Investigation of 4-piperidinols as novel H3 antagonists.
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.
Anderson
James T
JT
Athersys Inc., 3201 Carnegie Ave., Cleveland, OH 44115-2634, USA. andersj12@wyeth.com
Campbell
Michael
M
Wang
Jianmin
J
Brunden
Kurt R
KR
Harrington
John J
JJ
Stricker-Krongrad
Alain
A
Song
Jianping
J
Doucette
Chris
C
Murphy
Steven
S
Bennani
Youssef L
YL
D000818:Animals; D018360:Crystallography, X-Ray; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D008958:Models, Molecular; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D051638:Ether-A-Go-Go Potassium Channels; D054828:Histamine H3 Antagonists; D007202:Indicators and Reagents; D010880:Piperidines