Pilocarpine Hydrochloride (Synonyms: 盐酸毛果芸香碱)
Pilocarpine Hydrochloride 是一种有效的 M3 型毒蕈碱乙酰dan碱受体 (M3 muscarinic receptor) 激动剂。
生物活性
Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
IC50 & Target
M3 muscarinic receptor[1]
体外研究(In Vitro)
To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls[2]. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM)[3].
体内研究(In Vivo)
The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na+ concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05)[1].
分子量：244.72
Formula：C11H17ClN2O2
CAS 号：54-71-7
中文名称：匹鲁卡品盐酸盐；盐酸毛果芸香碱
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：
4°C, sealed storage, away from moisture
*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
DMSO : 50 mg/mL (204.32 mM; Need ultrasonic)
H2O : ≥ 37 mg/mL (151.19 mM)
* "≥" means soluble, but saturation unknown.
| 浓度溶剂体积质量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0863 mL | 20.4315 mL | 40.8630 mL |
| 5 mM | 0.8173 mL | 4.0863 mL | 8.1726 mL |
| 10 mM | 0.4086 mL | 2.0432 mL | 4.0863 mL |
请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。
以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
- 1.
请依序添加每种溶剂： PBS
Solubility: 130 mg/mL (531.22 mM); Clear solution; Need ultrasonic
- 2.
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution
- 3.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution
- 4.
请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution
参考文献
[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93.
[2]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32.
[3]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11.
[4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52.
注：产品仅用于科研
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