In cellular models, S 38093 was able to antagonize mice H3 receptors (KB=0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11µM).
In vivo, S 38093 (0.3 and 3 mg/kg/d p.o., 28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice. In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3 mg/kg p.o. and antagonized R-α-Methylhistamine-induced dipsogenia from 10 mg/kg i.p..
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 9 mg/mL (Need warming and ultrasonic)|
Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats.
Chaumette T, et al. Eur J Pain. 2018 Jan;22(1):127-141. PMID: 28877402.
Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors.
Sors A, et al. Eur J Pharmacol. 2017 May 15;803:11-23. PMID: 28336400.
S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice.
Guilloux JP, et al. Sci Rep. 2017 Feb 20;7:42946. PMID: 28218311.
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