Bromdiphenhydramine (1.5 and 3 μg/g, single dose) prevents mice from being challenged with a virulent strain of Salmonella typhimurium and causes the liver, spleen, and kidneys of protected animals to significantly decrease in comparison to unprotected controls. as well as the microbial growth in the blood [2].

Absorption, Distribution and Excretion
Absorbed well in the digestive tract. Metabolism/Metabolites Hepatic (cytochrome P-450 system); minor renal metabolism. Half-life: 1 to 4 hours.

Toxicity Summary
Bromhexine competes with free histamine for binding to HA receptor sites. This antagonizes the effect of histamine on HA receptors, thereby alleviating adverse symptoms caused by histamine binding to HA receptors.

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Protein Binding
96%

[1]. MOLINA EB. [A new antihistaminic, bromodiphenhydramine hydrochloride, in the control of cutaneous allergies]. Sem Med. 1960 Jul 11;117:151-2. Spanish.

[2]. Antibacterial activity of ambodryl and benadryl. J Appl Bacteriol. 1976 Oct;41(2):209-14.

[3]. Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property. Indian J Exp Biol. 1990 Mar;28(3):253-8.

Bromozine is a tertiary amine compound, specifically the 4-bromodiphenyl methyl ether of 2-(dimethylamino)ethanol. It is an antihistamine with antibacterial properties used to control skin allergies. It has dual action, acting as an antibacterial, muscarinic receptor antagonist, and H1 receptor antagonist. It is a tertiary amine compound and an organic bromine compound containing bromozine hydrochloride. Bromodiphenhydramine is an ethanolamine antihistamine with antibacterial properties. Bromodiphenhydramine is used to control skin allergies. Ethanolamine antihistamines produce significant sedation in most patients. Bromodiphenhydramine is a brominated derivative of diphenhydramine, an ethanolamine derivative and histamine H1 receptor antagonist with anti-allergic, sedative, antiemetic, and anticholinergic properties. Bromozine relieves symptoms caused by endogenous histamine on the bronchial, capillary, and gastrointestinal smooth muscle by competitively and selectively blocking central and peripheral histamine H1 receptors. This can prevent histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, itching, and gastrointestinal smooth muscle spasms. Furthermore, bromozine can bind to and block peripheral and central muscarinic receptors. Bromhexine has only been found in individuals who have taken the drug. It is an ethanolamine antihistamine with antibacterial properties. Bromhexine is used to control skin allergies. Ethanolamine antihistamines produce significant sedation in most patients. Bromhexine competes with free histamine for binding to HA receptors. This product antagonizes the effect of histamine on HA receptors, thereby reducing the adverse symptoms caused by histamine binding to HA receptors. Drug Indications Used to treat hay fever and other types of allergies, and to help with expectoration, thinning secretions, and producing phlegm. Mechanism of Action Bromhexine competes with free histamine for HA receptor binding sites. This antagonizes the effect of histamine on HA receptors, thereby reducing the adverse symptoms caused by histamine binding to HA receptors.

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Pharmacodynamics
Bromhexine is an ethanolamine antihistamine. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to common allergic symptoms, this drug can treat irritating cough and nausea, vomiting, and dizziness associated with motion sickness. It is also commonly used to treat drug-induced extrapyramidal symptoms and mild Parkinson's disease. Unlike sodium cromoglycate and nedolomim, which inhibit histamine release, bromhexine competitively binds to HA receptors with free histamine. Bromhexine competitively antagonizes the effects of histamine on HA receptors in the gastrointestinal tract, uterus, large blood vessels, and bronchial smooth muscle. The anticholinergic activity of ethanolamine derivatives is stronger than that of other antihistamines, which may explain bromhexine's anti-movement disorder effects. This anticholinergic effect appears to be due to its central antimuscarinic effect, which may also be the reason for its antiemetic effect, but the exact mechanism is unclear.

C17H20NOBR

334.2508

333.073

118-23-0

Bromodiphenhydramine hydrochloride;1808-12-4

2444

Typically exists as solid at room temperature

1.259g/cm3

397.3ºC at 760mmHg

194.1ºC

4.116

0

2

6

20

258

0

CN(CCOC(C1=CC=CC=C1)C2=CC=CC=C2)CBr

NUNIWXHYABYXKF-UHFFFAOYSA-N

InChI=1S/C17H20BrNO/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

2-[(4-bromophenyl)-phenylmethoxy]-N,N-dimethylethanamine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)