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Bromodiphenhydramine (hydrochloride) Sale

(Synonyms: Ambodryl hydrochloride) 目录号 : GC46024

A histamine H1 receptor antagonist

Bromodiphenhydramine (hydrochloride) Chemical Structure

Cas No.:1808-12-4

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产品描述

Bromodiphenhydramine is a histamine H1 receptor antagonist.1 It induces histamine release in isolated guinea pig lung when used at a concentration of 1 mM but completely prevents ovalbumin-induced histamine release in lungs isolated from ovalbumin-sensitized guinea pigs when used at concentrations of 100 and 200 μg/ml.2 Bromodiphenhydramine (17 mg/kg) inhibits formalin-induced paw edema in rats.1 It increases survival in a mouse model of systemic S. typhimurium infection when administered at doses of 1.5 and 3 mg/kg.3

|1. Ahmadi, A., Khalili, M., Nafarie, A., et al. Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H1-antihistaminic drugs. Mini Rev. Med. Chem. 12(12), 1282-1292 (2012).|2. Mota, I., and Da Silva, W.D. The anti-anaphylactic and histamine-releasing properties of the antihistamines. Their effect on the mast cells. Br. J. Pharmacol. Chemother. 15(3), 396-404 (1960).|3. Dastidar, S.G., Saha, P.K., Sanyamat, B., et al. Antibacterial activity of ambodryl and benadryl. J. Appl. Bacteriol. 41(2), 209-214 (1976).

Chemical Properties

Cas No. 1808-12-4 SDF
别名 Ambodryl hydrochloride
Canonical SMILES CN(C)CCOC(C1=CC=C(Br)C=C1)C2=CC=CC=C2.Cl
分子式 C17H20BrNO.HCl 分子量 370.7
溶解度 DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6976 mL 13.488 mL 26.976 mL
5 mM 0.5395 mL 2.6976 mL 5.3952 mL
10 mM 0.2698 mL 1.3488 mL 2.6976 mL
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Research Update

Pedagogical patronizing of the pharmacodynamic promises of illicit drugs

J Drug Educ 1992;22(1):9-13.PMID:1593391DOI:10.2190/J9KW-KRLM-GP55-AGVC.

A review of popular drug education textbooks and curricula indicated most juxtapose the physiologic effects of licitly manufactured drugs under headings representing illicitly prepared drugs. This misrepresentation ignores the literature, which is undivided, in reporting that illicit drugs contain adulterants and substitutes such as: sodium acetate, sodium cyclamate, dolomite, acetaminophen, gypsum, mannitol, inositol, lidocaine, amydricaine, benzocaine, caffeine, ephedrine, intercaine, phenylpropanolamine, piperocaine, procainamide, azopyridine, Bromodiphenhydramine, ibuprofen, methaqualone, phenobarital trazodone, acetylcodine, codeine, quinine, quinidine, thallium, arsenic and strychnine. The temptation to extrapolate the results of licitly pure drug lots administered at precisely measured doses to represent the pharmacodynamics of illegally prepared drug lots administered at indiscernible doses must be avoided in drug educational resources. There is a pressing need to correct the factual base, both implied and suggestive, of drug education resources regarding the purity and toxicity of illicitly manufactured and purchased drugs.

Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H(1)-antihistaminic drugs

Mini Rev Med Chem 2012 Oct;12(12):1282-92.PMID:22876948DOI:10.2174/138955712802762013.

In addition to their antihistamine effects, H1-receptor antagonists possess pharmacological properties that are not uniformly distributed among this class of drugs, such as anti-inflammatory, anti-allergic and antiplatelet activities. In this paper, Cyclizine (1-benzhydryl-4-methyl-piperazine, I), Bromodiphenhydramine (2-[(4-bromophenyl)-phenylmethoxy]-N, N-dimethylethanamine, II) and some of their new piperazine and ethanolamine derivatives (III-VIII) inducing changes in substitution of phenyl and amine moieties were synthesized and their acute and chronic antiinflammatory effects were evaluated by standard pharmacological tests. The results showed that substitution of phenyl by tolyl, anisol and cumene groups in piperazine family could remarkably decrease acute inflammation in these new drugs. Also, substitution of dimethylamine by morpholine group could not decrease this inflammation in new synthesized ethanolamine family. But the results from the cotton pellet-induced granuloma formation in rats showed that none of drugs (I-VIII) were effective to reduce the chronic inflammation.

Reverse phase thin-layer chromatographic separation of Bromodiphenhydramine and diphenhydramine

J Chromatogr Sci 1975 Dec;13(12):563-4.PMID:1194397DOI:10.1093/chromsci/13.12.563.

A thin-layer chromatographic system is described for the separation of diphenhydramine and Bromodiphenhydramine which is based on a reverse phase paper chromatographic system developed by J. Vecerková (2,3) in 1962. Chromatographic systems for this separation described in the literature and several systems attempted in this laboratory using normal chromatography have not proven successful. The method using reverse phase thin-layer chromatography involves a stationary phase of mineral oil on silica gel G and a mobile phase of ethanol:water:ammonium hydroxide, 28% NH3, (55:43:2). A 10-cm length of run requires about three hours and provides an excellent separation of the two compounds for identification-differentiation purposes.

Studies on synergism between penicillins and ambodryl (Bromodiphenhydramine HCl), an antihistamine with antimicrobial property

Indian J Exp Biol 1990 Mar;28(3):253-8.PMID:1973150doi

With respect to 31 different selected test bacteria, all sensitive to benzyl penicillin (Pc), ampicillin (Ap), methicillin (Me), ceporan (Ce), cloxacillin (Cx), streptomycin (Sm), kanamycin (Km), gentamicin (Gm), chloramphenicol (Cm), tetracycline (Tc), polymyxin (Pm) as well as ambodryl [Am; an antihistamine (Bromodiphenhydramine HCl) with distinct antimicrobial properties], it was found that Am in combination either with Pc, Ap, Ce or Me consistently showed enhancement of antimicrobial effects resulting from synergism. A combination of Am with either Sm, Km, Gm or Tc, on the other hand, showed only additive effects. An interaction of the activities of Am with Pm also resulted in indifference effects. Determination of the area of inhibition zone, calculated from its diameter for the degree of synergism in case of Am and Pc, showed these synergistic effects to be significant (P less than 0.05) in comparison with their individual effects: this was corroborated by the determination of the fractional inhibitory concentration (FIC) index which was found to be less than 0.5. The synergism of Am-Pc combination was confirmed by in vivo studies by challenging mice with a virulent strain of S. typhimurium and looking for protection.

Aggregation of antihistamines in aqueous solution. The effect of electrolyte on the miscellar properties of some diphenylmethane derivatives

J Pharm Pharmacol 1975 Jun;27(6):395-9.PMID:237086DOI:10.1111/j.2042-7158.1975.tb09467.x.

The effect of sodium chloride on the micellar properties of the antihistamines, dephenhydramine hydrochloride, Bromodiphenhydramine hydrochloride, chlorcyclizine hydrochloride and diphenylpyraline hydrochloride in aqueous solution has been investigated by light scattering and viscometric methods. The drugs behaved as typical ionic surfactants showing an increase in aggregation number and decrease in critical micelle concentration as the electrolyte concentration was increased over the range 0.05 to 0.154 mol kg-minus1. A linear relation between log critical micelle concentration and log counterion concentration was established, from which values of the degree of ionization and the free energy of micellization were calculated. The intrinsic viscosity was decreased by the addition of electrolyte and this has been attributed to a decrease in micellar hydration due to a removal of hydrogen-bonded water.