5-Iodowillardiine Explained

5-Iodowillardiine is a selective agonist for the kainate receptor, with only limited effects at the AMPA receptor.^[1] It is selective for kainate receptors composed of GluR5 subunits.^{[2] [3]} It is an excitotoxic neurotoxin in vivo,^{[4] [5]} but has proved highly useful for characterising the subtypes and function of the various kainate receptors in the brain and spinal cord.^{[6] [7] [8]}

Notes and References

1. Patneau . DK . Mayer . ML . Jane . DE . Watkins . JC . Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine . Journal of Neuroscience . 12 . 2 . 595–606 . 1992 . 1371315 . 10.1523/jneurosci.12-02-00595.1992 . 6575614 . free .
2. Swanson . GT . Green . T . Heinemann . SF . Kainate receptors exhibit differential sensitivities to (S)-5-iodowillardiine . Molecular Pharmacology . 53 . 5 . 942–9 . 1998 . 9584222 .
3. Cui . C . Mayer . ML . Heteromeric kainate receptors formed by the coassembly of GluR5, GluR6, and GluR7 . Journal of Neuroscience . 19 . 19 . 8281–91 . 1999 . 10493729 . 10.1523/JNEUROSCI.19-19-08281.1999 . 6782997 . free .
4. Moldrich . RX . Cheung . NS . Pascoe . CJ . Beart . PM . Excitotoxic injury profiles of low-affinity kainate receptor agonists in cortical neuronal cultures . European Journal of Pharmacology . 378 . 2 . R1–3 . 1999 . 10478637 . 10.1016/S0014-2999(99)00456-2.
5. Moldrich . RX . Beart . PM . Pascoe . CJ . Cheung . NS . Low-affinity kainate receptor agonists induce insult-dependent apoptosis and necrosis in cultured murine cortical neurons . Journal of Neuroscience Research . 59 . 6 . 788–96 . 2000 . 10700016 . 10.1002/(SICI)1097-4547(20000315)59:6<788::AID-JNR11>3.0.CO;2-K . 21898801 .
6. Mascias . P . Scheede . M . Bloms-Funke . P . Chizh . B . 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 . 2002 . 12243762 . 10.1016/S0028-3908(02)00112-0. 29126134 .
7. Alt . A . Weiss . B . Ogden . AM . Knauss . JL . Oler . J . Ho . K . Large . TH . Bleakman . D . Pharmacological characterization of glutamatergic agonists and antagonists at recombinant human homomeric and heteromeric kainate receptors in vitro . Neuropharmacology . 46 . 6 . 793–806 . 2004 . 15033339 . 10.1016/j.neuropharm.2003.11.026 . 23514969 .
8. Jane . DE . Lodge . D . Collingridge . GL . Kainate receptors: pharmacology, function and therapeutic potential . Neuropharmacology . 56 . 1 . 90–113 . 2009 . 18793656 . 10.1016/j.neuropharm.2008.08.023 . 25291377 .