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LSP2-9166

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
LSP2-9166
Identifiers
  • (2S)-2-amino-4-[[[4-(carboxymethoxy)-3-(trifluoromethoxy)phenyl]-hydroxymethyl]-hydroxyphosphoryl]butanoic acid
CAS Number
PubChemCID
ChemSpider
Chemical and physical data
FormulaC14H17F3NO9P
Molar mass431.257 g·mol−1
3D model (JSmol)
  • C1=CC(=C(C=C1C(O)P(=O)(CC[C@@H](C(=O)O)N)O)OC(F)(F)F)OCC(=O)O
  • InChI=1S/C14H17F3NO9P/c15-14(16,17)27-10-5-7(1-2-9(10)26-6-11(19)20)13(23)28(24,25)4-3-8(18)12(21)22/h1-2,5,8,13,23H,3-4,6,18H2,(H,19,20)(H,21,22)(H,24,25)/t8-,13?/m0/s1
  • Key:NTRJZUQSNSIKLO-OADYLZGLSA-N

LSP2-9166 is a drug which acts as a selectiveagonist for the group IIImetabotropic glutamate receptors, with a reasonably potent EC50 of 70nM atmGluR4 and 220nM atmGluR7, and weaker activity of 1380nM atmGluR6 and 4800nM atmGluR8.[1] It hasanticonvulsant effects in animal studies,[2][3] and reduces self-administration of various addictive drugs.[4][5][6]


References

[edit]
  1. ^Acher FC, Cabayé A, Eshak F, Goupil-Lamy A, Pin JP (February 2022)."Metabotropic glutamate receptor orthosteric ligands and their binding sites".Neuropharmacology.204 108886.doi:10.1016/j.neuropharm.2021.108886.PMID 34813860.
  2. ^Girard B, Tuduri P, Moreno MP, Sakkaki S, Barboux C, Bouschet T, et al. (September 2019)."The mGlu7 receptor provides protective effects against epileptogenesis and epileptic seizures".Neurobiology of Disease.129:13–28.doi:10.1016/j.nbd.2019.04.016.PMID 31051234.
  3. ^Kovalenko AA, Zakharova MV, Schwarz AP, Dyomina AV, Zubareva OE, Zaitsev AV (March 2022)."Changes in Metabotropic Glutamate Receptor Gene Expression in Rat Brain in a Lithium-Pilocarpine Model of Temporal Lobe Epilepsy".International Journal of Molecular Sciences.23 (5): 2752.doi:10.3390/ijms23052752.PMC 8910969.PMID 35269897.
  4. ^Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N (March 2018). "Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist".Neuropharmacology.131:424–430.doi:10.1016/j.neuropharm.2018.01.002.PMID 29307544.S2CID 3391450.
  5. ^Lebourgeois S, Vilpoux C, Jeanblanc J, Acher F, Marie N, Noble F, Naassila M (May 2018). "Pharmacological activation of mGlu4 and mGlu7 receptors, by LSP2-9166, reduces ethanol consumption and relapse in rat".Neuropharmacology.133:163–170.doi:10.1016/j.neuropharm.2018.01.031.PMID 29378211.S2CID 3959313.
  6. ^De Sa Nogueira D, Bourdy R, Filliol D, Quessada C, McCort-Tranchepain I, Acher F, et al. (November 2021)."LSP2-9166, an orthosteric mGlu4 and mGlu7 receptor agonist, reduces cocaine self-administration under a progressive ratio schedule in rats"(PDF).Neuroscience Letters.764 135603.doi:10.1016/j.neulet.2020.135603.PMID 33387661.S2CID 229724310.
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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