Pregnenolone sulfate (sodium salt)
(Synonyms: 3β-Hydroxy-5-pregnen-20-one monosulfate sodium) 目录号 : GC44680Pregnenolone sulfate (sodium salt)是一种孕烯醇酮的神经活性代谢产物，对氨基丁酸A型受体（GABAAR）的IC50值为26±2μmol/L，对不含γ亚基的GABAAR的IC50值为18±3μmol/L。
Cas No.:1852-38-6
Sample solution is provided at 25 µL, 10mM.
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Pregnenolone sulfate (sodium salt), a neuroactive metabolite of pregnenolone, exhibits the IC50 value of 26±2μmol/L for the aminobutyric acid type A receptor (GABAAR) and the IC50 value of 18±3μmol/L for GABAAR without the γ subunit[1]. Pregnenolone sulfate is a potent enhancer of intracellular Ca2+, with the EC50 value of 2pmol/L[2]. Pregnenolone sulfate has been used in neurological studies and seizure studies[3].
In vitro, Pregnenolone sulfate (200μmol/L) treatment for 24 hours significantly inhibited human T cell proliferation and viability[4]. Pregnenolone sulfate suppressed acetylcholine-induced catecholamine secretion (IC50=27μmol/L) and inhibited the Ca2+(IC50=20μmol/L) influx in bovine adrenal chromaffin cells after 10min treatment[5]. Pregnenolone sulfate (100μmol/L, 10 seconds) promoted NR1 movement to the cell surface in Xenopus laevis oocytes expressing NR1/NR2A a G protein-coupled pathway that requires both intracellular Ca2+ and phospholipase C activation[6].
In vivo, Pregnenolone sulfate (10mg/kg/day, s.c.) treatment for 4 days in adult male rats resulted in cognitive enhancement, with improvement in spatial orientation acquisition[7]. Subcutaneous injection of Pregnenolone sulfate (40mg/kg) for 30 minutes significantly shortened the immobility time and promoted the movement of male albino mice[8].
References:
[1] Sachidanandan D, Bera A K. Inhibition of the GABA A receptor by sulfated neurosteroids: a mechanistic comparison study between pregnenolone sulfate and dehydroepiandrosterone sulfate[J]. Journal of Molecular Neuroscience, 2015, 56: 868-877.
[2] Smith C C, Martin S C, Sugunan K, et al. A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation[J]. Molecular pharmacology, 2014, 86(4): 390-398.
[3] Williamson J, Mtchedlishvili Z, Kapur J. Characterization of the convulsant action of pregnenolone sulfate[J]. Neuropharmacology, 2004, 46(6): 856-864.
[4] El Hajj Y, Shahin T, Dieng M M, et al. Pregnenolone sulfate induces transcriptional and immunoregulatory effects on T cells[J]. Scientific reports, 2024, 14(1): 6782.
[5] Kudo K, Tachikawa E, Kashimoto T. Inhibition by pregnenolone sulfate of nicotinic acetylcholine response in adrenal chromaffin cells[J]. European journal of pharmacology, 2002, 456(1-3): 19-27.
[6] Kostakis E, Smith C, Jang M K, et al. The neuroactive steroid pregnenolone sulfate stimulates trafficking of functional N-methyl D-aspartate receptors to the cell surface via a noncanonical, G protein, and Ca2+-dependent mechanism[J]. Molecular pharmacology, 2013, 84(2): 261-274.
[7] Plescia F, Sardo P, Rizzo V, et al. Pregnenolone sulphate enhances spatial orientation and object discrimination in adult male rats: evidence from a behavioural and electrophysiological study[J]. Behavioural brain research, 2014, 258: 193-201.
[8] Dhir A, Kulkarni S K. Involvement of sigma (σ1) receptors in modulating the anti-depressant effect of neurosteroids (dehydroepiandrosterone or pregnenolone) in mouse tail-suspension test[J]. Journal of Psychopharmacology, 2008, 22(6): 691-696.
