LSP2-9166

Last updated
LSP2-9166
LSP2-9166 structure.png
Identifiers
  • (2S)-2-amino-4-[[[4-(carboxymethoxy)-3-(trifluoromethoxy)phenyl]-hydroxymethyl]-hydroxyphosphoryl]butanoic acid
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C14H17F3NO9P
Molar mass 431.257 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 selective agonist for the group III metabotropic glutamate receptors, with a reasonably potent EC50 of 70nM at mGluR4 and 220nM at mGluR7, and weaker activity of 1380nM at mGluR6 and 4800nM at mGluR8. [1] It has anticonvulsant effects in animal studies, [2] [3] and reduces self-administration of various addictive drugs. [4] [5] [6]


References

  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.


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