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]
[edit] References
- ^ 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.
- ^ Jan Egebjerg, Povl Krogsgaard-Larsen, Arne Schousboe. Glutamate and gaba receptors and transporters: structure, function and pharmacology. pp 171-173. Taylor & Francis, 2002. ISBN 0748408819
- ^ 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
- ^ 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
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Agonists: Glutamate/acite site competitive agonists: Aspartate • Glutamate • Homoquinolinic acid • Ibotenic acid • NMDA • Quinolinic acid • Tetrazolylglycine; Glycine site agonists: ACBD • ACPC • ACPD • Alanine • CCG • Cycloserine • DHPG • Fluoroalanine • Glycine • HA-966 • L-687,414 • Milacemide • Sarcosine • Serine • Tetrazolylglycine; Polyamine site agonists: Acamprosate • Spermidine • Spermine
Antagonists: Competitive antagonists: AP5 (APV) • AP7 • CGP-37849 • CGP-39551 • CGP-39653 • CGP-40116 • CGS-19755 • CPP • LY-233,053 • LY-235,959 • LY-274,614 • MDL-100,453 • Midafotel (d-CPPene) • NPC-12,626 • NPC-17,742 • PBPD • PEAQX • Perzinfotel • PPDA • SDZ-220581 • Selfotel; Noncompetitive antagonists: ARR-15,896 • Caroverine • Dexanabinol • FPL-12495 • FR-115,427 • Hodgkinsine • Magnesium • MDL-27,266 • NPS-1506 • Psychotridine • Zinc; Uncompetitive pore blockers: 2-MDP • 3-MeO-PCP • 8A-PDHQ • Alaproclate • Amantadine • Aptiganel • ARL-12,495 • ARL-15,896-AR • ARL-16,247 • Budipine • Delucemine • Dexoxadrol • Dextrallorphan • Dieticyclidine • Dizocilpine • Endopsychosin • Esketamine • Etoxadrol • Eticyclidine • Gacyclidine • Ibogaine • Indantadol • Ketamine • Ketobemidone • Loperamide • Memantine • Meperidine (Pethidine) • Methadone • Methorphan ( Dextromethorphan, Levomethorphan) • Methoxetamine • Milnacipran • Morphanol ( Dextrorphan, Levorphanol) • NEFA • Neramexane • Nitrous oxide • Noribogaine • Orphenadrine • PCPr • Phencyclamine • Phencyclidine • Propoxyphene • Remacemide • Rhynchophylline • Riluzole • Rimantadine • Rolicyclidine • Sabeluzole • Tenocyclidine • Tiletamine • Tramadol • Xenon; Glycine site antagonists: ACEA-1021 • ACEA-1328 • ACPC • Carisoprodol • CGP-39653 • CKA • DCKA • Felbamate • Gavestinel • GV-196,771 • Kynurenic acid • L-689,560 • L-701,324 • Lacosamide • Licostinel • LU-73,068 • MDL-105,519 • Meprobamate • MRZ 2/576 • PNQX • ZD-9379; NR2B subunit antagonists: Besonprodil • CO-101,244 (PD-174,494) • CP-101,606 • Eliprodil • Haloperidol • Ifenprodil • Isoxsuprine • Nylidrin • Ro8-4304 • Ro25-6981 • Traxoprodil; Polyamine site antagonists: Arcaine • Co 101676 • Diaminopropane • Acamprosate • Diethylenetriamine • Huperzine A • Putrescine • Ro 25-6981; Unclassified/unsorted antagonists: Chloroform • Diethyl ether • Enflurane • Ethanol (Alcohol) • Halothane • Isoflurane • Methoxyflurane • Toluene • Trichloroethane • Trichloroethanol • Trichloroethylene • Xylene
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Transporter
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