Chemical Name: (2R,4bS,6aS,12bS,12cR,14aS)-5,6,6a,7,12,12b,12c,13,14,14a-Decahydro-4b-hydroxy-2-(1-hydroxy-1-methylethyl)-12b,12c-dimethyl-2H-pyrano[2'',3'':5',6']benz[1',2':6,7]indeno[1,2-b]indol-3(4bH)-one
Biological ActivityPaxilline is a potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels. Binds to the α-subunit of BKCa (Ki = 1.9 nM for block of currents in α-subunit-expressing oocytes) and enhances binding of charybdotoxin to BKCa channels in vascular smooth muscle. Also inhibits sarco/endoplasmic reticulum Ca2+-ATPase (IC50 = 5 - 50 μM).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels.
Knaus et al.
Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel.
Sanchez and McManus
The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline.
Bilmen et al.
Citations for Paxilline
The citations listed below are publications that use Tocris products. Selected citations for Paxilline include:
19 Citations: Showing 1 - 10
Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1.
Authors: Madry Et al.
Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons.
Authors: Fernadez-Fernandez Et al.
PLoS One 2018;13:e0199282
Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus.
Authors: Abrahao Et al.
BK channel inactivation gates daytime excitability in the circadian clock.
Authors: Whitt Et al.
Nat Commun 2016;7:10837
Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
Authors: Kim Et al.
J Neurophysiol 2015;35:8245
BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells.
Authors: Hirono Et al.
J Neurosci 2015;35:7082
Aging-Related Hyperexcitability in CA3 Pyramidal Neurons Is Mediated by Enhanced A-Type K+ Channel Function and Expression.
Authors: Simkin Et al.
J Neurosci 2015;35:13206
Prostaglandin E2 excitatory effects on guinea pig urinary bladder smooth muscle: a novel regulatory mechanism mediated by large-conductance voltage- and Ca2+-activated K+ channels.
Authors: Parajuli Et al.
Eur J Pharmacol 2014;738:179
BK channels regulate sinoatrial node firing rate and cardiac pacing in vivo.
Authors: Lai Et al.
Am J Physiol Heart Circ Physiol 2014;307:H1327
Properties of BK-type Ca(+) (+)-dependent K(+) channel currents in medial prefrontal cortex pyramidal neurons in rats of different ages.
Authors: Ksiazek Et al.
Front Cell Neurosci 2013;7:185
Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior.
Authors: Montgomery Et al.
Am J Physiol Cell Physiol 2013;304:C299
Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice.
Authors: Wan Et al.
Nat Commun 2013;27:1859
Function and expression of ryanodine receptors and inositol 1,4,5-trisphosphate receptors in smooth muscle cells of murine feed arteries and arterioles.
Authors: Westcott Et al.
J Physiol 2012;590:1849
The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea.
Authors: Pulkkinen Et al.
Am J Physiol Lung Cell Mol Physiol 2012;303:L956
Redox sensitive calcium stores underlie enhanced after hyperpolarization of aged neurons: role for ryanodine receptor mediated calcium signaling.
Authors: Bodhinathan Et al.
J Neurophysiol 2010;104:2586
Mechanisms of sustained high firing rates in two classes of vestibular nucleus neurons: differential contributions of resurgent Na, Kv3, and BK currents.
Authors: Gittis Et al.
J Neurosci 2010;104:1625
Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model.
Authors: Zhang Et al.
Brain Res 2009;1247:196
Resveratrol attenuates early pyramidal neuron excitability impairment and death in acute rat hippocampal slices caused by oxygen-glucose deprivation.
Authors: Zhang Et al.
Exp Neurol 2008;212:44
Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells.
Authors: Pyott Et al.
FASEB J 2004;24:9469
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Reviews for Paxilline
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High-affinity and specific potassium channel blocker, used to study how it works to block SK (small conductance) channels. The product dissolved in DMSO and was excellent under lab conditions. Inhibition of SK channels were observed.