|N1-(4-甲氧基苄基)-N2,N2-二甲基-N1-(吡啶-2-基)乙烷-1,2-二胺马来酸盐|CsnPharm

CAS No.: 59-33-6

Mepyramine maleate/吡拉明马来酸盐 Catalog No. CSN11809

Synonyms: Pyrilamine maleate;Anisopyradamine;Diaminide Maleate

Mepyramine maleate is an antagonist of histamine H1 receptor.

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技术信息

生物活性

描述Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor^[3]. Mepyramine maleate has the potential to be helpful for dogs with angioedema^[4]. Mepyramine inhibited the lidocaine 3-hydroxylation activity catalyzed by P450 2D1 but did not inhibit the testosterone hydroxylation activities catalyzed by P450s other than P450 2D forms. The Ki value of mepyramine was especially low, at 34 nM. In human hepatic microsomes, mepyramine inhibited the debrisoquine 4-hydroxylation activity catalyzed by P450 2D6^[5]. Measurement of the time course of the block of H1-mediated blood pressure responses in conscious guinea pigs following a single i.p. injection of mepyramine, 5 mg/kg, suggested that some degree of block persisted for up to 16 h. Treatment of guinea pigs with two daily doses of 5 mg mepyramine/kg, i.p., for 10 days had no consistent effect on the KD or capacity of promethazine-sensitive [3H]mepyramine binding to cerebellum or hypothalamus^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02601235	Nasal Congestion	Phase 3	Recruiting	September 2018	Brazil ... more >> Faculdade de Medicina do ABC Recruiting Santo André, SP, Brazil Principal Investigator: Neusa Wandalsen, MD Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4909 mL
- 12.4547 mL
- 24.9093 mL
- 5 mM
- 0.4982 mL
- 2.4909 mL
- 4.9819 mL
- 10 mM
- 0.2491 mL
- 1.2455 mL
- 2.4909 mL

技术信息

CAS号

59-33-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H27N3O5

运输

蓝冰

分子量

401.46

别名

Pyrilamine maleate;Anisopyradamine;Diaminide Maleate;Paraminyl Maleate;Mepyramine (maleate);NSC 3604;Pyrilamine;Mepyramine Maleate;Minihist;Kriptin;Maleate;Mepyramine;吡拉明马来酸盐

溶解度

DMSO	185.0 mg/mL (460.8 mM)
Water	260.0 mg/mL (647.6 mM)

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Mepyramine maleate/吡拉明马来酸盐 Catalog No. CSN11809

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