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(R)-(-)-α-Methylhistamine dihydrobromide

Cat. No. M30758
(R)-(-)-α-Methylhistamine dihydrobromide Structure
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Biological Activity

(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats.

Chemical Information
Molecular Weight 287
Formula C6H13Br2N3
CAS Number 868698-49-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jian Xu, et al. J Biol Chem. The histamine H3 receptor modulates dopamine D2 receptor-dependent signaling pathways and mouse behaviors

[2] Jia-Ji Lin, et al. Oncotarget. Inhibition of histamine receptor 3 suppresses glioblastoma tumor growth, invasion, and epithelial-to-mesenchymal transition

[3] Heather Francis, et al. Mol Cancer Res. H3 histamine receptor-mediated activation of protein kinase Calpha inhibits the growth of cholangiocarcinoma in vitro and in vivo

[4] Heather Francis, et al. Lab Invest. H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway

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Keywords: (R)-(-)-α-Methylhistamine dihydrobromide supplier, Histamine Receptor, inhibitors, activators


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