Ropivacaine mesylate
(Synonyms: 甲磺酸罗哌卡因) 目录号 : GC39843
Ropivacaine mesylate 是一种氨基酰胺化合物，有阻断神经性疼痛的作用。Ropivacaine mesylate 是一种 K2P (双孔钾通道) TREK-1 抑制剂，在 COS-7 细胞膜上其 IC50 值为 402.7 μM。Ropivacaine mesylate 能在急性高血压模型中抑制压力诱导的肺内皮细胞高通透性。
Cas No.:854056-07-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ropivacaine mesylate is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine mesylate is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine mesylate inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension[1][2].
[1]. Li TF, et al. Epidural sustained release ropivacaine prolongs anti-allodynia and anti-hyperalgesia in developing and established neuropathic pain. PLoS One. 2015 Jan 24;10(1):e0117321. [2]. Milan Patel, et al. Ropivacaine Inhibits Pressure-Induced Lung Endothelial Hyperpermeability in Models of Acute Hypertension. Life Sci. 2019 Apr 1;222:22-28.
| Cas No. | 854056-07-8 | SDF | |
| 别名 | 甲磺酸罗哌卡因 | ||
| Canonical SMILES | O=C([C@H]1N(CCC)CCCC1)NC2=C(C)C=CC=C2C.CS(=O)(O)=O | ||
| 分子式 | C18H30N2O4S | 分子量 | 370.51 |
| 溶解度 | Water: 250 mg/mL (674.75 mM); DMSO: 20mg/mL | 储存条件 | Store at -20°C |
| 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 | 2.699 mL | 13.4949 mL | 26.9898 mL |
| 5 mM | 0.5398 mL | 2.699 mL | 5.398 mL |
| 10 mM | 0.2699 mL | 1.3495 mL | 2.699 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
Ropivacaine mesylate exerts neurotoxicity via up-regulation of Fas/FasL expression in rat pheochromocytoma PC12 cells
Am J Transl Res 2019 Mar 15;11(3):1626-1634.PMID:30972188doi
It has been shown that local anesthetics have potential neurotoxicity, but the exact mechanism remains unclear. In this study, PC12 cells were treated with different concentrations of Ropivacaine mesylate (0.1, 0.5, 1, 2 and 4 mmol/L) for 24 h, the cell viability was assessed by CCK-8 assay. Then, cells in 0.5 mmol/L ropivacaine group, 2 mmol/L ropivacaine group and control group were subjected to morphological observation under a light microscope, assessment of cell necrosis by Hoechst33342/PI staining and apoptosis by Annexin V-FITC/PI staining, and the detection of Fas and FasL expression by qPCR, immunofluorescence and Western blot. Results showed that the cell viability decreased significantly (P<0.05), necrosis and apoptosis rate increased markedly (P<0.05), and the expression of Fas, FasL, caspase-3 and caspase-8 increased dramatically (P<0.05) with the increase in the concentration of Ropivacaine mesylate. Therefore, Ropivacaine mesylate may induce the apoptosis of PC12 cells, which may be related to the up-regulation of Fas/FasL.
Epidural sustained release ropivacaine prolongs anti-allodynia and anti-hyperalgesia in developing and established neuropathic pain
PLoS One 2015 Jan 24;10(1):e0117321.PMID:25617901DOI:10.1371/journal.pone.0117321.
Ropivacaine is a local anesthetic widely used for regional anesthesia and epidural analgesia, but its relatively short duration limits its clinical use. A novel sustained release lipid formulation of ropivacaine has been recently developed to prolong its duration. We examined the epidural anti-hypersensitivity and preemptive effects of ropivacaine in mesylate injection and sustained release suspension forms in a rat model of neuropathy produced by peripheral nerve injury. Epidural administration of Ropivacaine mesylate injection specifically blocked mechanical allodynia and thermal hyperalgesia by approximately 50% with a biological half-effective duration of approximately 3 hrs. The equivalent dose of ropivacaine free-base in sustained release suspension significantly prolonged the duration of anti-allodynia and anti-hyperalgesia by approximately 2 times. Multiple daily epidural injections of ropivacaine in both the mesylate injection and sustained-release suspension forms did not induce tolerance or potentiation to anti-allodynia or anti-hyperalgesia. Moreover, the single or multiple daily administration of Ropivacaine mesylate injection before surgery in particular, markedly blocked the initiation and development of neuropathic pain, increasing the biological half-effective duration from less than 4 hrs up to 1 or 2 days. The single and multiple daily epidural injection of ropivacaine sustained release suspension further delayed the biological half-lives to 2 and 3 days, respectively. Our results indicate that the epidural administration of ropivacaine effectively blocks neuropathic pain without the induction of analgesic tolerance, and significantly delays the development of neuropathy produced by peripheral nerve injury. Epidural ropivacaine sustained release suspension produces much longer blockade effects of mechanical allodynia and heat hyperalgesia, and more significantly delays the development of neuropathic pain.
