Benzydamine
(Synonyms: 苄达明) 目录号 : GC40704
An Analytical Reference Standard
Cas No.:642-72-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Benzydamine is commonly used, in its hydrochloride form, as a local analgesic and anti-inflammatory at oral and vaginal mucosal surfaces. Among its many effects, it locally suppresses histamine-induced vasodilation and vascular permeability and blocks the production of TNF-α by monocytes (IC50 = 25 μM). Benzydamine is also abused by inhalation and gestation. This product is intended for forensic and research purposes.
| Cas No. | 642-72-8 | SDF | |
| 别名 | 苄达明 | ||
| Canonical SMILES | CN(C)CCCOC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3 | ||
| 分子式 | C19H23N3O | 分子量 | 309.4 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 50 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/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 | 3.2321 mL | 16.1603 mL | 32.3206 mL |
| 5 mM | 0.6464 mL | 3.2321 mL | 6.4641 mL |
| 10 mM | 0.3232 mL | 1.616 mL | 3.2321 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。
Effect of Honey-Lemon Spray Versus Benzydamine Hydrochloride Spray on Radiation-Induced Acute Oral Mucositis in Head and Neck Cancer Patients: A Pilot, Randomized, Double-Blind, Active-Controlled Clinical Trial
J Altern Complement Med 2021 Mar;27(3):255-262.PMID:33512251DOI:10.1089/acm.2020.0468.
Introduction: Oral mucositis (OM) is the most prevalent side effect in patients with head and neck cancer (HNC). It causes an obvious decrease in quality of life (QoL) in these patients, so different medications have been recommended for OM, however, without optimal response. This randomized trial aimed to assess the effects of a honey-lemon spray compared with Benzydamine hydrochloride in prevention of radiation-induced OM in patients with HNC. Materials and Methods: Forty-six patients with HNC received external beam radiotherapy for 5 days per week. Patients were randomized to treatment with either Benzydamine hydrochloride spray or honey-lemon spray for 5 weeks and continued for 1 week after the end of treatment. The oral cavity was examined weekly, with a score given to each site based on the degree of mucositis using a 4-point scale, and a mean mucositis score was calculated as the primary outcome. Occurrence of OM, pain, QoL, and adverse effects were defined as secondary outcomes. Patients, therapists, and outcome assessors were blinded to group allocation. Results: No significant group differences occurred in the mucositis score, pain, or QoL. Mucositis occurrence rates were higher in the Benzydamine hydrochloride group compared with the honey-lemon group (hazard ratio = 2.1, 95% confidence interval: 1.1 to 4.2). Two patients in the honey-lemon group had mild nausea and burning throat; no adverse effects occurred in the Benzydamine hydrochloride group. Conclusions: There were no significant group differences in mucositis severity between patients treated with honey-lemon spray and Benzydamine hydrochloride. The potential preventive effects of honey-lemon spray need to be confirmed in further trials. The trial registration number is IRCT20161024030467N1.
Repurposed Benzydamine targeting CDK2 suppresses the growth of esophageal squamous cell carcinoma
Front Med 2022 Dec 29.PMID:36580233DOI:10.1007/s11684-022-0956-8.
Esophageal squamous cell carcinoma (ESCC) is one of the leading causes of cancer death worldwide. It is urgent to develop new drugs to improve the prognosis of ESCC patients. Here, we found Benzydamine, a locally acting non-steroidal anti-inflammatory drug, had potent cytotoxic effect on ESCC cells. Benzydamine could suppress ESCC proliferation in vivo and in vitro. In terms of mechanism, CDK2 was identified as a target of Benzydamine by molecular docking, pull-down assay and in vitro kinase assay. Specifically, Benzydamine inhibited the growth of ESCC cells by inhibiting CDK2 activity and affecting downstream phosphorylation of MCM2, c-Myc and Rb, resulting in cell cycle arrest. Our study illustrates that Benzydamine inhibits the growth of ESCC cells by downregulating the CDK2 pathway.
