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4-Methylhistamine

Cat. No. M41849
4-Methylhistamine Structure
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Biological Activity

4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R).

Chemical Information
Molecular Weight 125.17
Formula C6H11N3
CAS Number 36507-31-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Abdulaziz M S Alsaad et al. Int J Mol Sci. Histamine H4 Receptor Agonist, 4-Methylhistamine, Aggravates Disease Progression and Promotes Pro-Inflammatory Signaling in B Cells in an Experimental Autoimmune Encephalomyelitis Mouse Model

[2] Arianna Giannetti et al. Medicina (Kaunas). Mast Cell Activation Disorders

[3] Sheikh Fayaz Ahmad et al. Immunobiology. Stimulation of the histamine 4 receptor with 4-methylhistamine modulates the effects of chronic stress on the Th1/Th2 cytokine balance

[4] L A Barker et al. Br J Pharmacol. Selectivity of 4-methylhistamine at H1- and H2-receptors in the guinea-pig isolated ileum

[5] P Reggio et al. J Med Chem. Molecular determinants for the agonist activity of 2-methylhistamine and 4-methylhistamine at H2-receptors

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Keywords: 4-Methylhistamine supplier, Histamine Receptor, inhibitors, activators


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