936095-50-0

936095-50-0 structure

Name: ACET
Chemical Name: 1(2H)-Pyrimidinepropanoic acid, α-amino-3-[(2-carboxy-5-phenyl-3-thienyl)methyl]-3,4-dihydro-5-methyl-2,4-dioxo-, (αS)
CAS Number: 936095-50-0
Molecular Formula: C₂₀H₁₉N₃O₆S
Molecular Weight: 429.44600
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2017-08-24 09:43:56
Modify Date: 2025-09-02 18:23:22
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].

Name	1(2H)-Pyrimidinepropanoic acid, α-amino-3-[(2-carboxy-5-phenyl-3-thienyl)methyl]-3,4-dihydro-5-methyl-2,4-dioxo-, (αS)
Synonyms	Arecaidine propargyl ester tosylate UPB 316

Description	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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> iGluR Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Target	Kb: 1.4 nM (GluK1)[1]
In Vitro	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].
References	[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.