| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
Bromodiphenhydramine (Bromazine; trade names: Ambodryl, Ambrodil and others) hydrochloride is the hydrochloride salt form of bromodiphenhydramine, a synthetic ethanolamine with histamine H1 antagonistic and sedative properties. The symptoms of histamine activity on capillaries, bronchial smooth muscle, and gastrointestinal smooth muscle—vasodilation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscle—are prevented by bromodiphenhydramine hydrochloride, which blocks the H1 histamine receptor. Additionally, this medication keeps mucous membranes from itching and hurting due to histamine.
| Targets |
This study investigates the antibacterial activity of Bromodiphenhydramine HCl. Its primary known pharmacology is as an antihistamine. [2]
|
|---|---|
| ln Vitro |
Bromodiphenhydramine hydrochloride (1.5 and 3 μg/g, single) protects mice from a virulent strain of Salmonella typhimurium challenge and also significantly lowers the organism's growth in the protected animals' liver, spleen, and blood when compared to the unprotected controls[2].
Among nine antihistamines screened, Bromodiphenhydramine HCl (Ambodryl) exhibited the broadest and most potent in vitro antibacterial activity. At concentrations of 50-100 µg/mL, it inhibited a large number of Gram-positive and Gram-negative bacterial strains. Its spectrum was broader than its analog Diphenhydramine HCl (Benadryl). [2] Specifically, at 50 µg/mL, Ambodryl inhibited 88 out of 111 Salmonella strains, 47 out of 73 Shigella strains, 54 out of 60 Staphylococcus aureus strains, and all 6 Vibrio cholerae strains tested. It was not active against Pseudomonas aeruginosa or Bordetella bronchiseptica. [2] The antibacterial effect was bactericidal, as bacteria exposed to the drug for 48 hours failed to grow upon transfer to fresh medium. [2] |
| ln Vivo |
Bromdiphenhydramine hydrochloride (1.5 and 3 μg/g, single dose) protects mice against challenge with a virulent strain of Salmonella typhimurium and also significantly reduces the risk of death in protected animals compared with unprotected animals. Control of the reproduction of this microorganism in the liver, spleen and blood [2].
In a mouse model of infection, a single intraperitoneal dose of Ambodryl (3 µg/g body weight, administered 3 hours before challenge) significantly protected Swiss white mice against a lethal challenge with 50 LD₅₀ of Salmonella typhimurium 11. Mortality was reduced compared to untreated controls (P < 0.01). [2] Treatment with Ambodryl (3 µg/g) also significantly reduced the bacterial load (CFU/mL) in the liver and spleen homogenates of infected mice at 2 and 18 hours post-challenge compared to saline-treated controls (P < 0.01 for 2-hour liver samples; P < 0.05 for others). [2] |
| Animal Protocol |
In vivo antibacterial efficacy test: Swiss white mice (15-18 g) were used. A virulent strain of Salmonella typhimurium 11 (mouse-passaged, LD₅₀ determined) was used for challenge. The challenge dose was 50 LD₅₀ (3.5 × 10⁷ CFU) suspended in 0.5 mL of peptone water, administered intraperitoneally. [2]
Ambodryl was dissolved in sterile saline. Mice received a single intraperitoneal injection of the drug (at doses of 0.75, 1.5, or 3 µg/g body weight, corresponding to 0.1 mL of solutions containing 125, 250, or 500 µg/mL, respectively) 3 hours prior to bacterial challenge. Control groups received 0.1 mL saline. [2] For bacterial load assessment, groups of mice were euthanized at 2 or 18 hours post-challenge. Livers and spleens were aseptically removed, homogenized, and viable bacterial counts (CFU/mL) were determined by plating serial dilutions on nutrient agar. Heart blood was also collected for bacteremia assessment and serum drug level analysis. [2] Serum drug level assay: Drug concentration in mouse serum was estimated using a microbiological assay. Filter paper discs soaked with serum were placed on peptone water agar plates seeded with S. typhimurium 11. The diameter of the inhibition zone was measured and compared to a standard curve prepared with known drug concentrations. [2] |
| ADME/Pharmacokinetics |
In mice treated with a dose of 3 µg/g of Ambodryl, the concentration of free drug in serum was determined. At 0 and 2 hours post-administration, serum drug concentrations were between 2 and 3 µg/mL. By 18 hours, drug concentrations decreased to between 1 and 2 µg/mL. Serum drug concentrations were similar in uninfected (drug-only) and infected (drug + bacteria) mice. [2]
|
| Toxicity/Toxicokinetics |
Mice treated with ambroxol (at doses up to 3 µg/g) without bacterial infection showed no obvious toxicity or death, indicating that, under experimental conditions, the drug alone (at doses up to 3 µg/g) did not cause acute death in the short term. [2]
|
| References | |
| Additional Infomation |
Bromodiphenhydramine Hydrochloride is the hydrochloride salt form of bromhexidine, a synthetic ethanolamine with histamine H1 receptor antagonism and sedative effects. Bromodiphenhydramine Hydrochloride blocks H1 histamine receptors, thereby preventing symptoms caused by histamine acting on capillary, bronchial, and gastrointestinal smooth muscle, including vasodilation, increased capillary permeability, bronchoconstriction, and gastrointestinal smooth muscle spasms. This drug also prevents histamine-induced mucosal pain and itching.
See also: Bromodiphenhydramine Hydrochloride; Zinc acetate (ingredients)...see more... Bromodiphenhydramine Hydrochloride (Ambrodiol) is primarily used as an antihistamine. This study reports its direct broad-spectrum antibacterial activity, which appears to be unrelated to its antihistamine function. [2] The chemical structure of Ambodryl differs from that of its analogue Diphenhydramine in that the former contains a bromine atom, which may contribute to its enhanced antibacterial spectrum and efficacy. [2] The authors believe that these findings may help in screening and developing derivatives with potent antibacterial activity but extremely low antihistamine activity. [2] |
| Molecular Formula |
C17H21BRCLNO
|
|---|---|
| Molecular Weight |
370.71174
|
| Exact Mass |
369.05
|
| Elemental Analysis |
C, 55.08; H, 5.71; Br, 21.55; Cl, 9.56; N, 3.78; O, 4.32
|
| CAS # |
1808-12-4
|
| Related CAS # |
Bromodiphenhydramine; 118-23-0
|
| PubChem CID |
519514
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
397.3ºC at 760 mmHg
|
| Flash Point |
194.1ºC
|
| Vapour Pressure |
1.61E-06mmHg at 25°C
|
| LogP |
4.918
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
21
|
| Complexity |
258
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.CN(CCOC(C1C=CC(Br)=CC=1)C1C=CC=CC=1)C
|
| InChi Key |
ZQDJSWUEGOYDGT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H20BrNO.ClH/c1-19(2)12-13-20-17(14-6-4-3-5-7-14)15-8-10-16(18)11-9-15;/h3-11,17H,12-13H2,1-2H3;1H
|
| Chemical Name |
2-[(4-bromophenyl)-phenylmethoxy]-N,N-dimethylethanamine;hydrochloride
|
| Synonyms |
Bromodiphenhydramine HCl; Bromodiphenhydramine hydrochloride
|
| HS Tariff Code |
2934.99.03.00
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6975 mL | 13.4876 mL | 26.9753 mL | |
| 5 mM | 0.5395 mL | 2.6975 mL | 5.3951 mL | |
| 10 mM | 0.2698 mL | 1.3488 mL | 2.6975 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA