Nα-Alkylated Derivatives of 2-Phenylhistamines: Synthesis and in Vitro Activity of Potent Histamine H1-Receptor Agonists

Article abstract of DOI:10.1016/S0960-894X(98)00461-2

New potent N^α-alkylated histamine H₁-receptor agonists have been prepared and functionally evaluated for partial agonist potency and selectivity. N^α-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.