Molecular Formula | C21H31NaO5S |
Molar Mass | 418.52 |
Melting Point | 192°C(lit.) |
Solubility | methanol and water: 1.93 mg/mL |
Storage Condition | -20°C |
Physical and Chemical Properties | Bioactive Pregnenolone mono-sodium salt (3β-Hydroxy-5-pregnen-20-one mono-sodium salt) is a powerful neurosteroid that is the main precursor of various steroid hormones, including steroid ketones. Pregnenol mono-sulfate sodium salt is a cannabinoid CB1 receptor signaling-specific inhibitor that inhibits the effects of tetrahydrocannabinol (THC) mediated by the CB1 receptor. Pregnenolone mono sulfate sodium salt protects the brain from cannabis toxicity. |
Target | CB1 Human Endogenous Metabolite |
In vitro study | CB1 receptor stimulation increases brain Pregnenolone levels, which in turn exerts a negative feedback on the activity of the CB1 receptor antagonizing most of the known behavioral and somatic effects of THC. Pregnenolone likely acts as a signaling-specific negative allosteric modulator binding to a site distinct from that occupied by orthosteric ligands. Pregnenolone does not modify agonist binding but only agonist efficacy. The effect of THC is significantly attenuated when slices are pre-treated with Pregnenolone 100 nM (15.1±1.8 % of inhibition). These effects are likely due to a pre-synaptic action of Pregnenolone. Thus, Pregnenolone blocks the increase in paired-pulse ratio (PPR) induced by THC but does not modify either the amplitude or the decay time of miniature EPSC (mEPSC). |
In vivo study | Pregnenolone administration (2-6 mg/kg) blocks THC-induced food-intake in Wistar rats and in C57BL/6N mice, and blunts the memory impairment induced by THC in mice, but it does not modify these behaviors per se . Injections of Pregnenolone (2 and 4mg/kg) before each self-administration session reduce the intake of WIN 55,212-2 and reduce the break-point in a progressive ratio schedule. |
WGK Germany | 3 |