LSP2-9166

LSP2-9166
LSP2-9166
LSP2-9166 structure.png
식별자
  • (2S)-2-아미노-4-[[[4-(카르복시메톡시)-3-(트리플루오로메톡시)페닐]-히드록시메틸]-히드록시포스포릴]부탄산
PubChem CID
켐스파이더
화학 및 물리 데이터
공식C14H17F3NO9P
몰 질량431.257 g/120−1
3D 모델(JSmol)
  • C1=CC(=C(C=C1C(O)P(=O)(CC[C@H](=O)N)O)OC(F)OC(=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)221-2,13,23,13,23
  • 키: NTRJZUQSIKLO-OADYLZGLSA-N

LSP2-9166은 mGluR에서4 70nM, mGluR에서7 220nM의 상당히 강력한50 EC를 가지며 mGluR에서6 1380NM, [1]mGluR에서8 4800NM의 약한 활성을 가지는 III족 메타고트로픽 글루탐산 수용체의 선택적 작용제 역할을 하는 약물이다.그것은 [2][3]동물 연구에서 항경련 효과가 있고, 다양한 [4][5][6]중독성 약물의 자가 투여를 감소시킨다.


레퍼런스

  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). 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.


Stub icon

신경계에 관한 이 약물 기사는 엉터리이다.위키피디아를 확장함으로써 위키피디아를 도울 수 있습니다.