bkca-channel

GAL-021 an intravenous BKCa-channel blocker.

GAL-021 sulfate is a BKCa channel blocker that inhibits the analgesic effects of opioids and is used in the study of respiratory control diseases.

(±)-Naringenin (Naringenine) is a natural product. It displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.

KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, exhibiting no inhibitory activity against P-gp or MRP1.

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

NS19504 is an activator of Ca2+-activated K+ channel with EC50 of 11.0 µM. NS19504 shows relaxing effect on bladder smooth muscle spontaneous phasic contractions[1].

NS1619 have cardio-protective effects after ischemia-reperfusion injury.

BMS-191011 (BMS-A) is an activator of large-conductance calcium-activated potassium (BKCa) channels ,effective in stroke models

Eicosapentaenoic acid (EPA) is metabolized into epoxyeicosatetraenoic acids (EpETE) by multiple cytochrome P450 isoforms. The predominant compound of this epoxygenase pathway, (±)17(18)-EpETE, induces relaxation in vascular and airway smooth muscles through its action on large conductance Ca2+-activated K+ (BKCa) channels, specifically by binding to the BKα channel subunits. Another notable epoxygenase pathway derivative, (±)11(12)-EpETE, also generated from EPA via CYP450 activity in both in vitro and in vivo studies, has biological and physiological roles that are yet to be fully elucidated.

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)