Investigation of 4-piperidinols as novel H3 antagonists

  • Bioorg Med Chem Lett. 2010 Nov 1;20(21):6246-9. doi: 10.1016/j.bmcl.2010.08.099.
James T Anderson  1 ,  Michael Campbell ,  Jianmin Wang ,  Kurt R Brunden ,  John J Harrington ,  Alain Stricker-Krongrad ,  Jianping Song ,  Chris Doucette ,  Steven Murphy ,  Youssef L Bennani
Affiliations
PMID: 20833043 DOI: 10.1016/j.bmcl.2010.08.099
Abstract

Compounds containing a substituted 4-piperidinol core have been found to be potent antagonists of the human H(3) receptor. The compounds exhibited up to a 60-fold preference for inhibiting the human H(3) receptor over the mouse and showed a low binding affinity for the hERG channel.