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Merck

Investigation of 4-piperidinols as novel H3 antagonists.

Bioorganic & medicinal chemistry letters (2010-09-14)
James T Anderson, Michael Campbell, Jianmin Wang, Kurt R Brunden, John J Harrington, Alain Stricker-Krongrad, Jianping Song, Chris Doucette, Steven Murphy, Youssef L Bennani
摘要

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.

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4-羟基哌啶, 98%