Benzydamine-An Affordable Over-the-Counter Drug with Psychoactive Properties-From Chemical Structure to Possible Pharmacological Properties
Pharmaceuticals (Basel) 2023 Apr 10;16(4):566.PMID:37111323DOI:10.3390/ph16040566.
Benzydamine is a non-steroidal anti-inflammatory drug with distinct pharmacological properties from other compounds in the same therapeutic class. The differences are structural and pharmacological in nature; the anti-inflammatory mechanism is not strictly explained by the ability to interfere with the synthesis of prostaglandins. The compound is used strictly in local inflammatory diseases (inflammation in the oral and vaginal mucosa). In addition to the therapeutic indications found in the summary of product characteristics (SPC), the compound is used, in high doses, as a psychotropic substance for oral administration, having similar properties to lysergic acid diethylamide (LSD). As an over-the-counter (OTC) compound, it is easy to obtain, and the consequences of using it for purposes other than those assumed by the manufacturer raise various concerns. The reasons are related to the pharmacodynamic and pharmaco-toxicological properties, since neither the mechanism of action nor the possible side effects that would result from systemic consumption, in high doses, even occasionally, have been fully elucidated. The present review aims to analyze the pharmacodynamic properties of Benzydamine, starting from the chemical structure, by comparison with structurally similar compounds registered in therapy (as an anti-inflammatory or analgesic) or used for recreational purposes.
Benzydamine Reverses TMexCD-TOprJ-Mediated High-Level Tigecycline Resistance in Gram-Negative Bacteria
Pharmaceuticals (Basel) 2021 Sep 7;14(9):907.PMID:34577607DOI:10.3390/ph14090907.
Recently, a novel efflux pump gene cluster called tmexCD1-toprJ1 and its variants have been identified, which undermine the antibacterial activity of tigecycline, one of the last remaining options effective against multidrug-resistant (MDR) Gram-negative bacteria. Herein, we report the potent synergistic effect of the non-steroidal anti-inflammatory drug Benzydamine in combination with tigecycline at sub-inhibitory concentrations against various temxCD-toprJ-positive Gram-negative pathogens. The combination of Benzydamine and tigecycline killed all drug-resistant pathogens during 24 h of incubation. In addition, the evolution of tigecycline resistance was significantly suppressed in the presence of Benzydamine. Studies on the mechanisms of synergism showed that Benzydamine disrupted the bacterial proton motive force and the functionality of this kind of novel plasmid-encoded resistance-nodulation-division efflux pump, thereby promoting the intracellular accumulation of tigecycline. Most importantly, the combination therapy of Benzydamine and tigecycline effectively improved the survival of Galleria mellonella larvae compared to tigecycline monotherapy. Our findings provide a promising drug combination therapeutic strategy for combating superbugs carrying the tmexCD-toprJ gene.
Casein Microgels as Benzydamine Hydrochloride Carriers for Prolonged Release
Materials (Basel) 2022 Feb 11;15(4):1333.PMID:35207872DOI:10.3390/ma15041333.
This research aims to investigate the properties of nano- and micro-sized casein hydrogels crosslinked by sodium tripolyphosphate as drug delivery systems. Benzydamine hydrochloride was chosen as a model hydrophilic drug. The gels were synthesized by varying different parameters: casein concentration, casein/crosslinking ratio, and addition of ethanol as a co-solvent. The electrostatic attractive interactions between the casein and the sodium tripolyphosphate were confirmed by FTIR spectroscopy. The particle sizes was determined by dynamic light scattering and varied in the range between several hundred nanometers and several microns. The yield of the gelation process was high for all investigated samples and varied between 55.3% and 78.3%. The encapsulation efficiency of the particles was strongly influenced by the casein concentration and casein/crosslinker ratio and its values were between 4.6% and 22.4%. The release study confirmed that casein particles are useful as Benzydamine carriers and ensured prolonged release over 72 h.