For research use only. Not for therapeutic Use.
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist[1].
UBP316 is ineffective at GluK2 (GluR6) receptors at all concentrations tested (up to 100 μM) and had no effect at GluK3 (GluR7) when tested at 1 μM[1].
UBP316 (200 nM) reduces short-term facilitation of pre-synaptic calcium transients following repetitive spikes[1].
UBP316 effectively antagonises GluK1-mediated depression of excitatory transmission in CA1 region of the hippocampus in vitro[1].
UBP316 blocks induction of NMDA receptor-independent long-term potentiation (LTP)[1].
| Catalog Number | I010615 |
| CAS Number | 936095-50-0 |
| Synonyms | 3-[[3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxopyrimidin-1-yl]methyl]-5-phenylthiophene-2-carboxylic acid |
| Molecular Formula | C20H19N3O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C20H19N3O6S/c1-11-8-22(10-14(21)18(25)26)20(29)23(17(11)24)9-13-7-15(30-16(13)19(27)28)12-5-3-2-4-6-12/h2-8,14H,9-10,21H2,1H3,(H,25,26)(H,27,28)/t14-/m0/s1 |
| InChIKey | LCZDCKMQSBGXAH-AWEZNQCLSA-N |
| SMILES | CC1=CN(C(=O)N(C1=O)CC2=C(SC(=C2)C3=CC=CC=C3)C(=O)O)CC(C(=O)O)N |
| Reference | [1]. Sheila L Dargan, et al. ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology. 2009 Jan;56(1):121-30. |
