Penehyclidine hydrochloride
(Synonyms: 盐酸戊乙奎醚(同分异构体混合物),Penequinine hydrochloride) 目录号 : GC64793
Penehyclidine (Penequinine) hydrochloride 是一种抗胆碱能药物，选择性的 M1 和 M3 受体拮抗剂。Penehyclidine hydrochloride 可激活肺组织中的 NF-kβ 并抑制炎症因子的释放。Penehyclidine hydrochloride 可减轻慢性阻塞性肺病 (COPD) 大鼠机械通气时的肺部炎症反应。
Cas No.:151937-76-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation[1].
[1]. Zhi-Yuan Chen, et al. The Mechanism of Penehyclidine Hydrochloride and Its Effect on the Inflammatory Response of Lung Tissue in Rats with Chronic Obstructive Pulmonary Disease During Mechanical Ventilation. Int J Chron Obstruct Pulmon Dis. 2021 Mar 31;16:877-885.
| Cas No. | 151937-76-7 | SDF | Download SDF |
| 别名 | 盐酸戊乙奎醚(同分异构体混合物),Penequinine hydrochloride | ||
| 分子式 | C20H30ClNO2 | 分子量 | 351.91 |
| 溶解度 | H2O : 2 mg/mL (5.68 mM; Need ultrasonic and warming) | 储存条件 | -20°C, away from moisture |
| 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 | 2.8416 mL | 14.2082 mL | 28.4164 mL |
| 5 mM | 0.5683 mL | 2.8416 mL | 5.6833 mL |
| 10 mM | 0.2842 mL | 1.4208 mL | 2.8416 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。
Penehyclidine hydrochloride: a potential drug for treating COPD by attenuating Toll-like receptors
Drug Des Devel Ther 2012;6:317-22.PMID:23139625DOI:10.2147/DDDT.S36555.
Background: The aim of this review was to evaluate and summarize the available scientific information on Penehyclidine hydrochloride (PHC) for the treatment of chronic obstructive pulmonary disease (COPD) as a result of its ability to attenuate Toll-like receptors. Penehyclidine hydrochloride is an anticholinergic drug manufactured in China, with both antimuscarinic and antinicotinic activity. PHC is used widely in the clinic as a reversal agent in cases of organic phosphorus poisoning and soman poisoning, but also may also have an important role as a bronchodilator in the treatment of obstructive airway disease, including asthma and, in particular, COPD. Methods: Our bibliographic sources included the CAPLUS, MEDLINE, REGISTRY, CASREACT, CHEMLIST, CHEMCATS, and CNKI databases, updated to September 2012. In order to assess the data in detail, we used the search terms "Penehyclidine hydrochloride," "COPD," "muscarinic receptor," and "toll-like receptors." Papers were restricted to those published in the English and Chinese languages, and to "paper" and "review" as the document type. Patents were also reviewed. Results: Our survey mainly yielded the results of research on PHC and the mechanisms of COPD. COPD is a preventable and treatable disease with some significant extrapulmonary manifestations that may contribute to its severity in some patients. Recently, it has been shown that muscarinic receptors may interact with Toll-like receptors. Basic and clinical studies of the relationship between the mechanism of action and the effects of PHC in the respiratory tract have been studied by a number of laboratories and institutions. The main advantages of PHC are that it has few M(2) receptor-associated cardiovascular side effects and attenuates Toll-like receptors. Conclusion: PHC may be a promising candidate agent in the treatment of COPD in the future because of its ability to attenuate Toll-like receptors. This review should be of help to those intending to research this topic further.
Pleiotropic effects and pharmacological properties of Penehyclidine hydrochloride
Drug Des Devel Ther 2018 Oct 5;12:3289-3299.PMID:30323561DOI:10.2147/DDDT.S177435.
Background: Penehyclidine hydrochloride (PHC) is an anticholinergic drug manufactured in China. It is used widely in clinics as a reversal agent in cases of organic phosphorus poisoning and as a preanesthetic medication. Compared with other anticholinergic agents, PHC confers substantial advantages. Here, in this review, we focus on its important clinical effects for organic phosphorus poisoning, preanesthetic medication, and the protective effects on certain visceral organs. Materials and methods: Our bibliographic sources include the PubMed and China National Knowledge Infrastructure (CNKI) databases, updated in March 2018. To assess the data in detail, we used the search terms "Penehyclidine hydrochloride," "preanesthetic medication," and "organic phosphorus." Papers were restricted to those published in the English and Chinese languages, and to "paper" and "review" as the document type. Results: PHC can effectively antagonize the symptoms of central and peripheral poisoning caused by organophosphorus poisoning. As a preanesthetic medication, it can not only effectively reduce mucus secretion and vascular infiltration but can also relax airway smooth muscles, dilate bronchioles in pulmonary conditions such as bronchiectasis, and increase pulmonary dynamic compliance. It can also prevent reflexive actions of the vagus nerve caused by excessive acetylcholine release such as abnormal airway contraction. Furthermore, it can strengthen sedation, bidirectionally regulate heart rate, and effectively inhibit respiratory secretions. In recent studies, PHC was shown to also have protective effects on various organs, such as the heart, lungs, brain, kidneys, intestines, and liver. Conclusion: PHC has beneficial pharmacological properties used in the treatment of organophosphorus poisoning and as a preanesthetic medication for its few side effects. It also has protective effects on multiple organs, suggesting that PHC has extensive clinical application value which is worth further research. This review should be of help to those intending to research these topics further.
Penehyclidine hydrochloride suppressed peripheral nerve injury-induced neuropathic pain by inhibiting microglial MAPK/p-p38/IL-1 β pathway activation
Mol Pain 2019 Jan-Dec;15:1744806919858260.PMID:31149893DOI:10.1177/1744806919858260.
