178920-25-7Relevant academic research and scientific papers
2-Alkyl-substituted histamines and hydroxyethylimidazoles with G-protein-stimulatory activity
Detert,Leschke,Toegel,Seifert,Schunack
, p. 397 - 405 (1996)
Cationic-amphiphilic 2-substituted histamines activate pertussis toxin-sensitive guanine nucleotide-binding proteins (G-proteins) by a receptor-independent mechanism. From our recent studies it became apparent that lipophilicity is an important determinan
Nα-Alkylated Derivatives of 2-Phenylhistamines: Synthesis and in Vitro Activity of Potent Histamine H1-Receptor Agonists
Kramer, K.,Elz, S.,Pertz, H. H.,Schunack, W.
, p. 2583 - 2588 (1998)
New potent Nα-alkylated histamine H1-receptor agonists have been prepared and functionally evaluated for partial agonist potency and selectivity. Nα-Methyl-2-(3-trifluoromethylphenyl)histamine contracts ileal segments and aortic rings of guinea-pig with a relative potency of 174 percent (95 percent confid. lim. 161-188 percent) and 217 percent (164-287 percent), respectively (histamine: 100 percent) and is the most potent H1 receptor agonist described so far.
