Carbenoxolone (disodium)

Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD^[1]. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication^[2]. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation. Carbenoxolone disodium inhibits Vaccinia virus replication. IC50 & Target: IC50: human 11β-HSD; bacterial 3α, 20β-HSD^[1]; gap junction; Vaccinia virus^[2] In Vitro: Carbenoxolone disodium (6-150 μM; pre-treatment 1 hour) inhibits Vaccinia virus (VACV) replication in a gap junction-independent in HaCaT cells, and it has toxicity effects on VACV-A5L-EGFP infected cells at 48 h^[2].
Carbenoxolone (30 μM; pre-treatment 1 hour) does not upregulate PP2A expression, but induces the late protein A27 expression in hacat cells^[2].
In Vivo: Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Diazepam) does not induce a muscle relaxant activity and shows muscle relaxant activity compared to normal saline, and this effect was more than diazepam in the traction test^[3].
Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Pentylenetetrazole) significantly increases sleeping time and decreases latency in mice as a dose-dependent manner in Pentylenetetrazole (PTZ) Seizure model. The ED₅₀ value is 83.3 mg/kg (%95 CL:556.29)^[3].