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1247-64-9

中文名稱 PREGNENOLONE MONOSULFATE
英文名稱 (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
CAS 1247-64-9
分子式 C21H32O5S
分子量 396.54
MOL 文件 1247-64-9.mol
1247-64-9 結(jié)構(gòu)式 1247-64-9 結(jié)構(gòu)式

基本信息

中文別名
糖酮硫酸鹽
化合物 T12536
英文別名
Pregnenolone sulfate
Pregnenolone sulphate
Pregnenolone monosulfate
DIJBBUIOWGGQOP-OZIWPBGVSA-N
Pregn-5-en-20-one, 3-(sulfooxy)-, (3β)-
3β-Hydroxy-5-pregnen-20-one monosulfate
Di[(pregn-5-en-20-one)-3-yl] =sulfate ester
(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
所屬類別
醫(yī)藥中間體:原料藥中間體

物理化學(xué)性質(zhì)

密度1.25±0.1 g/cm3(Predicted)
儲存條件Store at -20°C,stored under nitrogen
溶解度DMSO: 62.5 mg/mL (157.61 mM)
酸度系數(shù)(pKa)-3.51±0.18(Predicted)
形態(tài)Solid
顏色White to off-white
PREGNENOLONE MONOSULFATE價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-B1739PREGNENOLONE MONOSULFATE
Pregnenolone monosulfate
1247-64-95mg600元
2024/11/08HY-B1739PREGNENOLONE MONOSULFATE
Pregnenolone monosulfate
1247-64-910mM * 1mLin DMSO660元
2024/11/08HY-B1739PREGNENOLONE MONOSULFATE
Pregnenolone monosulfate
1247-64-910mg1000元

常見問題列表

生物活性
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) 是一種功能強大的神經(jīng)甾體,是包括甾體酮在內(nèi)的各種甾體激素的主要前體。Pregnenolone monosulfate 是大麻素 CB1 受體的信號傳導(dǎo)特異性抑制劑,抑制由 CB1 受體介導(dǎo)的四氫大麻酚 (THC) 的作用。Pregnenolone monosulfate 可以保護大腦免受大麻中毒。
靶點

CB1

Human Endogenous Metabolite

體外研究

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).

體內(nèi)研究

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.

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