[Clinical effectiveness of Ropivacaine mesylate in epidural anesthesia and postoperative analgesia]
Zhongguo Yi Xue Ke Xue Yuan Xue Bao 2004 Dec;26(6):700-3.PMID:15663236doi
Objective: To compare the clinical effectiveness of Ropivacaine mesylate and ropivacaine hydrochloride in epidural anesthesia and postoperative analgesia. Methods: Forty-four patients undergoing epidural anesthesia for intraperitoneal hysterectomy or hysteromyomectomy were randomly assigned to two equal groups. Group ropivacaine hydrochloride received 15 ml ropivacaine hydrochloride of 7.5 mg/ml in anesthetic and 2 mg/ml in postoperative analgesic subsequently while group Ropivacaine mesylate correspondingly received Ropivacaine mesylate of both 15 ml of 8.94 mg/ml and 2.374 mg/ml. Results: No significant differences were found in the onset, extent, and duration of sensory and motor blockage, and also in the hemodynamic stability, when Ropivacaine mesylate was comparable with ropivacaine hydrochloride. No severe adverse events were observed in this study. Conclusion: Ropivacaine mesylate is an effective and safe alternative to ropivacaine hydrochloride in epidural anesthesia and postoperative analgesia.
[Effect of Ropivacaine Combined with Dexmedetomidine for Serratus Anterior Plane Block Plus Patient-Controlled Intravenous Analgesia on Postoperative Recovery Quality of Patients Undergoing Thoracoscopic Radical Resection of Lung Cancer]
Sichuan Da Xue Xue Bao Yi Xue Ban 2023 Jan;54(1):155-160.PMID:36647659DOI:10.12182/20230160102.
Objective: To study the postoperative analgesic effect of ropivacaine combined with dexmedetomidine for serratus anterior plane block (SAPB) under ultrasound visualization plus patient-controlled intravenous analgesia (PCIA) in patients undergoing thoracoscopic radical resection of lung cancer. Methods: A total of 129 patients undergoing elective thoracoscopic surgery were enrolled. The patients were randomly assigned to three groups ( n=43 in each group), a normal saline group (control group), a Ropivacaine mesylate group (Group R) and a Ropivacaine mesylate combined with dexmetomidine hydrochloride group (Group RD). After operation, ultrasound-guided SAPB was performed and patients in the three groups received the injection of 0 mL of 0.9% normal saline, 25 mL of 0.5% ropivacaine, and 25 mL of 0.5% ropivacaine+1 μg/kg dextrometomidine hydrochloride mixture, respectively. In addition, PCIA was used for all the patients. The button on the PCIA pump was pressed when the postoperative pain visual analogue score (VAS)≥4 on coughing, and rescue analgesic of sufentanil was given intravenously at 2.5 μg/bolus. The primary outcome was the VAS scores at rest and on coughing at 10 min (T 1), 6 h (T 2), 12 h (T 3), 24 h (T 4), and 48 h (T 5) after extubation. The secondary outcomes included hemodynamics, the quality of sleep for the first 3 nights after operation, number of times the button on the PCIA pump was pressed, intraoperative and postoperative opioid dosage, time of first postoperative rescue analgesic, duraion of intubation, length of stay at the hospital, adverse reactions, etc. Results: Compared with those of the control group, the VAS scores of the Group R and Group RD were significantly lower at 10 min, 6 h, and 12 h after extubation ( P<0.05). In comparison with Group R, the number of patients requiring rescue analgesia, the time of first postoperative rescue analgesic, the number of times the button on the PCIA pump was pressed, and the total dose of rescue sufentanil were all significantly lower ( P<0.05) in the Group RD. Patients in the Group RD had better sleep quality in the second and third nights after operation and lower incidence of nausea and vomiting ( P<0.05). Conclusion: 0.5% ropivacaine and 1 μg/kg dexmedetomidine SAPB combined with PCIA can significantly reduce postoperative pain and improve postoperative recovery quality in patients undergoing thoracoscopic radical resection of lung cancer.
[Circumcision versus the foreskin-deglove plus shaft-fix procedure for phimosis or redundant prepuce in obese adult patients]
Zhonghua Nan Ke Xue 2016 Mar;22(3):233-6.PMID:27172663doi
Objective: To compare the clinical effects of circumcision and the foreskin-deglove plus shaft-fix (FDSF) procedure in the treatment of phimosis or redundant prepuce in obese adult males (body mass index [BMI] ≥ 28 kg/m²). Methods: Forty-four obese adult men with phimosis or redundant prepuce underwent circumcision (n = 24) or FDSF (n = 20) according to their own wishes. The patients in the circumcision and FDSF groups were aged (26.38 ± 4.24) and (26.90 ± 3.14) years, with BMIs of (27.77 ± 0.77) and (28.07 ± 2.28) kg/m² and penis lengths of (3.51 ± 0.46) and (3.50 ± 0.59) cm, respectively. The operations were performed under local anesthesia with lidocaine plus Ropivacaine mesylate. Results: The operation time of circumcision was (28.04 ± 2.65) min and that of FDSF was (45.45 ± 3.49) min. At 6 months after surgery, normal penile erection was found in all the patients, the penis length was significantly longer in the FDSF than in the circumcision group ([5.01 ± 0.73] vs [3.70 ± 0.47] cm) , and the rate of satisfaction with penile appearance was markedly higher in the former than in the latter group (3.25 ± 0.71 vs 2.83 ± 0.56). Conclusion: The foreskin-deglove plus shaft-fix procedure under local anesthesia with lidocaine and Ropivacaine mesylate may achieve desirable penile erection and appearance in the treatment of phimosis or redundant prepuce in obese adult patients.