Tetracaine (Amethocaine)
(Synonyms: 丁卡因,Amethocaine) 目录号 : GC30838
An Analytical Reference Standard
Cas No.:94-24-6
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
Tetracaine is an analytical reference standard categorized as an anesthetic.1 Tetracaine has been found as an adulterant in products marketed as male sexual function enhancers.2 This product is intended for research and forensic applications.
1.Ireland, P.E., Ferguson, J.K.W., and Stark, E.J.The clinical and experimental comparison of cocaine and pontocaine as topical anesthetics in otolaryngological practiceTrans. Am. Laryngol. Rhinol. Otol. Soc.57(55th Meeting)438-450(1951) 2.Lee, J.H., Cho, S.-H., Kim, J.Y., et al.Determination and quantification of nine adulterant local anaesthetics in illegal treatments for male premature ejaculation by GC-FID and GC-MSInt. J. Pharm. Pharm. Sci.8(3)135-140(2016)
| Cas No. | 94-24-6 | SDF | |
| 别名 | 丁卡因,Amethocaine | ||
| Canonical SMILES | O=C(OCCN(C)C)C1=CC=C(NCCCC)C=C1 | ||
| 分子式 | C15H24N2O2 | 分子量 | 264.36 |
| 溶解度 | DMSO : ≥ 43 mg/mL (162.66 mM) | 储存条件 | Store at 2-8°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 | 3.7827 mL | 18.9136 mL | 37.8272 mL |
| 5 mM | 0.7565 mL | 3.7827 mL | 7.5654 mL |
| 10 mM | 0.3783 mL | 1.8914 mL | 3.7827 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。
Amethocaine hydrochloride
Tetracaine hydrochloride induces cell cycle arrest in melanoma by downregulating hnRNPA1
Recent evidence suggests potential benefits of applying local anesthetics in cancer patients. Specifically, tetracaine has a potent antitumor effect in diverse cancers, including neuroblastoma, breast cancer, and melanoma; however, the underlying molecular mechanisms remain unclear. Here, we reported that tetracaine hydrochloride inhibited the growth of melanoma cells and arrested melanoma cells in the G0/G1 phase. Tetracaine hydrochloride treatment resulted in translocation of hnRNPA1 from the nucleoplasm to the nuclear envelope and reduced the protein stability of hnRNPA1 possibly by disrupting the dynamic balance of ubiquitination and neddylation. Elevated hnRNPA1 upregulated cyclin D1 to promote cell cycle in melanoma. The hnRNPA1 overexpression attenuated the effect of tetracaine hydrochloride on melanoma cell growth suppression and cell cycle arrest. Furthermore, melanoma homograft experiments demonstrated that tetracaine hydrochloride suppressed melanoma growth, while hnRNPA1 overexpression alleviated tetracaine's antitumor effect on melanoma. Taken together, our findings suggest that tetracaine hydrochloride exerts a potent antitumor effect on melanoma both in vitro and in vivo, and the effect involves cell cycle arrest induction via downregulation of hnRNPA1.
A critical review of the topical local anesthetic amethocaine (Ametop) for pediatric pain
A topical formulation of the ester-type local anesthetic amethocaine (tetracaine) [Ametop ] is currently available for reducing pain from cutaneous procedures such as venipuncture. The Ametop mark preparation contains 40 mg of amethocaine base (4% w/w) and produces anesthesia within 30-45 minutes of application; duration of action ranges from 4 to 6 hours. Clinical studies have demonstrated the superiority of the 4% amethocaine preparation over placebo in pediatric populations for indications such as intravenous cannulation, vaccination, and venipuncture. Amethocaine has been shown to produce anesthesia comparable to that of 5% lidocaine-prilocaine for procedures such as venipuncture and accessing centrally placed devices; in general, anesthesia was achieved more rapidly with amethocaine than lidocaine-prilocaine. In the neonatal population amethocaine was found to be ineffective at reducing the pain of heel prick and peripherally inserted central catheters. Depending on the type of procedure, amethocaine application times between 30 and 60 minutes have produced clinically acceptable anesthesia; application times <30 minutes have not been associated with reliable anesthesia. The 4% amethocaine preparation is well tolerated; the most commonly reported local skin reaction is transient local erythema while local edema and itching have been reported more rarely. There have been no accounts of systemic toxicity with topical use of the preparation. Several cases of sensitization have been described in adults upon repeated exposure to topical amethocaine. In summary, the novel preparation of 4% amethocaine gel has been shown to be clinically effective for managing pain associated with minor cutaneous procedures while maintaining a good tolerability profile. Amethocaine has also demonstrated similar efficacy to lidocaine-prilocaine when appropriate application times are used; the more rapid onset of action and extended duration of action of amethocaine may make it more useful than lidocaine-prilocaine in busy clinical settings.
Lidocaine/tetracaine medicated plaster: in minor dermatological and needle puncture procedures
The lidocaine/tetracaine medicated plaster comprises a lidocaine/tetracaine 70 mg/70 mg patch and a controlled heat-assisted drug delivery pod that increases the diffusion of lidocaine and tetracaine into the dermis. Following a 1-hour application period, systemic absorption of lidocaine or tetracaine from the plaster was minimal. The lidocaine/tetracaine medicated plaster provided effective pain relief for adult (including elderly) patients undergoing minor dermatological procedures and for adult and paediatric patients undergoing vascular access procedures. In randomized, double-blind clinical trials, patient-reported median pain scores were significantly lower with the lidocaine/tetracaine medicated plaster than with an identical plaster containing placebo in patients undergoing minor dermatological or vascular access procedures. Furthermore, patient-reported median pain scores were significantly lower with the lidocaine/tetracaine medicated plaster than with a lidocaine/prilocaine cream in patients undergoing vascular access procedures. In a large, randomized, double-blind trial in paediatric patients undergoing venipuncture, the overall incidence of pain was significantly lower with the lidocaine/tetracaine medicated plaster than with a lidocaine/prilocaine plaster. The lidocaine/tetracaine medicated plaster was well tolerated, with the most frequent treatment-related adverse events resolving spontaneously.
Does topical Amethocaine cream increase first-time successful cannulation in children compared with a eutectic mixture of local anaesthetics (EMLA) cream? A systematic review and meta-analysis of randomised controlled trials
Background: Cannulation of children is often required for administration of intravenous fluids and medications, but can cause pain and anxiety. Amethocaine and a eutectic mixture of local anaesthetics (EMLA) cream are two of the most commonly used local anaesthetic creams.
Objective: To examine the evidence for the superiority of Amethocaine cream compared with EMLA cream in facilitating successful first-time cannulation in children.
Method: A systematic search was undertaken in MEDLINE and EMBASE in June 2014. Studies examining cannulation, undertaken with children and providing data about first-time cannulation success rates were considered for inclusion. Three randomised controlled trials met the inclusion criteria and were included in the meta-analysis. Data extraction was undertaken independently by the two authors using predefined data fields.
Results: Pooled analysis was based on a random effects model. Low statistical heterogeneity was observed. Amethocaine cream increased the likelihood of successful first-time cannulation (RR 1.046, CI 0.975 to 1.122), although this did not reach statistical significance (p=0.211).
Conclusions: Amethocaine cream does not appear to significantly facilitate successful first-time cannulation. Lack of precision and design weaknesses of the included studies hinder the formation of a strong recommendation for either cream.
Implications: Based on the evidence reviewed here and considering analgesic properties and cost-savings associated with both creams, a weak recommendation can be issued in favour of Amethocaine cream for cannulation in children based on high-quality evidence but where the treatment choice will depend on other factors including cost and provider preference.