bk-channel

Paxilline 是一种来自 Penicillium paxilli 的吲哚生物碱霉菌毒素，是一种常用的大电导、电压和 Ca（2+） 依赖性 BK 型 K（+） 通道的特异性抑制剂，具有抗惊厥活性，抑制 BK 通道，抑制肌质网 Ca2+ 刺激的 ATP 酶 (SERCA)，可减轻沙利度胺引起的小鼠突触和认知功能障碍。

NS19504 是 Ca2+激活的 K+通道激活剂 (EC50=11.0 µM)，对膀胱平滑肌自发性相位收缩具有松弛作用。

Bupivacaine is a BK SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

Penitrem A is a selective antagonist of BK channel with antiproliferative and anti-invasive activities against multiple malignancies.

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases in the spontaneous beating of NRCMs.3,4 1.Schwarz, D., Kisselev, P., Ericksen, S.S., et al.Arachidonic and eicosapentaenoic acid metabolism by human CYP1A1: Highly steroselective formation of 17(R), 18(S)-epoxyeicosatetraenoic acidBiochem. Pharmacol.67(8)1445-1457(2004) 2.Lauterbach, B., Barbosa-Sicard, E., Wang, M.H., et al.Cytochrome P450-dependent eicosapentaenoic acid metabolites are novel BK channel activatorsHypertension39(2 Pt. 2)609-613(2002) 3.Falck, J.R., Wallukat, G., Puli, N., et al.17(R),18(S)-Epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: Structure-activity relationships and stable analoguesJ. Med. Chem.54(12)4109-4118(2011) 4.Arnold, C., Markovic, M., Blossey, K., et al.Arachidonic acid-metabolizing cytochrome P450 enzymes are targets of omega-3 fatty acidsJ. Biol. Chem.285(43)32720-32733(2010)

12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, exhibits potent calcium-activated potassium (BK) channel opening activity. It effectively inhibits GABA-dependent chloride influx in the mammalian brain, functioning as a non-competitive antagonist of GABA A receptors. Moreover, 12,14-Dichlorodehydroabietic acid induces an elevation in cytosolic free calcium levels and promotes the release of neurotransmitters.

BK channel activator (EC50 = 251 nM). Shifts the voltage required for half maximal negatively (DV1 2 = -104 mV).