2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT 1D serotonin receptor ligands

Abstract

Depending on appended substituents, 2-(anilino)- and 2-(benzyl)imidazoline derivatives (X = NH or CH 2) bind at h5-HT 1D receptors with varying affinities and selectivities over h5-HT 1B receptors. Functional and pharmacokinetic data are provided for examples of 2-(benzyl)imidazolines and a ring-expanded analog: 2-(benzyl)-3,4,5,6- tetrahydropyrimidine. 2-(Anilino)imidazolines were identified as novel human 5-HT 1D receptor ligands, but offered no particular advantage over previously reported 2-(benzyl)imidazolines. Pharmacokinetic and functional data were obtained for selected 2-(benzyl)imidazoline derivatives. © 2004 Elsevier Ltd. All rights reserved.