Pilocarpine HCl
(Synonyms: 盐酸毛果芸香碱) 目录号 : GC17256
A muscarinic acetylcholine receptor agonist
Cas No.:54-71-7
Sample solution is provided at 25 µL, 10mM.
Pilocarpine HCl is a miotic drug that acts as a M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist, causing ciliary muscle contraction that opens up the trabecular meshwork which allows aqueous humour drainage and a resultant reduction in IOP[1]. Pilocarpine HCl is a hydrophilic drug used for managing IOP in the treatment of glaucoma[2]
Pilocarpine HCl encapsulated by liposomes can keep their integrity and physicochemical properties for at least 15 month[3].Pilocarpine HCl specifically inhibits Candida albicans biofilm formation and pathogenicity through interaction with a muscarinic-like receptor[4]. Pilocarpine HCl has acaricidal activity on larvae (LC50=2.6 mg?mL-1) and engorged females (LC50=11.8 mg?mL-1) of R.(B.) microplus[5]
Pilocarpine HCl have apparent functional protective effects in xerostomia models: an increase in the volume of saliva without any change in salivary content. This prophylactic action of pilocarpine HCl may provide a new clinical treatment for irradiation xerostomia in patients with head and neck cancer[6]. Oral activity responses to pilocarpine HCl are enhanced in neonatal 6-OHDA-treated rats[7]
References:
[1]. Jain N, Verma A, et al. Formulation and investigation of pilocarpine hydrochloride niosomal gels for the treatment of glaucoma: intraocular pressure measurement in white albino rabbits. Drug Deliv. 2020;27(1):888-899.
[2]. Owodeha-Ashaka K, Ilomuanya MO, et al. Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery [published correction appears in Prog Biomater. 2021 Oct 5;:]. Prog Biomater. 2021;10(3):207-220.
[3]. Monem AS, Ali FM, et al. Prolonged effect of liposomes encapsulating pilocarpine HCl in normal and glaucomatous rabbits. Int J Pharm. 2000;198(1):29-38.
[4]. Nile C, Falleni M, et al. Repurposing Pilocarpine Hydrochloride for Treatment of Candida albicans Infections. mSphere. 2019;4(1):e00689-18. Published 2019 Jan 23.
[5]. Castro KN, Lima DF, et al. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus. Rev Bras Parasitol Vet. 2016;25(2):248-253.
[6]. Asari T, Komatsu Y, et al. Prophylactic effects of pilocarpine hydrochloride on xerostomia models induced by X-ray irradiation in rats. Clin Exp Pharmacol Physiol. 2001;28(7):545-550.
[7]. Kostrzewa RM, Neely D. Enhanced pilocarpine-induced oral activity responses in neonatal 6-OHDA treated rats. Pharmacol Biochem Behav. 1993;45(3):737-740.
盐酸毛果芸香碱是一种缩瞳药，作为 M3 型毒蕈碱型乙酰胆碱受体（M3 毒蕈碱受体）激动剂，引起睫状肌收缩，打开小梁网，允许房水排出，从而降低眼压 [1]。盐酸毛果芸香碱是一种亲水性药物，在治疗青光眼时用于控制眼压[2]
脂质体包封的盐酸毛果芸香碱可保持其完整性和理化性质至少 15 个月[3]。盐酸毛果芸香碱通过与毒蕈碱样受体相互作用特异性抑制白色念珠菌生物膜形成和致病性[4]。盐酸毛果芸香碱对幼虫(LC50=2.6 mg•mL-1)和饱食雌虫(LC50=11.8 mg•mL)具有杀螨活性-1) 的 R.(B.) microplus[5]
盐酸毛果芸香碱对口干症模型具有明显的功能性保护作用:唾液量增加而唾液含量没有任何变化。盐酸毛果芸香碱的这一预防作用可能为头颈癌患者的辐照口干症提供一种新的临床治疗方法[6]。新生 6-OHDA 处理的大鼠对盐酸毛果芸香碱的口腔活动反应增强[7]
| Cell experiment [1]: | |
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Cell lines |
C.albicans SC5314 |
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Preparation Method |
Standardized C. albicans SC5314 (1×106 cells/ml) were inoculated in RPMI with or without Pilocarpine HCl on Thermanox coverslips (13mm) within a 24-well tissue culture plate and then incubated for 24h at 37℃. |
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Reaction Conditions |
0-50mM |
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Applications |
Light microscopy revealed that Pilocarpine HCl inhibited filamentation and biofilm formation in a dose-dependent manner. Furthermore, visually, in the presence of increasing concentrations of Pilocarpine HCl, more C.albicans cells maintained a yeast morphology, suggesting that Pilocarpine HCl was inhibiting the yeast-to-hypha transition. Scanning electron microscopy analysis further confirmed the fact that Pilocarpine HCl inhibited biofilm formation due to inhibition of the yeast-to-hypha transition in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley rats, seven-week-old |
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Preparation Method |
Each rat was fasted overnight before the experiment, but had free access to drinking water. The rat was anaesthetized with urethane (1.25 g/kg, s.c.) and its body temperature was maintained at 37℃ during the subsequent experiment. After intubating the trachea, the duct of the right parotid gland was cannulated for the collection of saliva. Pilocarpine hydrochloride (0.05, 0.1, 0.2 or 0.4mg/kg in 1mL) or distilled water was administered intraduodenally and the saliva was collected for 120min after this administration |
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Dosage form |
0.05, 0.1, 0.2 or 0.4mg/kg in 1mL |
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Applications |
The mean salivary output for 120min without pilocarpine hydrochloride was 1.58±0.99μL (n=6). Pilocarpine hydrochloride (0.05-0.4mg/kg, intraduodenal) dose-dependently increased salivary output for 120 min in normal rats, the total volumes being 3.02±0.73 μL (0.05 mg/kg; n = 6), 3.91±0.50 μL (0.1 mg/kg; n = 6; P < 0.05 vs control), 5.74±0.99 μL (0.2 mg/kg; n = 6; P < 0.05 vs control) and 23.65±3.25 μL (0.4 mg/kg; n = 6; P < 0.05 vs control). |
|
References: [1]. Nile C, Falleni M, et al. Repurposing Pilocarpine Hydrochloride for Treatment of Candida albicans Infections. mSphere. 2019;4(1):e00689-18. Published 2019 Jan 23. [2]. Asari T, Komatsu Y, et al. Prophylactic effects of pilocarpine hydrochloride on xerostomia models induced by X-ray irradiation in rats. Clin Exp Pharmacol Physiol. 2001;28(7):545-550. |
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| Cas No. | 54-71-7 | SDF | |
| 别名 | 盐酸毛果芸香碱 | ||
| 化学名 | (3S,4R)-3-ethyl-4-((1-methyl-1H-imidazol-5-yl)methyl)dihydrofuran-2(3H)-one hydrochloride | ||
| Canonical SMILES | Cl[H].O=C1OC([H])([H])[C@@](C([H])([H])C2=C([H])N=C([H])N2C([H])([H])[H])([H])[C@]1([H])C([H])([H])C([H])([H])[H] | ||
| 分子式 | C11H16N2O2.HCl | 分子量 | 244.72 |
| 溶解度 | 50 mg/mL in DMSO(Need ultrasonic); 20mg/mL in Water | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0863 mL | 20.4315 mL | 40.863 mL |
| 5 mM | 0.8173 mL | 4.0863 mL | 8.1726 mL |
| 10 mM | 0.4086 mL | 2.0432 mL | 4.0863 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet