LY-307,452
LY-341,495
MCPG
MGS-0039; Negative allosteric modulators: Decoglurant
RO4491533

Group III

mGluR₄Tooltip Metabotropic glutamate receptor 4	Agonists: Glutamate L-AP4 LSP2-9166 PHCCC VU-001,171 VU-0155,041; Positive allosteric modulators: Foliglurax MPEP Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₆Tooltip Metabotropic glutamate receptor 6	Agonists: Glutamate L-AP4 Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₇Tooltip Metabotropic glutamate receptor 7	Agonists: AMN082 Glutamate L-AP4 LSP2-9166 Antagonists: CPPG MAP4 MMPIP MPPG MSOP MTPG UBP-1112 XAP044; Negative allosteric modulators: ADX71743
mGluR₈Tooltip Metabotropic glutamate receptor 8	Agonists: DCPG Glutamate L-AP4; Positive allosteric modulators: AZ12216052 Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112

See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

Categories:

Hidden categories: