397275-34-2Relevant academic research and scientific papers
4-Phenoxypiperidines: Potent, conformationally restricted, non-imidazole histamine H3 antagonists
Dvorak, Curt A.,Apodaca, Richard,Barbier, Ann J.,Berridge, Craig W.,Wilson, Sandy J.,Boggs, Jamin D.,Xiao, Wei,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 2229 - 2238 (2007/10/03)
Two new series of 4-(1-alkyl-piperidin-4-yloxy)-benzonitriles and 4-(1-isopropyl-piperidin-4-yloxy)-benzylamines have been prepared. In vitro activity was determined at the recombinant human H3 receptor and several members of these new series were found to be potent H3 antagonists. The present compounds contain a 4-phenoxypiperidine core, which behaves as a conformationally restricted version of the 3-amino-1-propanol moiety common to the many previously described non-imidazole histamine H 3 ligands. One selected member of the new series, 4-[4-(1-isopropyl-piperidin-4-yloxy)-benzyl]-morpholine (13g), was found to be a potent, highly selective H3 receptor antagonist with in vivo efficacy in a rat EEG model of wakefulness at doses as low as 1 mg/kg sc.