Background: Millions of people suffered from neuropathic pain, which is related to neuroinflammation in the central nervous system. Penehyclidine hydrochloride is a premedication of general anesthesia, which has been confirmed possessing neuroprotective effects against various neurodegenerative or neuroinflammatory diseases. However, it is not clear that whether Penehyclidine hydrochloride could suppress neuropathic pain through its anti-neuroinflammatory effects. Methods: This study investigated the effects of Penehyclidine hydrochloride on rat spinal nerve ligation injury-induced neuropathic pain with behavioral, morphological, and molecular biological methods in animals. Results: The results indicated that Penehyclidine hydrochloride could attenuate spinal nerve ligation-induced neuropathic pain without any motor impairment and had no effect on sham-operated animals after repeated intraperitoneal administration. Intraperitoneal Penehyclidine hydrochloride could suppress spinal nerve ligation-induced ipsilateral spinal dorsal horn microglial activation with downregulation of OX42 expression. Moreover, intraperitoneal Penehyclidine hydrochloride inhibited spinal nerve ligation-induced spinal p-p38 mitogen-activated protein kinase expression, which was specially colocalized with the spinal dorsal horn microglia. Furthermore, intraperitoneal Penehyclidine hydrochloride could depress spinal neuroinflammation by suppressing spinal nerve ligation-induced interleukin (IL)-1β over-expression. Conclusion: These results indicated that the anti-allodynic effects of Penehyclidine hydrochloride on spinal nerve ligation-induced neuropathic pain did not rely on motor impairment. Inhibiting spinal microglial p-p38/IL-1β pathway activation might contribute to the anti-allodynic effect of Penehyclidine hydrochloride on nerve injury-induced neuropathic pain.
Penehyclidine hydrochloride Decreases Pulmonary Microvascular Endothelial Inflammatory Injury Through a Beta-Arrestin-1-Dependent Mechanism
Inflammation 2018 Oct;41(5):1610-1620.PMID:29766401DOI:10.1007/s10753-018-0804-9.
Penehyclidine hydrochloride (PHC), a type of hyoscyamus drug, has both antimuscarinic and antinicotinic activities and retains potent central and peripheral anticholinergic activities. Compared with other hyoscyamine, the notable advantage of PHC is that it has few M2 receptor-associated cardiovascular side effects. Recent studies and clinical trials have suggested that treatment with Penehyclidine hydrochloride may also possess good effects in the treatment of lung injury. The mechanism responsible for this effect has yet to be determined; however, one possibility is that they might do so by a direct effect on pulmonary vascular endothelium. Since inflammatory reactions of the endothelium are signs of endothelial injury in the pathogenesis of lung injury, we determined the effects of Penehyclidine hydrochloride on endothelial inflammatory injury in cultured human pulmonary microvascular endothelial cells (HPMVEC). Furthermore, human pulmonary microvascular endothelial cells were transfected with a shRNA-containing plasmid that specifically targets beta-arrestin-1 mRNA, to test whether the effect of Penehyclidine hydrochloride on lipopolysaccharide (LPS)-induced endothelial cell injury is dependent on its upregulation of beta-arrestin-1 or not. Penehyclidine hydrochloride reduced the inflammatory responses to LPS stimulation, as evidenced by reduced lactate dehydrogenase (LDH), tumor necrosis factor-alpha (TNF-α), and interleukelin-6 (IL-6) levels, as well as vascular cell adhesion molecule 1 (VCAM-1) and intercellular cell adhesion molecule-1 (ICAM-1) expressions. This was found to result from increased beta-arrestin-1 expression and decreased nuclear transcription factor-κB (NF-κB) activation. Expression of a shRNA-containing plasmid that specifically targets beta-arrestin-1 mRNA nullified these effects of Penehyclidine hydrochloride. The results indicate that Penehyclidine hydrochloride exerts a protective effect on pulmonary microvascular endothelial inflammatory injury induced by LPS. We also demonstrate that this is due to its ability to increase beta-arrestin-1, which in turn inhibits NF-κB activation.
Penehyclidine hydrochloride on postoperatively cognitive function
Med Hypotheses 2019 Aug;129:109246.PMID:31371081DOI:10.1016/j.mehy.2019.109246.
There are many drugs that affect postoperative cognitive function in patients under general anesthesia. Pentanethaquine hydrochloride (PHC), as a new type of anti-cholinergic drug, has been widely used. In clinical practice, many patients, especially elderly patients, have suffered from obvious postoperative cognitive dysfunction, but the incidence of pulmonary infection, reduced probably due to the decease of secretion production. Therefore, the effect of PHC on postoperative cognitive functions and inflammatory factors in elderly lung cancer patients under general anesthesia were mainly discussed to determine the clinical advantages and disadvantages. Ninety elderly patients undergoing thoracoscopic surgery for lung cancer under general anesthesia were selected and divided into PHC group (group A, n = 30), atropine group (group B, n = 30) and normal saline control group (group C, n = 30). The incidence of postoperative blurred vision was higher in group A compared to group B and C (both p < 0.05). The incidence of other adverse reactions was higher in group A compared to group C (all p < 0.05), but there was no difference between group A and group B (all p > 0.05). There was no significant difference in preoperative and day 1 post-surgery mini-mental state examination (MMSE) scores among the three groups (both p > 0.05), but the day 1 post-surgery MMSE scores of three groups were lower (all p < 0.05). PHC increased the incidence of postoperative cognitive impairment and postoperative delirium in elderly lung cancer patients undergoing thoracoscopic surgery under general anesthesia, but reduced the incidence of postoperative pulmonary complications possibly by reducing the expression of pro-inflammatory cytokines.