Pilocarpine Hydrochloride (Synonyms: 鹽酸毛果蕓香堿)

Pilocarpine Hydrochloride 是一種有效的 M3 型毒蕈堿乙酰dan堿受體 (M3 muscarinic receptor) 激動劑。

生物活性

Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

IC₅₀ & Target

M3 muscarinic receptor^[1]

體外研究(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].

體內(nèi)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 號：54-71-7

中文名稱：匹魯卡品鹽酸鹽；鹽酸毛果蕓香堿

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

4°C, sealed storage, away from moisture

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)

參考文獻

[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：產(chǎn)品僅用于科研