UBP316

• CAT Number: I010615
• CAS Number: 936095-50-0
• Molecular Formula: C20H19N3O6S
• Molecular Weight: 429.45
• Purity: ≥95%
• Synonyms: 3-[[3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxopyrimidin-1-yl]methyl]-5-phenylthiophene-2-carboxylic acid
• 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

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].

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.
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