Dehydroabietic acid derivatives as a novel scaffold for large-conductance calcium-activated K+ channel openers.
We found that the dehydroabietic acid structure is a new scaffold for chemical modulators of large-conductance calcium-activated K+ channels (BK channels). Structure-activity relationship (SAR) studies of the dehydroabietic acid derivatives and related non-aromatic compounds such as pimaric acid revealed the importance of the carboxyl functionality and an appropriate hydrophobic moiety of the molecules for BK channel-opening ability.
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan. ohwada@mol.f.u-tokyo.ac.jp
Tomohiko
T
Ohwada
Taro
T
Nonomura
Keisuke
K
Maki
Kazuho
K
Sakamoto
Susumu
S
Ohya
Katsuhiko
K
Muraki
Yuji
Y
Imaizumi
D045784:Abietanes / Q000737:chemistry* / Q000494:pharmacology*; D015640:Ion Channel Gating / Q000187:drug effects*; D007700:Kinetics; D051036:Large-Conductance Calcium-Activated Potassium Channels; D008958:Models, Molecular; D018408:Patch-Clamp Techniques; D024681:Potassium Channels, Calcium-Activated / Q000187:drug effects / Q000502:physiology*; D013329:Structure-Activity Relationship
D045784:Abietanes; D051036:Large-Conductance Calcium-Activated Potassium Channels; D024681:Potassium Channels, Calcium-Activated; C013913:dehydroabietic acid