5-HT6R/FAAH modulator 2

5-HT6R/FAAH modulator 2 (Compound 4c) potently binds to and antagonizes human 5-HT₆R with a pK_i of 7.24 and pKb of 7.00, while moderately inhibiting human recombinant FAAH with a pIC₅₀ of 5.47, and exhibits low affinity for off-target monoaminergic receptors^[1].
5-HT₆R/FAAH modulator 2 shows moderate metabolic stability in rat liver microsomes, with a half-life of 44 min and intrinsic clearance of 15.8 μL min⁻¹·mg⁻¹, and is metabolized primarily via sulfur oxidation^[1].
5-HT₆R/FAAH modulator 2 (0.8-20 μM; 1 h pre-incubation, 24 h co-incubation with okadaic acid) significantly preserves cell membrane integrity in okadaic acid-treated SH-SY5Y neuroblastoma cells^[1].
5-HT₆R/FAAH modulator 2 (10 μM) does not modulate β-amyloid aggregation^[1].
5-HT₆R/FAAH modulator 2 (10 μM; 1 h pre-incubation, 24 h co-incubation with glutamate) significantly protects HT-22 hippocampal neuronal cells from glutamate-induced toxicity, preserving membrane integrity and partially reducing caspase-3/7 activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.