| Bioactivity | 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]. | ||||||||||||
| Target | Kb: 1.4 nM (GluK1) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | UBP316 | ||||||||||||
| CAS | 936095-50-0 | ||||||||||||
| Formula | C20H19N3O6S | ||||||||||||
| Molar Mass | 429.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |