Inhibitor of large-conductance Ca2+-activated K+ channels
Paxilline is an indole diterpene from fungi which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).[1],[2]It also enhances the binding of charybdotoxin, a peptidyl neurotoxin, to BKCa channels.[3] Paxilline is currently used to evaluate the role of BKCa channels in various cell processes and responses.[4],[5]
帕西林是一种来自真菌的吲哚二萜，可强有力、可逆地抑制大电导钙激活钾（BKCa）通道，这在贴片钳和整个平滑肌细胞研究中已有证实（Ki = 1.9 nM和Ki = 35.7 nM）[1],[2]。它还增强了BKCa通道对小蠕虫毒素（一种肽毒素）的结合[3]。帕西林目前用于评估BKCa通道在各种细胞过程和反应中的作用[4],[5]。
Reference:
[1]. Sanchez, M., and McManus, O.B. Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 35(7), 963-968 (1996).
[2]. Li, G., and Cheung, D.W. Effects of paxilline on K+ channels in rat mesenteric arterial cells. European Journal of Pharmacology 372, 103-107 (1999).
[3]. Knaus, H.G., McManus, O.B., Lee, S.H., et al. Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33(19), 5819-5828 (1994).
[4]. Jackson-Weaver, O., Paredes, D.A., Gonzalez Bosc, L.V., et al. Intermittent hypoxia in rats increases myogenic tone through loss of hydrogen sulfide activation of large-conductance Ca2+-activated potassium channels. Circulation Research 108(12), 1439-1447 (2011).
[5]. Tajima, N., Itokazu, Y., Korpi, E.R., et al. Activity of BKCa channel is modulated by membrane cholesterol content and association with Na+/K+-ATPase in human melanoma IGR39 cells. The Journal of Biological Chemisty 286(7), 5624-5638 (2011).
动态评分
0.0