Chemical Name: rel-4-[3-[(3aR,6aS)-Hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy]benzamide
Biological ActivityH3 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice.
Guilloux et al.
Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats.
Chaumette et al.
Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists.
Riddy et al.
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