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Biological Activity for Zatebradine hydrochloride
Zatebradine hydrochloride is a bradycardic agent that produces use-dependent inhibition of hyperpolarization-activated current If (HCN channel) in sinoatrial node cells (EC50 = 480 nM) and Purkinje fibres. Displays negative chronotropic activity in isolated guinea pig atria (EC50 of 13.4 μM).
Technical Data for Zatebradine hydrochloride
|Storage||Desiccate at +4°C|
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.
Solubility Data for Zatebradine hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Zatebradine hydrochloride
The following data is based on the product molecular weight 493.04. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.03 mL||10.14 mL||20.28 mL|
|5 mM||0.41 mL||2.03 mL||4.06 mL|
|10 mM||0.2 mL||1.01 mL||2.03 mL|
|50 mM||0.04 mL||0.2 mL||0.41 mL|
Product Datasheets for Zatebradine hydrochloride
References for Zatebradine hydrochloride
References are publications that support the biological activity of the product.
Van Bogaert et al (1990) Use- and frequency-dependent blockade by UL-FS 49 of the if pacemaker current in sheep cardiac Purkinje fibres. Eur.J.Pharmacol. 187 241 PMID: 2272362
Goethals et al (1993) Use-dependent block of the pacemaker current I(f) in rabbit sinoatrial node cells by zatebradine (UL-FS 49). On the mode of action of sinus node inhibitors. Circulation 88 2389 PMID: 8222132
Romanelli et al (2005) Design, synthesis and preliminary biological evaluation of zatebradine analogues as potential blockers of the hyperpolarization-activated current. Bioorg.Med.Chem. 13 1211 PMID: 15670930
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Keywords: Zatebradine hydrochloride, Zatebradine hydrochloride supplier, Bradycardic, agent, blocks, If, pacemaker, current, Channel, modulators, VDAC, ULFS49, HCN, blockers, UL-FS, 49, Channels, 2202, Tocris Bioscience
1 Citation for Zatebradine hydrochloride
Citations are publications that use Tocris products. Selected citations for Zatebradine hydrochloride include:
Bender et al (2007) Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation. J Neurosci 27 4697 PMID: 17460082
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.