160208-18-4Relevant academic research and scientific papers
Acylated and alkylated histamine derivatives as new histamine H3-receptor antagonists
Stark, H.,Lipp, R.,Arrang, J. M.,Garbarg, M.,Schwartz, J. C.,Schunack, W.
, p. 695 - 700 (1994)
New histamine H3-receptor antagonists were prepared and investigated for their ability to increase synthesis and release of histamine mediated by inhibition of presynaptically located H3-receptors.Acyl derivatives of histamine methylated at different positions show poor activity at H3-receptors, whereas Nα-alkyl and particularly Nα-acyl derivatives of histamine possess moderate to good H3-receptor antagonist activity.A not-too-bulky and lipophilic residue in an optimal distance of 3-4 methylene groups from the amide function leads to potent and selective H3-receptor antagonists.Nα-Histamine-γ-phenylbutyramide 11 and Nα-histamine-γ-cyclohexylbutyramide 13 are H3-receptor antagonists with -log Ki of 7.1 and 7.3, respectively.Structure-activity relationships of different substitution patterns are discussed. histamine / histamine H3-receptor antagonist / Nα-alkylated histamine / Nα-acylated histamine / Nα-histamine-γ-cyclohexylbutyramide
