Molecular Formula | C17H24N2O2 |
Molar Mass | 288.38 |
Density | 1.130±0.06 g/cm3(Predicted) |
Boling Point | 473.5±25.0 °C(Predicted) |
Solubility | DMSO: 15 mg/mL |
pKa | 16.34±0.50(Predicted) |
Storage Condition | 2-8°C |
In vitro study | In the cell model, S38093 was able to antagonize the mouse H3 receptor (KB = 0.65 μm) and inhibit the decrease of cAMP induced by H3 agonist (KB = 0.11 μm). Among the four histamine receptor subtypes, S38093 is selective for H3 receptors with weak binding affinity for H1, H2 and H4 receptors. |
In vivo study | S 38093 is a novel H3 receptor antagonist/inverse agonist that crosses the blood-brain barrier in 3-and 16-month-old mice, maturation and survival play a role. S38093 induces reversal of age-related effects on hippocampal brain-derived neurotrophic factor transcripts BDNF-IX, BDNF-IV, and BDNF-I in aging animal models. A neurogenesis-related "context dissection test" was performed in aged mice to observe the effect of long-term administration of S38093 on mice: increasing age alters mouse CCS, long-term administration of S38093 will significantly improve CS, increase adult hippocampal neurogenesis, and provide innovative ideas for the treatment of age-related cognitive deficits. Mean drug concentrations of 0.3-1 mg/kg p.o/I. p were active in various behavioral tests in mice. S38093 improved attention, executive function and cognitive flexibility in MPTP-treated of monkeys. In addition, S38093 concentration-dependently increases extracellular histamine levels in the prefrontal cortex and promotes cholinergic transmission in the hippocampus and prefrontal cortex (rat). S38093 is rapidly absorbed in mice and rats (Tmax = 0.25-0.5h) and slower in monkeys (2h), with bioavailability ranging from 20-60%, the half-life was 1.5 h-7.4 h. After administration of S38093, it is widely distributed in the body, with a medium distribution volume and low protein binding rate. S38093 was rapidly distributed in brain tissue. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.468 ml | 17.338 ml | 34.676 ml |
5 mM | 0.694 ml | 3.468 ml | 6.935 ml |
10 mM | 0.347 ml | 1.734 ml | 3.468 ml |
5 mM | 0.069 ml | 0.347 ml | 0.694 ml |