To investigate the excitatory effects of Hydroxy-α-sanshool on central neurons, it was found to excite cerebellar granule neurons by inhibiting KCNK channels
Nat Neurosci. 2008 Jul;11(7):772-9
Mouse trigeminal ganglion neurons
100 μM
To investigate the excitatory effects of Hydroxy-α-sanshool on sensory neurons, it was found to excite neurons by inhibiting pH- and anesthetic-sensitive two-pore potassium channels (KCNK3, KCNK9, and KCNK18)
Nat Neurosci. 2008 Jul;11(7):772-9
HEK293 cells expressing TRPV1
1.1 μM (EC50)
To determine the activation effect of a-SOH on TRPV1, results showed that a-SOH effectively activated TRPV1 channels
Br J Pharmacol. 2009 Aug;157(8):1398-409
HEK293 cells expressing TRPA1
69 μM (EC50)
To determine the activation effect of a-SOH on TRPA1, results showed that a-SOH effectively activated TRPA1 channels
Br J Pharmacol. 2009 Aug;157(8):1398-409
dorsal root ganglia neurons
500 μM
5 seconds
To evaluate the activation of TRPA1 and TRPV1 channels by a-SOH, results showed that a-SOH activated neurons expressing TRPA1 and TRPV1
Br J Pharmacol. 2009 Aug;157(8):1398-409
Chinese hamster ovary cells (expressing human Nav1.1, 1.2, 1.3, 1.6, 1.7, or 1.8)
200 μM
To study the inhibitory effect of sanshool on different sodium channel subtypes, it was found that Nav1.7 and Nav1.3 currents were most significantly inhibited.
J Physiol. 2013 Jul 1;591(13):3325-40
Dorsal root ganglion (DRG) neurons
200 μM
To investigate the effect of sanshool on the electrical excitability of DRG neurons, it was found that sanshool completely inhibited AP firing in 35% of neurons and significantly reduced AP amplitude in another 29% of neurons.
J Physiol. 2013 Jul 1;591(13):3325-40
HepG2 cells
2.5, 5, 10 μg/ml
24 hours
HAS significantly increased glucose uptake and glycogen synthesis in GlcN-induced HepG2 cells and activated the PI3K/Akt pathway, increased GSK-3β phosphorylation, suppressed phosphorylation of glycogen synthase (GS), and increased glycogen synthesis in liver cells.
Front Pharmacol. 2022 Dec 13;13:1089558
trigeminal ganglion neurons
100 μM
To study the excitatory effects of sanshool on trigeminal ganglion neurons, finding that some neurons were excited by sanshool.
J Neurosci. 2010 Mar 24;30(12):4353-61
dorsal root ganglion neurons
100 μM
To study the excitatory effects of sanshool on dorsal root ganglion neurons, finding that 52% of neurons were excited by sanshool.
World J Gastroenterol. 2018 Sep 21;24(35):4036-4053
Hydroxy-α-sanshool/羟基-α-山椒素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Kunming mice
Insulin resistance model
Intragastric administration
8 mg/kg·bw
Once daily for 28 days
To explore the hydroxy-alpha-sanshool (HAS) effects on the intestinal metabolites of insulin-resistant mice, the results showed that HAS intervention significantly decreased GSP, GHb, TG, and TC levels, improved gut microbiota and metabolite composition.
Foods. 2022 Jul 10;11(14):2040
Mice
TRPV1 TRPA1 double-knockout mice
Oral
1 mM
3 hours per day for 7 days
To investigate the behavioral effects of Hydroxy-α-sanshool in mice, it was found that double-knockout and wild-type mice showed the same aversion to Hydroxy-α-sanshool, indicating that TRPV1 and TRPA1 channels are not involved in its action
Nat Neurosci. 2008 Jul;11(7):772-9
Mice
TRPV1 knockout mice
Brief-access taste test
500 μM and 1 mM
30 min testing periods
To evaluate the aversive response to a-SOH, results showed that TRPV1 KO mice exhibited significantly reduced aversion to a-SOH
Br J Pharmacol. 2009 Aug;157(8):1398-409
Kunming male mice
High-fat and high-glucose diet-induced insulin resistance model
Gavage
High-dose group 12 mg/(kg·d·bw), medium-dose group 8 mg/(kg·d·bw), low-dose group 4 mg/(kg·d·bw)
Daily administration for 28 days
HAS significantly reduced fasting blood glucose, promoted insulin secretion, decreased levels of inflammatory factors, and improved hepatic steatosis.
Mol Med. 2025 Feb 21;31(1):76
C57BL/6J mice
DSS-induced ulcerative colitis model
Gavage
2.5 mg/kg/d
Once daily for 7 days
Alleviate colitis symptoms, restore intestinal barrier function, and modulate gut microbiota
Antioxidants (Basel). 2024 Jan 25;13(2):153
Mice
Neurogenic inflammation model
Topical application
50 mM (5 μL applied to the hindpaw)
Single application, effects tested 30-60 minutes post-application
To investigate the effect of sanshool on mechanical and thermal pain sensitivity, it was found that sanshool selectively attenuated mechanical hypersensitivity but had no effect on thermal sensitivity.
J Physiol. 2013 Jul 1;591(13):3325-40
C57BL/6 J mice
High-fat diet and streptozotocin (STZ)-induced type 2 diabetic mouse model
Oral
1.25, 2.5, 5 mg/kg
Once daily for 4 weeks
HAS significantly reduced fasting blood glucose, alleviated pathological changes in the liver and pancreas, increased liver glycogen content, and improved hepatic insulin resistance and increased hepatic glycogen synthesis by activating the PI3K/Akt/GSK-3β/GS signaling pathway.
Front Pharmacol. 2022 Dec 13;13:1089558
C57BL/6 mice
Drinking water
1 mM
3 h every 24 h for 4-5 days
To study the effects of sanshool on drinking behavior in mice, finding that sanshool significantly reduced water consumption.
J Neurosci. 2010 Mar 24;30(12):4353-61
Sprague Dawley (SD) rats
Oral administration
10 mg/kg
Single dose
To study the pharmacokinetic properties of HAS in rats, results showed that HAS was rapidly absorbed in rats with a Tmax of 0.75 h, Cmax of 1253 ng/mL, and T1/2 of 1.02 h.
Toxics. 2024 Jan 24;12(2):100
Hydroxy-α-sanshool/羟基-α-山椒素 实验方案
计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.80mL
0.76mL
0.38mL
18.98mL
3.80mL
1.90mL
37.97mL
7.59mL
3.80mL
Hydroxy-α-sanshool/羟基-α-山椒素 技术信息
CAS号
83883-10-7
分子式
C16H25NO2
分子量
263.38
SMILES Code
C\C=C\C=C\C=C/CC\C=C\C(=O)NCC(C)(C)O
MDL No.
MFCD17779317
别名
运输
蓝冰
InChI Key
LHFKHAVGGJJQFF-UEOYEZOQSA-N
Pubchem ID
10084135
存储条件
In solvent-20°C:3-6个月-80°C:12个月
Pure formInert atmosphere, store in freezer, under -20°C
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