36507-31-0
36507-31-0
Chemical Structure
4-Methylhistamine
- CAS No.: 36507-31-0
- Formula:C6H11N3
- Molecular Weight:125.17
IUPAC Name: 2-(4-methyl-1H-imidazol-5-yl)ethan-1-amine
InChIKey: UGYXPZQILZRKJJ-UHFFFAOYSA-N
SMILES: NCCC1=C(C)N=CN1
Biological Activity: 4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation[1][2][3][4].
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4-Methylhistamine | 4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation. | |||||||||||||||||||||
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References
- [1]. Lim HD, et al. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. [Content Brief]
- [2]. Ahmad SF, et al. Stimulation of the histamine 4 receptor with 4-methylhistamine modulates the effects of chronic stress on the Th1/Th2 cytokine balance. Immunobiology. 2015 Mar;220(3):341-9. [Content Brief]
- [3]. Kim CH, et al. Inhibitory Effect of Imiquimod-Induced Psoriasis-Like Skin Inflammation in Mice by Histamine H4 Receptor Agonist 4-Methylhistamine. Scand J Immunol. 2016 Jun;83(6):409-17. [Content Brief]
- [4]. Cai WK, et al. Activation of histamine H4 receptors decreases epithelial-to-mesenchymal transition progress by inhibiting transforming growth factor-β1 signalling pathway in non-small cell lung cancer. Eur J Cancer. 2014 Apr;50(6):1195-206. [Content Brief]
