Triprolidine hydrochloride monohydrate
(Synonyms: 盐酸曲普利啶一水合物) 目录号 : GC39735Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
Cas No.:6138-79-0
Sample solution is provided at 25 µL, 10mM.
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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.
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 |
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。 |
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1 mg | 5 mg | 10 mg | |
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 |
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 | ||||||||||
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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。
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.