Penitrem A
Chemical Name: 2R,3S,3aR,4aS,4bS,6aR,7S,7dR,8R,9aR,14bS,14cR,16aS)-12-chloro-3,3a,6a,8,9,9a,10,11,14,14b,14c,15,16,16a-tetradecahydro-14b,14c,17,17-tetramethyl-10-methylene-2-(1-methylethenyl)-7,8-(epoxymethano)-2H,6H-cyclobuta[5,6]benz[1,2-e]oxireno[4',4'a]-1-benzopyrano[5',6':6,7]indeno[1,2-b]indole-3,4b,7d(5H,7H)-triol
Purity: ≥95%
Biological Activity
Penitrem A is a potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels.
Knaus et al.
Biochemistry, 1994;33:5819 -
Penitrem A as a tool for understanding the role of large conductance Ca2+/voltage-sensitive K+ channels in vascular function.
Asano et al.
J.Pharmacol.Exp.Ther., 2012;342:453
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Citations for Penitrem A
The citations listed below are publications that use Tocris products. Selected citations for Penitrem A include:
3 Citations: Showing 1 - 3
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BK channels regulate extracellular Tat-mediated HIV-1 LTR transactivation.
Authors: Khan Et al.
Sci Rep 2019;9:12285
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Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus.
Authors: Abrahao Et al.
Neuropsychopharmacology 2017;42:1070
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BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells.
Authors: Hirono Et al.
J Biol Chem 2015;35:7082
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