Biological Activity
S 38093 is a H3 antagonist and inverse agonist (Ki values are 8.8, 1.2 and 1.44 μM, at rat, human and mouse, respectively). Exhibits no activity at other histaminergic receptors. Antagonizes agonist action at mouse H3 receptors (KB = 0.65 μM). Displays inverse agonist action in cells expressing a high H3 receptor density, (EC50 values are 9 and 1.7 μM, at human and rat H3 receptors, respectively). Exhibits antihyperalgesic effect in a mouse diabetic neuropathy model in vivo. Promotes hippocampal neurogenesis in a mouse Alzheimer's disease model. Antinociceptive and procognitive. Also σ1 receptor antagonist. Exhibits ~30-fold selecitivity for σ1 over H3 and occupies σ1 but not H3 receptors at procognitive does in mice.
