S 38093

Biological Activity

S 38093 is a H₃ antagonist and inverse agonist (K_i 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 (K_B = 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. S 38093, a histamine H₃ antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice.
   Guilloux et al.
   Sci.Rep., 2017;7:42946
2. Effects of S 38093, an antagonist/inverse agonist of histamine H₃ receptors, in models of neuropathic pain in rats.
   Chaumette et al.
   Eur.J.Pain., 2018;22:127
3. Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists.
   Riddy et al.
   Neuropharmacology, 2019;144:244

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