Betahistine dihydrochloride is an orally activehistamine H1 receptoragonist and aH3 receptorantagonist^[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)^[3].

Betahistine dihydrochloride (0-10 μM) inhibits [¹²⁵I]iodoproxyfan binding to membranes of CHO (rH₃₍₄₄₅₎R) and CHO (hH₃₍₄₄₅₎R) cells withIC₅₀values of 1.9 μM and 3.3 μM, respectively. Lead to K_ivalues of 1.4 μM and 2.5 μM, respectively^[2].
Betahistine dihydrochloride (0-10 μM) has a regulating function on cAMP formation in CHO (rH₃₍₄₄₅₎R), CHO (rH₃₍₄₁₃₎R), and CHO (hH₃₍₄₄₅₎R) cells. At low concentrations, betahistine behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC₅₀values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, betahistine inhibits cAMP formation with an EC₅₀value of 0.1 μM in CHO (rH₃₍₄₄₅₎R) and full agonist activity^[2].

Betahistine dihydrochloride (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED₅₀of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED₅₀of 2 mg/kg in male Swissmice^[2].
Betahistine dihydrochloride (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice^[3].

209.12

Solid

C₈H₁₄Cl₂N₂

5579-84-0

盐酸倍他司汀；倍他司丁二盐酸盐

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

H₂O : ≥ 50 mg/mL(239.10 mM)

DMSO : 33.33 mg/mL(159.38 mM;Need ultrasonic)

DMF : 5 mg/mL(23.91 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 150 mg/mL (717.29 mM); Clear solution; Need ultrasonic