Biological ActivityApamin is a prototypical potent and highly selective inhibitor of the small-conductance Ca2+-activated K+-channel (KCa2, SK). Blocks medium after-hyperpolarization in vitro and is brain penetrant and convulsive in vivo.
(Modifications: Disulfide bridges: 1-11, 3-15, His-18 = C-terminal amide)
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Matching molecules to function: neuronal Ca2+-activated K+ channels and afterhyperpolarizations.
Stocker et al.
Potassium channel toxins.
Behavioral effects of apamin, a selective inhibitor of the SKCa-channel, in mice and rats.
van der Staay et al.
Citations for Apamin
The citations listed below are publications that use Tocris products. Selected citations for Apamin include:
23 Citations: Showing 1 - 10
TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations.
Authors: O'Malley Et al.
J Neurosci 2020;40:4813
Functional Coupling of Cav2.3 and BK Potassium Channels Regulates Action Potential Repolarization and Short-Term Plasticity in the Mouse Hippocampus.
Authors: Gutzmann Et al.
Front Cell Neurosci 2019;13:27
Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons.
Authors: Fernandez-Fernandez Et al.
PLoS One 2018;13:e0199282
Bidirectional Modulation of Intrinsic Excitability in Rat Prelimbic Cortex Neuronal Ensembles and Non-Ensembles after Operant Learning.
Authors: Whitaker Et al.
J Neurosci 2017;37:8845
Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels
Authors: Sargin Et al.
Cyclooxygenase-2 inhibition reduces stress-induced affective pathology.
Authors: Gamble-George Et al.
Cell type-specific transcriptomics of hypothalamic energy-sensing neuron responses to weight-loss.
Authors: Henry Et al.
Mol Pain 2015;4
Increased Basolateral Amygdala Pyramidal Cell Excitability May Contribute to the Anxiogenic Phenotype Induced by Chronic Early-Life Stress.
Authors: Rau Et al.
Heart Rhythm 2015;35:9730
Re-Emergent Inhibition of Cochlear Inner Hair Cells in a Mouse Model of Hearing Loss.
Authors: Zachary and Fuchs
J Neurosci 2015;35:9701
The role of K+ conductances in regulating membrane excitability in human gastric corpus smooth muscle.
Authors: Lee Et al.
FASEB J 2015;308:G625
Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available R.zole in a rat model of arthritis pain.
Authors: Thompson Et al.
J Neurosci 2015;11:51
Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents.
Authors: Yu Et al.
J Neurosci 2014;9:e96691
Amiodarone inhibits apamin-sensitive potassium currents.
Authors: Turker Et al.
PLoS One 2013;8:e70450
Synaptic NMDA receptor-dependent Ca2+ entry drives membrane potential and Ca2+ oscillations in spinal ventral horn neurons.
Authors: Alpert and Alford
PLoS One 2013;8:e63154
Proarrhythmic effect of blocking the small conductance calcium activated potassium channel in isolated canine left atrium.
Authors: Hsueh Et al.
Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release.
Authors: Few Et al.
Proc Natl Acad Sci U S A 2012;109:E452
Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels.
Authors: Geier Et al.
Am J Physiol Cell Physiol 2011;300:C937
Relaxin causes selective outward remodeling of brain parenchymal arterioles via activation of peroxisome proliferator-activated receptor-γ.
Authors: Chan and Cipolla
Sci Rep 2011;25:3229
Postnatal expression of an apamin-sensitive k(ca) current in vestibular calyx terminals.
Authors: Meredith Et al.
J Membr Biol 2011;244:81
NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+.
Authors: Zemkova Et al.
Visinin-like neuronal calcium sensor proteins regulate the slow calcium-activated afterhyperpolarizing current in the rat cerebral cortex.
Authors: Villalobos and Andrade
Am J Physiol Gastrointest Liver Physiol 2010;30:14361
Allosteric block of KCa2 channels by apamin.
Authors: Lamy Et al.
J Neurosci 2010;285:27067
DArgic modulation of spinal neuronal excitability.
Authors: Han Et al.
J Biol Chem 2007;27:13192
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Reviews for Apamin
Average Rating: 5 (Based on 1 Review)
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Apamin is a potent SK channel blocker which was studied on BK channels. At low concentrations, it shows minimal blocking effect on BK channels but at higher concentrations moderate effects are shown. Great product and would recommend.