82977-50-2Relevant academic research and scientific papers
Synthesis and histamine H3-receptor agonist activity of mono- and dialkyl-substituted histamine derivatives
Lipp, R.,Stark, H.,Arrang, J. M.,Garbarg, M.,Schwartz, J. C.,Schunack, W.
, p. 219 - 226 (2007/10/02)
In search for potential histamine H3-receptor agonists a series of mono- and dialkyl-substituted histamine derivatives was synthesized.All target compounds were tested in vitro for their agonist activity at H3-, H2, and H1-receptors.Introduction of one ethyl or two methyl residues into histamine led to compounds with decreased histamine H3-agonist potency in most cases.However, the non-chiral α,α-dimethylhistamine (15) was identified to be three times as active as histamine itself at H3-receptors.In addition 15 shows high receptor selectivity being20000 times as active at H3- as at H2- and H1-receptors, respectively. (αR)-αNτ-Dimethylhistamine 23, which is a potential metabolite of (αR)-α-methylhistamine 1, proved to be inactive at all three histamine receptor subtypes. α,α-dimethylhistamine / (αR)-αNτ-dimethylhistamine / histamine H3-receptor / agonist
