Paxilline is an indole diterpene from fungi which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa, KCa1.1) channels[1,2]. It also enhances the binding of charybdotoxin, a peptidyl neurotoxin, to BKCa channels. Paxilline also inhibits the sarco/endoplasmic reticulum Ca2+ ATPase (IC50 = 5 - 50 μM)[3].?
References:
[1]. Sanchez M, McManus O B. Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology, 1996, ?35(7): 963-968.
[2]. Li G, Cheung D W. Effects of paxilline on K+ channels in rat mesenteric arterial cells. European Journal of Pharmacology , 1999, 372: 103-107.
[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, 1994, 33(19): 5819-5828.
