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Medchemexpress LLC Betahistine dihydrochloride | 5579-84-0 | 99.8% | 10 G
SDP

Catalog No. 5000406005
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Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. It is used for the study of rheumatoid arthritis (RA). In vitro, Betahistine dihydrochloride 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, leading to Ki values of 1.4 μM and 2.5 μM. It has a regulating function on cAMP formation in CHO cells, acting as an apparent inverse agonist at low concentrations (EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM) and inhibiting cAMP formation at higher concentrations with an EC50 value of 0.1 μM in CHO (rH3(445)R). In vivo, acute administration of Betahistine dihydrochloride (0.1-30 mg/kg intraperitoneal or oral) increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg. Oral administration of 1 and 5 mg/kg daily for 3 weeks attenuated the severity of arthritis and reduced pro-inflammatory cytokines in CIA mice.

Catalog No. 50-004-06005 Supplier Medchemexpress LLC Supplier No. HYB0524A10G
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Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. It is used for the study of rheumatoid arthritis (RA). In vitro, Betahistine dihydrochloride 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, leading to Ki values of 1.4 μM and 2.5 μM. It has a regulating function on cAMP formation in CHO cells, acting as an apparent inverse agonist at low concentrations (EC50 values of 0.1 nM, 0.05 nM, and 0.3 nM) and inhibiting cAMP formation at higher concentrations with an EC50 value of 0.1 μM in CHO (rH3(445)R). In vivo, acute administration of Betahistine dihydrochloride (0.1-30 mg/kg intraperitoneal or oral) increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg. Oral administration of 1 and 5 mg/kg daily for 3 weeks attenuated the severity of arthritis and reduced pro-inflammatory cytokines in CIA mice.

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