Chemistry:LSP2-9166

From HandWiki
Short description: Chemical compound
LSP2-9166
LSP2-9166 structure.png
Identifiers
PubChem CID
ChemSpider
Chemical and physical data
FormulaC14H17F3NO9P
Molar mass431.257 g·mol−1
3D model (JSmol)

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. "Metabotropic glutamate receptor orthosteric ligands and their binding sites". Neuropharmacology 204: 108886. February 2022. doi:10.1016/j.neuropharm.2021.108886. PMID 34813860. 
  2. "The mGlu7 receptor provides protective effects against epileptogenesis and epileptic seizures". Neurobiology of Disease 129: 13–28. September 2019. doi:10.1016/j.nbd.2019.04.016. PMID 31051234. 
  3. "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. March 2022. doi:10.3390/ijms23052752. PMID 35269897. 
  4. "Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist". Neuropharmacology 131: 424–430. March 2018. doi:10.1016/j.neuropharm.2018.01.002. PMID 29307544. 
  5. "Pharmacological activation of mGlu4 and mGlu7 receptors, by LSP2-9166, reduces ethanol consumption and relapse in rat". Neuropharmacology 133: 163–170. May 2018. doi:10.1016/j.neuropharm.2018.01.031. PMID 29378211. 
  6. "LSP2-9166, an orthosteric mGlu4 and mGlu7 receptor agonist, reduces cocaine self-administration under a progressive ratio schedule in rats". Neuroscience Letters 764: 135603. November 2021. doi:10.1016/j.neulet.2020.135603. PMID 33387661. https://hal.archives-ouvertes.fr/hal-03359144/file/islandora_120558.pdf.