UBP 282

UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96[1][2].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

IC50: 10.3 μM (fast component of the dorsal root-evoked ventral root potential (fDR-VRP))[1] pA2: 4.96 (Kainate<-induced depolarisations of dorsal roots)[1]

UBP-282 (3-CBW) is selective for AMPA- and GluR5-containing kainate receptors vs NMDA, mGlu and kainate receptors expressed on motor neurones[1][2]. UBP-282 (3-CBW), at a concentration of 200 μM, blocks AMPA evoked depolarizations on motoneurones while responses to equi-effective doses of NMDA and DHPG were relatively unaffected. In the presence of 200 μM UBP-282, a concentration that completely abolishes AMPA-evoked depolarizations on motoneurones and kainate-evoked responses on dorsal root, there is still a noticeable depolarization evoked by kainate on motoneurones[1].

On neonatal rat motoneurones UBP-282 (3-CBW) (200 μM) almost completely abolished responses to AMPA while responses to NMDA, kainate and DHPG were 101.6%, 39.4% and 110.5% of control, respectively. UBP-282 can therefore be used to isolate kainate receptor responses from those mediated by AMPA receptors[1].

[1]. Julia C A More, et al. The novel antagonist 3-CBW discriminates between kainate receptors expressed on neonatal rat motoneurones and those on dorsal root C-fibres. Br J Pharmacol. 2002 Dec;137(7):1125-33.

[2]. Julia C A More, et al. Structural requirements for novel willardiine derivatives acting as AMPA and kainate receptor antagonists. Br J Pharmacol. 2003 Mar;138(6):1093-100.