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CAS No. : 59-33-6
MCE 国际站:Mepyramine maleate
产品活性:Mepyramine maleate 是第一代抗组胺剂,为 histamine H1 受体拮抗剂,对 H1,H2 和 H3 受体的 Kd 值分别为 0.8 nM,5200 nM 和 >3000 nM,对 H1 受体的 pKd 值为 9.4。
研究领域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation
作用靶点:Histamine Receptor
In Vitro: Mepyramine maleate 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. Mepyramine binds to the H1 receptor with different Kds in Guinea pig brain (0.8 nM), rat brain (9.1 nM) and DDT1-MF-2 and BC3H1 cell (276 nM). Mepyramine decreases the InsP levels in CHO-gpH1 cells, with log EC50 of -7.94 ± 0.11, and reduces the the maximal response to ATP in CHO-gpH1 cells.
In Vivo: Mepyramine obviously decreases the second phase of nociceptive response via i.p at 10 and 20 mg/kg, but shows no significant effect at 5 mg/kg in rats.
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