Promethazine
目录号 : GC25785Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.
Cas No.:60-87-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.
[1] C Cantisani, et al. Biomed Res Int. 2013;2013:151509. [2] Brittin T. Southard, Yasir Al Khalili. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan. [3] Daniel B Roquini, et al. Antimicrob Agents Chemother. 2019 Sep 16;63(12):e01208-19.
| Cas No. | 60-87-7 | SDF | Download SDF |
| 分子式 | C17H20N2S | 分子量 | 284.42 |
| 溶解度 | DMSO: 29 mg/mL (101.96 mM);Water: Insoluble;Ethanol: Insoluble | 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 | 3.5159 mL | 17.5796 mL | 35.1593 mL |
| 5 mM | 0.7032 mL | 3.5159 mL | 7.0319 mL |
| 10 mM | 0.3516 mL | 1.758 mL | 3.5159 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。
Should Promethazine in liquid form be available without prescription?
Pediatrics 1990 Aug;86(2):221-5.PMID:2196521doi
Promethazine, available by prescription only since its introduction in 1946, has been widely used for pediatric patients because of its antihistaminic, antiemetic, and sedative properties. Recently, it's makers have sought Federal Drug Administration approval to introduce two liquid over the counter allergy/cold/cough products containing Promethazine as an active ingredient. Although millions of doses have been administered, Promethazine use has not been free of risk. Promethazine has been reported to cause significant sedation, agitation, hallucinations, seizures, dystonic reactions, and possibly apparent life-threatening events or sudden infant death syndrome. The impact of these relatively uncommon adverse reactions on children would be minimal if parents would use over the counter Promethazine only for appropriate indications and only in children greater than 2 years of age. However, according to results of research evaluating the use of various over the counter medications by families for their children, Promethazine will be used inappropriately. Both its over the counter status, implying a certain margin of safety, and its formulation as a syrup, providing ease of administration, should increase its use in all age groups including that by children less than 2 years of age who may be most vulnerable to the adverse reactions associated with the drug's use.
Topical Promethazine side effects: our experience and review of the literature
Biomed Res Int 2013;2013:151509.PMID:24350243DOI:10.1155/2013/151509.
Promethazine hydrochloride is a first-generation H1 receptor antagonist, antihistamine, and antiemetic medication that can also have strong sedative effects. The apparent ability of topical H1r/2r antagonists to target epidermal H1/2r was translated into increased efficacy in the treatment of inflammatory dermatoses, likely due to decreased inflammation and enhanced barrier function.
Promethazine Downregulates Wnt/β-Catenin Signaling and Increases the Biomechanical Forces of the Injured Achilles Tendon in the Early Stage of Healing
Am J Sports Med 2022 Apr;50(5):1317-1327.PMID:35234523DOI:10.1177/03635465221077116.
Background: Wnt/β-catenin signaling suppresses the differentiation of cultured tenocytes, but its roles in tendon repair remain mostly elusive. No chemical compounds are currently available to treat tendon injury. Hypothesis: We hypothesized that the inhibition of Wnt/β-catenin signaling would accelerate tendon healing. Study design: Controlled laboratory study. Methods: Tendon-derived cells (TDCs) were isolated from rat Achilles tendons. The right Achilles tendon was injured via a dermal punch, while the left tendon was sham operated. A Wnt/β-catenin inhibitor, IWR-1, and an antihistamine agent, Promethazine (PH), were locally and intramuscularly injected, respectively, for 2 weeks after surgery. The healing tendons were histologically and biomechanically evaluated. Results: The amount of β-catenin protein was increased in the injured tendons from postoperative weeks 0.5 to 2. Inhibition of Wnt/β-catenin signaling by IWR-1 in healing tendons improved the histological abnormalities and decreased β-catenin, but it compromised the biomechanical properties. As we previously reported that antihistamine agents suppressed Wnt/β-catenin signaling in human chondrosarcoma cells, we examined the effects of antihistamines on TDCs. We found that a first-generation antihistamine agent, PH, increased the expression of the tendon marker genes Mkx and Tnmd in TDCs. Intramuscular injection of PH did not improve histological abnormalities, but it decreased β-catenin in healing tendons and increased the peak force and stiffness of the healing tendons on postoperative week 2. On postoperative week 8, however, the biomechanical properties of vehicle-treated tendons became similar to those of PH-treated tendons. Conclusion: IWR-1 and PH suppressed Wnt/β-catenin signaling and improved the histological abnormalities of healing tendons. IWR-1, however, compromised the biomechanical properties of healing tendons, whereas PH improved them. Clinical relevance: PH is a candidate repositioned drug that potentially accelerates tendon repair.
Promethazine-induced dystonic reaction
Pediatr Emerg Care 1987 Jun;3(2):91-2.PMID:3615241DOI:10.1097/00006565-198706000-00007.
The case of a 15-year-old girl who experienced an acute dystonic reaction to Promethazine therapy administered during an uncomplicated episode of acute gastroenteritis is reported. The pertinent literature is reviewed.
Preliminary experience with Promethazine hydrochloride injection in the sclerotherapy of oral mucocele
Int J Oral Maxillofac Surg 2021 Apr;50(4):516-521.PMID:32682647DOI:10.1016/j.ijom.2020.06.021.
Mucoceles are common in the minor salivary and sublingual glands. Sclerotherapy is a possible treatment strategy for mucoceles. The purpose of this study was to evaluate the clinical outcomes of sclerotherapy with Promethazine hydrochloride injection in treating mucoceles. Thirty-seven patients were enrolled. Sclerotherapy was performed with Promethazine hydrochloride injection (25mg/ml) through the mucosa. Patients were followed up at 1, 3, and 6 months after the last sclerotherapy. Clinical data were reviewed. The lesions (range 2-30mm in diameter) occurred on the ventral tongue tip (20 patients), lower lip (11 patients), and floor of the mouth (six patients). The amount of sclerosant per injection ranged from 0.2ml to 1ml. At the 6-month follow-up, 33 patients showed resolution with no recurrence. One patient showed a significant response with a 5-mm-diameter nodule remaining after two sclerotherapies. Three patients who underwent two or more sclerotherapies failed to show an improvement. The overall cure rate was 91.9% (96.8% for mucoceles of the minor salivary gland, 66.7% for ranulas). Complications were rare and mild. Sclerotherapy with Promethazine hydrochloride injection for the treatment of mucoceles is safe. It is effective for mucoceles of the minor salivary glands, but its application for ranulas requires further investigation.