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]。