A selective antagonist of post-synaptic GABAB receptors (IC50 = 34uM) that can permeate the blood brain barrier. Exhibits about 10-fold lower affinity for pre-synaptic receptors. Blocks K+-evoked glycine exocytosis in mouse spinal cord and hippocampal nerve endings. Shown to antagonize the potentiating effect of L-baclofen on noradrenaline-induced stimulation of adenylate cyclase in rat cortex slices.
Primary Target:GABA-B
Primary Target IC50:34u
Solubility:H2O
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
