Betahistine mesylate 

Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist^[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)^[3].

Betahistine mesylate (0-10 μM) inhibits [¹²⁵I]iodoproxyfan binding to membranes of CHO (rH₃₍₄₄₅₎R) and CHO (hH₃₍₄₄₅₎R) cells with IC₅₀ values of 1.9 μM and 3.3 μM, respectively. Lead to K_i values of 1.4 μM and 2.5 μM, respectively^[2].
Betahistine mesylate (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 mesylate behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC₅₀ values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, Betahistine mesylate inhibits cAMP formation with an EC₅₀ value of 0.1 μM in CHO (rH₃₍₄₄₅₎R) and full agonist activity^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Betahistine mesylate (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED₅₀ of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED₅₀ of 2 mg/kg in male Swissmice^[2].
Betahistine mesylate (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

328.41

Solid

C₁₀H₂₀N₂O₆S₂

54856-23-4

CNCCC1=NC=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O

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)

• [1]. Poyurovsky M, et al. The effect of Betahistine mesylate, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3.  [Content Brief]

  [2]. Gbahou F, et al. Effects of Betahistine mesylate at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54.  [Content Brief]

  [3]. Tang KT, et al. Betahistine mesylate attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245  [Content Brief]