Mepyramine maleate
(Synonyms: 吡拉明马来酸盐; Pyrilamine maleate) 目录号 : GC11291
Mepyramine maleate主要用作H1拮抗剂，其亲和pKd为9.4。
Cas No.:59-33-6
Sample solution is provided at 25 µL, 10mM.
Mepyramine maleate is mainly used as H1 antagonists, which has a high affinity pKd of 9.4[1]. Mepyramine maleate binds to histamine H1 receptors in bovine retinal vessels with a Kd value of 2.78±0.32nM[2]. Mepyramine maleate is a potent inhibitor at heteromeric potassium channel with IC50 value of 12.5μM[3].
Mepyramine maleate (100nM; 10min) inhibited intracellular calcium mobilization in Chinese hamster ovary cells[4]. Mepyramine maleate (1μmol/L; 48h) blocked the effects of supernatant from mucosal biopsies of a subgroup of irritable bowel syndrome patients on ATP-induced Ca2+ responses in enteric glial cells[5].
Mepyramine maleate (0.1-1.0μM; intra-articular injection of the knee; 10min) each partially inhibited bradykinin-induced synovial plasma extravasation in a dose-dependent manner within rat knee perfusion model (bradykinin perfusion into the knee)[6]. Mepyramine maleate (10 and 20mg/kg; i.p. ; 30min) significantly reduced formalin-induced the second phase of the biphasic pain response in rat model[7].
References:
[1] VAN DER GOOT H, TIMMERMAN H. Selective ligands as tools to study histamine receptors [J]. European journal of medicinal chemistry, 2000, 35(1): 5-20.
[2] MA W, YANG L, HE L. Overview of the detection methods for equilibrium dissociation constant K(D) of drug-receptor interaction [J]. J Pharm Anal, 2018, 8(3): 147-52.
[3] NAFFAA M M, AL-EWAIDAT O A. Ligand modulation of KCNQ-encoded (K(V)7) potassium channels in the heart and nervous system [J]. Eur J Pharmacol, 2021, 906(174278.
[4] FITZSIMONS C P, MONCZOR F, FERNANDEZ N, et al. Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein [J]. J Biol Chem, 2004, 279(33): 34431-9.
[5] LILLI N L, QUENEHERVE L, HADDARA S, et al. Glioplasticity in irritable bowel syndrome [J]. Neurogastroenterol Motil, 2018, 30(4): e13232.
[6] MORIYAMA K, LIU J, JANG Y, et al. Receptor mediation and nociceptin inhibition of bradykinin-induced plasma extravasation in the knee joint of the rat [J]. Inflamm Res, 2009, 58(12): 873-80.
[7] MOJTAHEDIN A, TAMADDONFARD E, ZANBOURI A. Effects of mepyramine and famotidine on the physostigmine-induced antinociception in the formalin test in rats [J]. Pak J Biol Sci, 2008, 11(22): 2573-8.
Mepyramine maleate主要用作H1拮抗剂，其亲和pKd为9.4[1]。Mepyramine maleate与牛视网膜血管组胺H1受体结合，Kd值为2.78±0.32nM[2]。Mepyramine maleate是一种有效的异聚钾通道抑制剂，IC50值为12.5μM[3]。
Mepyramine maleate（100nM; 10min）抑制中国仓鼠卵巢细胞内的钙动员[4]。Mepyramine maleate（1μmol/L; 48h）阻断在肠易激综合征患者亚组粘膜活检上清液里肠胶质细胞中ATP诱导的Ca2+反应[5]。
使用Mepyramine maleate（0.1-1.0μM; intra-articular injection of the knee; 10min）处理缓激肽灌注到大鼠膝关节内的大鼠模型，Mepyramine maleate以剂量依赖的方式部分抑制缓激肽诱导的滑膜血浆外渗[6]。使用Mepyramine maleate（10 and 20mg/kg; i.p. ; 30min）处理福尔马林诱导的大鼠双相疼痛反应模型，Mepyramine maleate显著降低大鼠双相疼痛反应第二阶段的疼痛[7]。
| Cell experiment [1]: | |
Cell lines | Chinese hamster ovary cells |
Preparation Method | Chinese hamster ovary cells were grown at 37°C in a humidified 5% CO2 incubator. The cells were cultured in DMEM containing 10% fetal calf serum, 2mM L-glutamine, 50μg/ml gentamicin. The cells were detached with trypsin, EDTA (0.5g/liter of trypsin, 0.2g/liter of EDTA, and 0.85g/liter NaCl) and resuspended in loading buffer (2mM CaCl2, 145mM NaCl, 10mM glucose, 5mM KCl, 1mM MgSO4, and 10mM HEPES, pH=7.4). The cells were then loaded in the presence of 5μM fluorescent Ca2+ indicator fura-2 acetoxymethyl ester for 20min at 37°C. The cells were 5-fold-diluted and incubated for 10min at 37°C to facilitate the hydrolysis of the ester to the acid form. Excess dye was removed by two cycles of centrifugation/resuspension in 2ml of loading buffer containing 0.1mM EGTA. Each Ca2+ measurement was preceded by a rapidcycle of centrifugation/resuspension in 2ml of loading buffer containing 0.1mM EGTA. Mepyramine maleate were preincubated for 10min. |
Reaction Conditions | 100nM; 10min |
Applications | Mepyramine maleate(100nM; 10min) inhibited intracellular calcium mobilization. |
| Animal experiment [2]: | |
Animal models | Male albino Wistar rats |
Preparation Method | Fifty microlitres of 1% formalin was injected subcutaneously into the ventral surface of right hind paw using a 29-gauge injection needle. The rat was then placed in the observation chamber with a mirror mounted at 45°beneath the floor to allow an unobstructed view of the paw. The time spent licking and biting the injected paw was taken as a measure of nociceptive response. Mepyramine maleate at doses of 10 and 20mg/kg were intraperitoneally injected into rats 30min before induction of nociception. |
Dosage form | 10 and 20mg/kg; i.p. ; 30min |
Applications | Mepyramine maleate significantly reduced formalin-induced the second phase of the biphasic pain response. |
References: | |
| Cas No. | 59-33-6 | SDF | |
| 别名 | 吡拉明马来酸盐; Pyrilamine maleate | ||
| 化学名 | N1-(4-methoxybenzyl)-N2,N2-dimethyl-N1-(pyridin-2-yl)ethane-1,2-diamine maleate | ||
| Canonical SMILES | CN(C)CCN(C1=NC=CC=C1)CC(C=C2)=CC=C2OC.OC(/C=C\C(O)=O)=O | ||
| 分子式 | C17H23N3O.C4H4O4 | 分子量 | 401.46 |
| 溶解度 | ≥ 20.073mg/mL in DMSO | 储存条件 | 4°C, protect from light |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4909 mL | 12.4545 mL | 24.9091 mL |
| 5 mM | 0.4982 mL | 2.4909 mL | 4.9818 mL |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 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 | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >99.50%
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