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Triprolidine hydrochloride monohydrate Sale

(Synonyms: 盐酸曲普利啶一水合物) 目录号 : GC39735

Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.

Triprolidine hydrochloride monohydrate Chemical Structure

Cas No.:6138-79-0

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10mg
¥324.00
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25mg
¥648.00
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50mg
¥972.00
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100mg
¥1,782.00
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产品描述

Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.

[1] Simons KJ, et al. J Allergy Clin Immunol. 1986, 77(2):326-30.

Chemical Properties

Cas No. 6138-79-0 SDF
别名 盐酸曲普利啶一水合物
Canonical SMILES CC1=CC=C(/C(C2=NC=CC=C2)=C\CN3CCCC3)C=C1.[H]Cl.[H]O[H]
分子式 C19H25ClN2O 分子量 332.87
溶解度 DMSO : 62mg/mL 储存条件 Store at -20°C
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1 mM 3.0042 mL 15.0209 mL 30.0418 mL
5 mM 0.6008 mL 3.0042 mL 6.0084 mL
10 mM 0.3004 mL 1.5021 mL 3.0042 mL
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Research Update

Microbial transformation of the antihistaminic drug triprolidine hydrochloride

J Pharm Sci 1988 Mar;77(3):259-64.PMID:3286859DOI:10.1002/jps.2600770316.

The production of a known mammalian metabolite of the antihistamine triprolidine through fungal metabolic transformation has been demonstrated. The filamentous fungus Cunninghamella elegans ATCC 9245 was grown in Sabouraud dextrose broth containing Triprolidine hydrochloride monohydrate. One major metabolite was extracted with methylene chloride, isolated by high-performance liquid chromatography, and identified by its proton-nuclear magnetic resonance and desorption chemical ionization mass spectral properties as hydroxymethyl triprolidine (2-[1-(4-hydroxymethylphenyl)-3-(1-pyrrolidinyl-1-propenyl)] pyridine). After 240 h of incubation, the hydroxymethyl derivative represented approximately 55.0% of the initial dose. Fungal oxidation of hydroxymethyl triprolidine to the corresponding carboxylic acid triprolidine derivative (also a known mammalian triprolidine metabolite) was not observed. No mutagenic activity was observed for triprolidine and hydroxymethyl triprolidine by reversion of Salmonella typhimurium strains TA97, TA98, TA100, and TA104 at concentrations up to 1000 and 200 micrograms/plate, respectively. These results suggest that the fungal metabolism of triprolidine to the hydroxymethyl derivative occurs predominantly through pathways which do not result in mutagenic activation. Incubation of C. elegans with triprolidine under an 18O2 atmosphere and subsequent electron impact mass spectral analysis of the hydroxymethyl triprolidine formed indicate that molecular oxygen was incorporated into the methyl group and suggest a mono-oxygenase catalyzed reaction. This study parallels previous studies on the mammalian metabolism of triprolidine and clearly indicates that the microbial transformation of triprolidine is a useful alternative for the synthesis of potential mammalian metabolites.

Trace analysis of the antihistamines methapyrilene hydrochloride, pyrilamine maleate and Triprolidine hydrochloride monohydrate in animal feed, human urine and wastewater by high-performance liquid chromatography and gas chromatography with nitrogen-phosphorus detection

J Chromatogr 1984 Jan 20;283:251-64.PMID:6142898DOI:10.1016/s0021-9673(00)96260-5.

Toxicological evaluation of the antihistamines methapyrilene hydrochloride, pyrilamine maleate, and Triprolidine hydrochloride monohydrate using methapyrilene hydrochloride as the positive indicator was investigated as part of a structure-activity relationship study in rats and mice. Prerequisites for the toxicological tests were the development of analytical procedures to certify the dose, homogeneity and stability of the drugs in animal feed and to monitor human urine for possible exposure and to ensure removal of the test agents from wastewater prior to its discharge into the environment. A high-performance liquid chromatographic (HPLC) system was developed using a fluorescence detector for the determination of methapyrilene hydrochloride and pyrilamine maleate in feed at levels as low as 100 ng/g and in human urine as low as 1 ng/g. An HPLC-UV procedure was developed for the determination of Triprolidine hydrochloride monohydrate in feed at levels as low as 10 micrograms/g. Data concerning p-values, extraction efficiencies from feed and stability experiments in feed are presented for these antihistamines. A gas chromatographic procedure using a nitrogen-phosphorus detector was also developed for determining the three antihistamines in admixture in wastewater at levels as low as 10 ng/g.

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers

Br J Clin Pharmacol 1984 Dec;18(6):901-6.PMID:6529531DOI:10.1111/j.1365-2125.1984.tb02562.x.

Plasma and milk concentrations of pseudoephedrine and triprolidine were determined (by radioimmunoassay) in three lactating mothers over 12-48 h after ingestion of a combination medication containing 60 mg of pseudoephedrine hydrochloride and 2.5 mg of Triprolidine hydrochloride monohydrate. Pseudoephedrine concentrations in milk were consistently higher than those in plasma. The total amount of drug in milk, as judged by areas under the respective curves (AUC), was two to three times greater than in plasma. Triprolidine concentrations in milk and plasma were more variable between subjects than those of pseudoephedrine. AUC values for milk and plasma were similar for one subject, while the plasma value exceeded that for milk in another woman. The fraction of the dose excreted in milk was estimated to be 0.4-0.7% for pseudoephedrine and 0.06-0.2% for triprolidine.