Cat. No. 4617
Chemical Name: 2R,3S,3aR,4aS,4bS,6aR,7S,7dR,8R,9aR
Biological ActivityPotent and selective blocker of BKCa (KCa1.1) channels (IC50 values are 6.4 and 64.4 nM for BKCa channels containing α subunits only, and those containing α and β1 respectively). Displays no effect on native delayed rectifier K+ and KATP currents, or cloned KV1.5 channels. Blocks BKCa channels in both inside-out and cell-attached patches. Shown to enhance smooth muscle contraction in vitro and increase total peripheral resistance in vivo.
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
Asano et al (2012) Penitrem A as a tool for understanding the role of large conductance Ca2+/voltage-sensitive K+ channels in vascular function. J.Pharmacol.Exp.Ther. 342 453. PMID: 22580348.
Knaus et al (1994) Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33 5819. PMID: 7514038.
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Citations are publications that use Tocris products. Selected citations for Penitrem A include:
Hirono et al (2015) BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells. J Biol Chem 35 7082. PMID: 25948259.
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