Carbenoxolone Sodium

Carbenoxolone induces astrocytes a reversible suppression of spontaneous action potential discharges, synaptic currents and synchronised calcium oscillations. Carbenoxolone inhibits oscillatory activity induced by the GABAA antagonist, bicuculline.Carbenoxolone causes an increase in the action potential threshold and strongly decreases the firing rate in response to a sustained depolarising current in astrocytes. ^[1] Carbenoxolone (100 μM) reduces photoreceptor-to-horizontal cell synaptic transmission by 92% in the Retina. Carbenoxolone (100 μM) reduces cone Ca channel current by 37%, reduces depolarization-evoked [Ca²⁺] signals in fluo-4 loaded retinal slices by 57% and inhibits Ca channels in Müller cells by 52% in the Retina. ^[2] Carbenoxolone abolishes the generation of full or partial ectopic spike generation, as well as spontaneous epileptiform activity in CA3 or CA1 regions of the rat hippocampal slices via closing GJ channels. ^[3]

Carbenoxolone (400 mg/kg) decreases the duration of seizure producing protection against seizure but failing to protect against mortality.Carbenoxolone significantly increases sleeping time and decreased latency in doses of 100 mg/kg, 200 mg/kg and 300 mg/kg in mice dose dependently. Carbenoxolone (400 mg/kg) shows muscle relaxant activity and in the accelerated rotarod test, Carbenoxolone in doses of 200 mg/kg and 300 mg/kg shows a decline in motor coordination. ^[3] Carbenoxolone (12.5 mg/day) leads to a significant reduction in average birth weight (20% fall) in rats. ^[4] Carbenoxolone treatment lowers birthweight and induces hypertension in the offspring of rats fed a protein-replete diet. ^[5]