2. Academic Validation
  3. Investigation of 4-piperidinols as novel H3 antagonists

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

Affiliation

  • 1 Athersys Inc., 3201 Carnegie Ave., Cleveland, OH 44115-2634, USA. andersj12@wyeth.com
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.

Figures