Apamin

Cat. No. 1652

Apamin Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Disulfide bridges: 1 - 11, 3 - 15)

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Biological Activity

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.

Technical Data

M.Wt:
2027.34
Formula:
C79H131N31O24S4
Sequence:
CNCKAPETALCARRCQQH

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

Solubility:
Soluble to 1 mg/ml in water
Storage:
Desiccate at -20°C
CAS No:
24345-16-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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.

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

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

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Apamin include:

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

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.

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.

Thompson et al (2015) Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. J Neurosci 11 51. PMID: 26311432.

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.

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.

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.

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.

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

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.

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.

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

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

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.

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

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Keywords: Apamin, supplier, K+, channels, blockers, small, conductance, ca2+-activated, ca2+-dependent, Potassium, KCa, KCa2, SK, Tocris Bioscience, Calcium-Activated Potassium (KCa) Channel Blocker products

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