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5-Iodowillardiine

From Wikipedia, the free encyclopedia
5-Iodowillardiine
Names
IUPAC name
(2S)-2-Amino-3-(5-iodo-2,4-dioxopyrimidin-1-yl)propanoic acid
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
  • InChI=1S/C7H8IN3O4/c8-3-1-11(2-4(9)6(13)14)7(15)10-5(3)12/h1,4H,2,9H2,(H,13,14)(H,10,12,15)/t4-/m0/s1 checkY
    Key: AXXYLTBQIQBTES-BYPYZUCNSA-N checkY
  • InChI=1/C7H8IN3O4/c8-3-1-11(2-4(9)6(13)14)7(15)10-5(3)12/h1,4H,2,9H2,(H,13,14)(H,10,12,15)/t4-/m0/s1
    Key: AXXYLTBQIQBTES-BYPYZUCNBL
  • C1=C(C(=O)NC(=O)N1C[C@@H](C(=O)O)N)I
  • O=C(O)[C@@H](N)CN1/C=C(/I)C(=O)NC1=O
Properties
C7H8IN3O4
Molar mass325.061 g/mol
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)
Chemical compound

5-Iodowillardiine is a selectiveagonist for somekainate receptor subunits with only limited effects atAMPA receptors.[1] It activates kainate receptors containing GluK1 (GluR5) or GluK5 (KA2) subunits, but it does not act on GluK2 (GluR6) subunits.[2][3][4][5] It is anexcitotoxicneurotoxinin vivo,[6][7] but has proved highly useful for characterising the subtypes and function of the various kainate receptors in thebrain andspinal cord.[8][9][10]

References

[edit]
  1. ^Patneau, DK; Mayer, ML; Jane, DE; Watkins, JC (1992)."Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine".Journal of Neuroscience.12 (2):595–606.doi:10.1523/jneurosci.12-02-00595.1992.PMC 6575614.PMID 1371315.
  2. ^Swanson, GT; Green, T; Heinemann, SF (1998). "Kainate receptors exhibit differential sensitivities to (S)-5-iodowillardiine".Molecular Pharmacology.53 (5):942–9.doi:10.1016/S0026-895X(24)13262-2.PMID 9584222.
  3. ^Cui, C; Mayer, ML (1999)."Heteromeric kainate receptors formed by the coassembly of GluR5, GluR6, and GluR7".Journal of Neuroscience.19 (19):8281–91.doi:10.1523/JNEUROSCI.19-19-08281.1999.PMC 6782997.PMID 10493729.
  4. ^Alt, A.; Weiss, B.; Ogden, A.M.; Knauss, J.L.; Oler, J.; Ho, K.; Large, T.H.; Bleakman, D. (2004)."Pharmacological characterization of glutamatergic agonists and antagonists at recombinant human homomeric and heteromeric kainate receptors in vitro".Neuropharmacology.46 (6):793–806.doi:10.1016/j.neuropharm.2003.11.026.PMID 15033339.
  5. ^Pollok, S.; Reiner, A. (2020)."Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization".Proceedings of the National Academy of Sciences.117 (41):25851–25858.Bibcode:2020PNAS..11725851P.doi:10.1073/pnas.2007471117.PMC 7568280.PMID 32999066.
  6. ^Moldrich, RX; Cheung, NS; Pascoe, CJ; Beart, PM (1999). "Excitotoxic injury profiles of low-affinity kainate receptor agonists in cortical neuronal cultures".European Journal of Pharmacology.378 (2): R1–3.doi:10.1016/S0014-2999(99)00456-2.PMID 10478637.
  7. ^Moldrich, RX; Beart, PM; Pascoe, CJ; Cheung, NS (2000). "Low-affinity kainate receptor agonists induce insult-dependent apoptosis and necrosis in cultured murine cortical neurons".Journal of Neuroscience Research.59 (6):788–96.doi:10.1002/(SICI)1097-4547(20000315)59:6<788::AID-JNR11>3.0.CO;2-K.PMID 10700016.S2CID 21898801.
  8. ^Mascias, P; Scheede, M; Bloms-Funke, P; Chizh, B (2002). "Modulation of spinal nociception by GluR5 kainate receptor ligands in acute and hyperalgesic states and the role of gabaergic mechanisms".Neuropharmacology.43 (3):327–39.doi:10.1016/S0028-3908(02)00112-0.PMID 12243762.S2CID 29126134.
  9. ^Alt, A; Weiss, B; Ogden, AM; Knauss, JL; Oler, J; Ho, K; Large, TH; Bleakman, D (2004). "Pharmacological characterization of glutamatergic agonists and antagonists at recombinant human homomeric and heteromeric kainate receptors in vitro".Neuropharmacology.46 (6):793–806.doi:10.1016/j.neuropharm.2003.11.026.PMID 15033339.S2CID 23514969.
  10. ^Jane, DE; Lodge, D; Collingridge, GL (2009). "Kainate receptors: pharmacology, function and therapeutic potential".Neuropharmacology.56 (1):90–113.doi:10.1016/j.neuropharm.2008.08.023.PMID 18793656.S2CID 25291377.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
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