Effects of (1R,9S)-beta-hydrastine on intracellular calcium concentration in PC12 cells.
(1R,9S)-beta-hydrastine (BHS) decreases the basal intracellular Ca(2+) concentration ([Ca(2+)](i)) in PC12 cells.(5) This study examined the effects of (1R,9S)-BHS on [Ca(2+)](i) in PC12 cells. (1R,9S)-BHS at 10-100 microM in combination with a high extracellular K+ level (56 mM) inhibited the release of dopamine in a concentration-dependent manner with an IC(50) value of 66.5 microM. BHS at 100 microM inhibited the sustained increase in [Ca(2+)](i) induced by a high K+ level (56 mM), and had an inhibitory effect on the 2 microM nifedipine-induced blockage of the K+ -stimulated sustained increase in [Ca(2+)](i). In addition, (1R,9S)-BHS at 100 microM prevented the rapid and sustained increase in [Ca(2+)](i) elicited by 20 mM caffeine, but did not have an effect on the increase induced by 1 microM thapsigargin, in the presence of external Ca(2+). These results suggest that the active sites of (1R,9S)-BHS are mainly L-type Ca(2+) channels and caffeine-sensitive Ca(2+)-permeable channels in PC12 cells.
College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 12 Gaeshijn-Dong, Heungduk-Gu, Cheongju 361-763, Republic of Korea.
Shou Yu
SY
Yin
Yu Mi
YM
Kim
Jae Joon
JJ
Lee
Chun Mei
CM
Jin
Yoo Jung
YJ
Yang
Seung-Kook
SK
Park
Se Kuel
SK
Yoo
Myung Koo
MK
Lee
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D044182:Benzylisoquinolines / Q000494:pharmacology*; D002110:Caffeine / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000494:pharmacology; D020746:Calcium Channels, L-Type / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology; D009543:Nifedipine / Q000494:pharmacology; D016716:PC12 Cells; D011188:Potassium / Q000494:pharmacology; D051381:Rats; D019284:Thapsigargin / Q000494:pharmacology
D000470:Alkaloids; D044182:Benzylisoquinolines; D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; D004791:Enzyme Inhibitors; D002110:Caffeine; D019284:Thapsigargin; C013024:hydrastine; D009543:Nifedipine; D011188:Potassium; D002118:Calcium; D004298:Dopamine