Pregnenolone sulfate (sodium salt)是一种孕烯醇酮的神经活性代谢产物，对氨基丁酸A型受体（GABAAR）的IC50值为26±2μmol/L，对不含γ亚基的GABAAR的IC50值为18±3μmol/L[1]。Pregnenolone sulfate能显著增强细胞内钙离子浓度，EC50值为2pmol/L[2]。Pregnenolone sulfate已被应用于神经学研究和癫痫发作研究领域[3]。
在体外，Pregnenolone sulfate（200μmol/L）处理24小时能显著抑制人类T细胞增殖和细胞活性[4]。Pregnenolone sulfate处理牛肾上腺嗜铬细胞10分钟后可抑制乙酰胆碱诱导的儿茶酚胺分泌（IC50=27μmol/L），并阻断Ca2+内流（IC50=20μmol/L）[5]。在表达NR1/NR2A的非洲爪蟾卵母细胞中，Pregnenolone sulfate（100μmol/L，10秒）通过依赖细胞内Ca2+和磷脂酶C激活的G蛋白偶联通路，促进NR1亚基向细胞膜表面转运[6]。
在体内，Pregnenolone sulfate（10mg/kg/day，皮下注射）连续给药4天可显著增强成年雄性大鼠的认知功能，并改善大鼠的空间定向学习能力[7]。皮下注射Pregnenolone sulfate（40mg/kg）30分钟后能显著缩短雄性白化小鼠的静止不动时间，并促进运动行为[8]。
| Cell experiment [1]: | |
Cell lines | Bovine adrenal chromaffin cells |
Preparation Method | Bovine adrenal chromaffin cells were mixed with Eagle's minimum essential medium and 10% calf serum and then added with antibiotics (100units/ml of penicillin, 100μg/ml of streptomycin and 0.3μg/ml of amphotericin B) plus 3μmol/L cytosine arabinoside before seeding cells on 35-mm diameter plastic culture dishes at 2×106cells per dish for monolayer culture. The cells needed for [3H]nicotine binding analysis were plated onto 24-well plates at 5×105cells per well. For four days the cells were kept at 37°C in a humidified incubator with 95% air and 5% CO2 atmosphere. 2×106cells contained 34.6±4.2μg of epinephrine and norepinephrine catecholamines combined. Following a 10-minute preincubation at 37°C in Krebs–Ringer–HEPES buffer (KRH buffer) with or without Pregnenolone sulfate (3-100μmol/L), the cells received further incubation in KRH buffer containing Ca2+ (37kBq) with or without Pregnenolone sulfate alongside either 50μmol/L acetylcholine or 56mmol/L K+ for 7 minutes. Following incubation medium removal, rapidly cool cells on ice before performing three washes with ice-cold KRH buffer lacking calcium but containing 10mmol/L LaCl3 and 2mmol/L EGTA. 10% Triton X-100 was added to the cells, which were then physically scraped off. The scintillation vials received the lysate mixed with scintillation fluid. The liquid scintillation counter measured the radioactivity levels. |
Reaction Conditions | 3-100μmol/L; 10min |
Applications | Pregnenolone sulfate (3-100μmol/L) significantly inhibited acetylcholine-induced Ca2+ influx in a concentration-dependent manner within bovine adrenal chromaffin cells. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Adult male Wistar rats were used as subjects for experimental procedures. Standard plastic cages held two animals each inside a room with controlled temperature at 22±2°C and humidity at 55±10%. The colony followed a 12-hour light-dark cycle from 8:00 to 20:00 while food and water remained accessible at all times. On the behavioral testing day, administer subcutaneously Pregnenolone sulfate at 10mg/kg to 16 rats, whilst another group of 16 rats received injections of vehicle consisting of 0.1% Tween 80. Pregnenolone sulfate dissolved in 0.1% Tween 80 was administered subcutaneously at a dose of 1ml/kg two hours before each experimental session to monitor minor inter-individual variability in effects. The control group received identical volume of vehicle at the same time. The rats entered the laboratory on test days and had at least a 60-minute acclimatization period before beginning experimental sessions. All experimental sessions took place in sound-isolated chambers from 8:00 to 14:00. A television camera in an adjacent room captured the animal's performance. All devices received a thorough cleaning before each animal introduction to eliminate any effects on behavior from the detection of another rat's scent by the test subject. |
Dosage form | 10mg/kg/day; s.c. |
Applications | Pregnenolone sulfate treatment in rats can exert cognitive enhancement, improving spatial orientation acquisition and object discrimination. |
References: | |
| Cas No. | 1852-38-6 | SDF | |
| 别名 | 3β-Hydroxy-5-pregnen-20-one monosulfate sodium | ||
| Canonical SMILES | C[C@]12C(C[C@@H](OS([O-])(=O)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC[C@@H]4C(C)=O.[Na+] | ||
| 分子式 | C21H31O5S•Na | 分子量 | 418.5 |
| 溶解度 | 30 mg/ml in DMSO(Need ultrasonic); 2 mg/ml in Ethanol. | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3895 mL | 11.9474 mL | 23.8949 mL |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.779 mL |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3895 mL |
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