Overview
- More, J.C. et al. (2002) Br. J. Pharmacol. 137, 1125.
- More, J.C. et al. (2003) Br. J. Pharmacol. 138, 1093.
Alomone Labs UBP 282 inhibits GluA1 channels expressed in Xenopus oocytes.Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 10 µM and 100 µM UBP 282 (#U-110), as indicated (bars), at a holding potential of -60 mV.
- More, J.C. et al. (2002) Br. J. Pharmacol. 137, 1125.
- More, J.C. et al. (2003) Br. J. Pharmacol. 138, 1093.
- Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
- Perrais, D. et al. (2009) Neuropharmacology 56, 131.
- Orav, E. et al. (2017) eNeuro 4, 1.
UBP 282 (3-CBW) is a synthetic willardiine analogue that acts as an antagonist of AMPA and Kainate glutamate receptors. The compound fully inhibits AMPA-evoked responses in neonatal motoneurons at 200 µM and reduces the AMPA-mediated fast component of dorsal root-evoked ventral root potential with IC50 value of 10.3 µM1,2.
The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors that mediate fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity and learning and memory3,4.
Kainate receptors (KARs) are highly expressed in the developing brain, where they are tonically activated to modulate synaptic transmission, network excitability, and synaptogenesis5.
UBP 282 (#U-110) is a highly pure, synthetic, and biologically active compound.
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