Betahistine mesylate

Betahistine mesylate functions as an orally active histamine H1 receptor agonist and a H3 receptor antagonist¹. It is utilized in the research of rheumatoid arthritis (RA)³.

Betahistine mesylate (0-10 μM) reduces 125Iiodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells, yielding IC50 values of 1.9 μM and 3.3 μM, respectively, leading to Ki values of 1.4 μM and 2.5 μM, respectively².

Betahistine mesylate (0-10 μM) regulates cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. It acts as an apparent inverse agonist at low concentrations, enhancing cAMP formation with EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM, respectively. However, at concentrations above 10 nM, it inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) cells, demonstrating full agonist activity².

Betahistine mesylate, with acute intraperitoneal or oral administration (0.1-30 mg/kg; single dose), elevates tele-methylhistamine (t-MeHA) levels, with an ED50 of 0.4 mg/kg, indicating inverse agonism. Acute oral administration also raises t-MeHA levels with an ED50 of 2 mg/kg in male Swiss mice².

Betahistine mesylate, administered orally at 1 and 5 mg/kg daily for 3 weeks, lessens the severity of arthritis and decreases pro-inflammatory cytokine levels in the paw tissues of CIA mice³.

Betahistine mesylate, with acute intraperitoneal or oral administration (0.1-30 mg/kg; single dose), elevates tele-methylhistamine (t-MeHA) levels, with an ED50 of 0.4 mg/kg, indicating inverse agonism. Acute oral administration also raises t-MeHA levels with an ED50 of 2 mg/kg in male Swiss mice².

Betahistine mesylate, administered orally at 1 and 5 mg/kg daily for 3 weeks, lessens the severity of arthritis and decreases pro-inflammatory cytokine levels in the paw tissues of CIA mice³.

溶解方案(细胞实验)

DMSO 中的溶解度 : 100 mg/mL (304.50 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (7.61 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (7.61 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (7.61 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"