PREGNENOLONE MONOSULFATE
| 中文名称 | PREGNENOLONE MONOSULFATE |
|---|---|
| 中文同义词 | 化合物 T12536;糖酮硫酸盐 |
| 英文名称 | (3S,8S,9R,10S,13S,14R,17R)-17-acetyl-10,13-dimethyl-3-sulfooxy-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene |
| 英文同义词 | Pregnenolone sulfate;(3S,8S,9R,10S,13S,14R,17R)-17-acetyl-10,13-dimethyl-3-sulfooxy-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene;Di[(pregn-5-en-20-one)-3-yl] =sulfate ester;Pregnenolone sulphate;DIJBBUIOWGGQOP-OZIWPBGVSA-N;Pregnenolone monosulfate;3β-Hydroxy-5-pregnen-20-one monosulfate;Pregn-5-en-20-one, 3-(sulfooxy)-, (3β)- |
| CAS号 | 1247-64-9 |
| 分子式 | C21H32O5S |
| 分子量 | 396.54 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1247-64-9.mol |
| 结构式 |  |
PREGNENOLONE MONOSULFATE 性质
| 密度 | 1.25±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C,stored under nitrogen |
| 溶解度 | 二甲基亚砜：62.5 mg/mL（157.61 mM） |
| 酸度系数(pKa) | -3.51±0.18(Predicted) |
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CB1
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Human Endogenous Metabolite
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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).
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.