Apamin. A Blocker of Small Conductance Ca2+-Activated K+ Channels (SK type).
Apamin is a natural peptide isolated and purified from Apis mellifera bee venom. Apamin blocks small conductance Ca2+-activated K+ channels (SK). It is specific for the SK1-3 isoforms, but ineffective in blocking other calcium activated K+ channels (see for example). In mammalian cell lines Apamin blocks expressed hSK1 with an IC50 of ~10nM, rSK1 and rSK2 with IC50 of ~3 and <1 nM respectively and liver rSK3 with IC50 <1nM. In Jurkat T-cells 5nM of Apamin blocks 70% of hSK2 currents.
Blocking these channels with Apamin slows down neuronal activity after hyperpolarization (see for example), as well as smooth muscle contraction and catecholamine secretion in adrenal gland. Electrophysiology application of long (~400ms) voltage ramps, covering the whole physiological range (-160 to +40mV), in the whole cell patch-clamp or voltage clamp configurations, before and after bath perfusion of the drug, allows the detection of the blocked channel currents (by comparison)
Alomone Labs is pleased to offer Apamin, a synthetic product in economical sizes at a very attractive price.
Ion Channel Modulators; K+ Channel Blockers.