GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 µM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-alpha, IL-6, IL-1beta, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-kappaB pathway activation by reducing IkappaBalpha and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage[1].
Molecular Weight:
408.36
Formula:
C18H31Cl2N3O3
Target:
5-HT Receptor,COX,GABA Receptor,IKK,Interleukin Related,NF-kappaB,NO Synthase,Reactive Oxygen Species (ROS),TNF Receptor
Application Notes:
MCE Product type: Reference compound
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