LSP2-9166

LSP2-9166
识别信息
	IUPAC命名法 (2S)-2-amino-4-[[[4-(carboxymethoxy)-3-(trifluoromethoxy)phenyl]-hydroxymethyl]-hydroxyphosphoryl]butanoic acid; ;
CAS号	1413405-60-3
PubChem CID	71042034;
ChemSpider	98651888;
化学信息
化学式	C14H17F3NO9P
摩尔质量	431.26 g·mol−1
3D模型（JSmol）	交互式图像;
	SMILES C1=CC(=C(C=C1C(O)P(=O)(CC[C@@H](C(=O)O)N)O)OC(F)(F)F)OCC(=O)O;
	InChI 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是一种选择性III型代谢型谷氨酸受体激动剂，对mGluR4（英语：Metabotropic glutamate receptor 4）的EC₅₀为70nM，对mGluR7（英语：Metabotropic glutamate receptor 7）的EC₅₀为220nM，对mGluR6（英语：Metabotropic glutamate receptor 6）的EC₅₀为1380nM，对mGluR8（英语：Metabotropic glutamate receptor 8）的EC₅₀为4800nM^[1]。在动物研究中，该化合物具有抗癫痫（英语：Anticonvulsant）作用^[2]^[3]，并能减少各种成瘾性药物的自身给药^[4]^[5]^[6]。

参考文献

^ Acher FC, Cabayé A, Eshak F, Goupil-Lamy A, Pin JP. Metabotropic glutamate receptor orthosteric ligands and their binding sites. Neuropharmacology. 2022-02, 204. PMID 34813860. doi:10.1016/j.neuropharm.2021.108886 .
^ Girard B, Tuduri P, Moreno MP, Sakkaki S, Barboux C, Bouschet T, et al. The mGlu7 receptor provides protective effects against epileptogenesis and epileptic seizures. Neurobiology of Disease. 2019-09, 129: 13–28. PMID 31051234. doi:10.1016/j.nbd.2019.04.016 .
^ Kovalenko AA, Zakharova MV, Schwarz AP, Dyomina AV, Zubareva OE, Zaitsev AV. Changes in Metabotropic Glutamate Receptor Gene Expression in Rat Brain in a Lithium-Pilocarpine Model of Temporal Lobe Epilepsy. International Journal of Molecular Sciences. 2022-03, 23 (5): 2752. PMC 8910969 . PMID 35269897. doi:10.3390/ijms23052752 .
^ Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N. Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist. Neuropharmacology. 2018-03, 131: 424–430. PMID 29307544. S2CID 3391450. doi:10.1016/j.neuropharm.2018.01.002.
^ Lebourgeois S, Vilpoux C, Jeanblanc J, Acher F, Marie N, Noble F, Naassila M. Pharmacological activation of mGlu4 and mGlu7 receptors, by LSP2-9166, reduces ethanol consumption and relapse in rat. Neuropharmacology. 2018-05, 133: 163–170. PMID 29378211. S2CID 3959313. doi:10.1016/j.neuropharm.2018.01.031.
^ De Sa Nogueira D, Bourdy R, Filliol D, Quessada C, McCort-Tranchepain I, Acher F, et al. LSP2-9166, an orthosteric mGlu4 and mGlu7 receptor agonist, reduces cocaine self-administration under a progressive ratio schedule in rats (PDF). Neuroscience Letters. 2021-11, 764 [2026-05-11]. PMID 33387661. S2CID 229724310. doi:10.1016/j.neulet.2020.135603. （原始内容存档 (PDF)于2022-07-01）.

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[pmid34813860-1] Acher FC, Cabayé A, Eshak F, Goupil-Lamy A, Pin JP. Metabotropic glutamate receptor orthosteric ligands and their binding sites. Neuropharmacology. 2022-02, 204. PMID 34813860. doi:10.1016/j.neuropharm.2021.108886 .

[2] Girard B, Tuduri P, Moreno MP, Sakkaki S, Barboux C, Bouschet T, et al. The mGlu7 receptor provides protective effects against epileptogenesis and epileptic seizures. Neurobiology of Disease. 2019-09, 129: 13–28. PMID 31051234. doi:10.1016/j.nbd.2019.04.016 .

[pmid35269897-3] Kovalenko AA, Zakharova MV, Schwarz AP, Dyomina AV, Zubareva OE, Zaitsev AV. Changes in Metabotropic Glutamate Receptor Gene Expression in Rat Brain in a Lithium-Pilocarpine Model of Temporal Lobe Epilepsy. International Journal of Molecular Sciences. 2022-03, 23 (5): 2752. PMC 8910969 . PMID 35269897. doi:10.3390/ijms23052752 .

[4] Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N. Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist. Neuropharmacology. 2018-03, 131: 424–430. PMID 29307544. S2CID 3391450. doi:10.1016/j.neuropharm.2018.01.002.

[5] Lebourgeois S, Vilpoux C, Jeanblanc J, Acher F, Marie N, Noble F, Naassila M. Pharmacological activation of mGlu4 and mGlu7 receptors, by LSP2-9166, reduces ethanol consumption and relapse in rat. Neuropharmacology. 2018-05, 133: 163–170. PMID 29378211. S2CID 3959313. doi:10.1016/j.neuropharm.2018.01.031.

[6] De Sa Nogueira D, Bourdy R, Filliol D, Quessada C, McCort-Tranchepain I, Acher F, et al. LSP2-9166, an orthosteric mGlu4 and mGlu7 receptor agonist, reduces cocaine self-administration under a progressive ratio schedule in rats (PDF). Neuroscience Letters. 2021-11, 764 [2026-05-11]. PMID 33387661. S2CID 229724310. doi:10.1016/j.neulet.2020.135603. （原始内容存档 (PDF)于2022-07-01）.

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