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说明: KCa2 (SK) channel blocker
纯度: ≥95% (HPLC)
引用文献 (23)
评论 (1)
文献 (2)

生物活性 for Apamin

Apamin 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.

技术数据 for Apamin

分子量 2027.34
公式 C79H131N31O24S4

(Modifications: Disulfide bridges: 1-11, 3-15, His-18 = C-terminal amide)

储存 Store at -20°C
纯度 ≥95% (HPLC)
CAS Number 24345-16-2
PubChem ID 16133797
Smiles [H]N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC2=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2=CNC=N2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)O


Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Apamin

溶解性 Soluble to 1 mg/ml in water

产品说明书 for Apamin


参考文献 for Apamin


Habermann (1984) Apamin. Pharmacol.Ther. 25 255 PMID: 6095335

Stocker et al (2004) Matching molecules to function: neuronal Ca2+-activated K+ channels and afterhyperpolarizations. Toxicon 43 933 PMID: 15208027

Strong (1990) Potassium channel toxins. Pharmacol.Ther. 46 137 PMID: 2181489

van der Staay et al (1999) Behavioral effects of apamin, a selective inhibitor of the SKCa-channel, in mice and rats. Neurosci.Biobehav.Rev. 23 1087 PMID: 10643819

If you know of a relevant reference for Apamin, please let us know.

关键词: Apamin, Apamin supplier, K+, channels, blockers, small, conductance, ca2+-activated, ca2+-dependent, Potassium, KCa, KCa2, SK, venoms, Ca2+-Activated, Channels, 1652, Tocris Bioscience

23 篇 Apamin 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Apamin 的部分引用包括:

Yu et al (2014) Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents. J Neurosci 9 e96691 PMID: 24798465

Chan and Cipolla (2011) Relaxin causes selective outward remodeling of brain parenchymal arterioles via activation of peroxisome proliferator-activated receptor-γ. Sci Rep 25 3229 PMID: 21602449

O'Malley et al (2020) TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations. J Neurosci 40 4813 PMID: 32414784

Whitaker et al (2017) Bidirectional Modulation of Intrinsic Excitability in Rat Prelimbic Cortex Neuronal Ensembles and Non-Ensembles after Operant Learning. J Neurosci 37 8845 PMID: 28779019

Zachary and Fuchs (2015) Re-Emergent Inhibition of Cochlear Inner Hair Cells in a Mouse Model of Hearing Loss. J Neurosci 35 9701 PMID: 26134652

Hsueh et al (2013) Proarrhythmic effect of blocking the small conductance calcium activated potassium channel in isolated canine left atrium. Elife 10 891 PMID: 23376397

Geier et al (2011) Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol 300 C937 PMID: 21228322

Meredith et al (2011) Postnatal expression of an apamin-sensitive k(ca) current in vestibular calyx terminals. J Membr Biol 244 81 PMID: 22057903

Zemkova et al (2011) NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology 152 3842 PMID: 21828176

Fernandez-Fernandez et al (2018) Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS One 13 e0199282 PMID: 29928032

Rau et al (2015) Increased Basolateral Amygdala Pyramidal Cell Excitability May Contribute to the Anxiogenic Phenotype Induced by Chronic Early-Life Stress. Heart Rhythm 35 9730 PMID: 26134655

Henry et al (2015) Cell type-specific transcriptomics of hypothalamic energy-sensing neuron responses to weight-loss. Mol Pain 4 PMID: 26329458

Thompson et al (2015) 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. J Neurosci 11 51 PMID: 26311432

Gutzmann et al (2019) Functional Coupling of Cav2.3 and BK Potassium Channels Regulates Action Potential Repolarization and Short-Term Plasticity in the Mouse Hippocampus. Front Cell Neurosci 13 27 PMID: 30846929

Sargin et al (2016) Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels Elife 5 e21416 PMID: 27874831

Lee et al (2015) The role of K+ conductances in regulating membrane excitability in human gastric corpus smooth muscle. FASEB J 308 G625 PMID: 25591864

Few et al (2012) Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release. Proc Natl Acad Sci U S A 109 E452 PMID: 22308469

Villalobos and Andrade (2010) Visinin-like neuronal calcium sensor proteins regulate the slow calcium-activated afterhyperpolarizing current in the rat cerebral cortex. Am J Physiol Gastrointest Liver Physiol 30 14361 PMID: 20980592

Gamble-George et al (2016) Cyclooxygenase-2 inhibition reduces stress-induced affective pathology. Elife 5 PMID: 27162170

Turker et al (2013) Amiodarone inhibits apamin-sensitive potassium currents. PLoS One 8 e70450 PMID: 23922993

Alpert and Alford (2013) Synaptic NMDA receptor-dependent Ca2+ entry drives membrane potential and Ca2+ oscillations in spinal ventral horn neurons. PLoS One 8 e63154 PMID: 23646190

Lamy et al (2010) Allosteric block of KCa2 channels by apamin. J Neurosci 285 27067 PMID: 20562108

Han et al (2007) DArgic modulation of spinal neuronal excitability. J Biol Chem 27 13192 PMID: 18045913

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Apamin 的评论

平均评分: 5 (Based on 1 Review.)

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Product is a potent SK channel blocker which was studied on BK channels.
By Anonymous on 10/29/2018
分析类型: In Vitro
种属: Human

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.

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