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HCN Channel Blocker Library

HCN Channel BlockerThe current produced by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels (termed If, cardiac pacemaker “funny” current, and Ih in neurons) is also considered a “pacemaker current” because it plays a key role in controlling the rhythmic activity of cardiac pacemaker cells and spontaneously firing neurons.

The pacemaker current is an inward current activated by voltage hyperpolarization and modulated by intracellular cAMP. The f-channels are encoded by four genes (HCN1–4) and are widely expressed through-out the heart and central nervous system.
HCN isoforms could serve as new genetic targets in the modulation of cellular rhythmicity [1]. The hyperpolarization-activated cation current is clearly an important target for the treatment of stable angina in the heart. Modulation of Ih may also be a promising approach for the treatment of disease processes in the central and peripheral nervous systems. Several results suggest that HCN channels also play a prominent role in neuropathic pain [2]. In this case, Ih blockers could be beneficial for analgesic therapy. Furthermore, the use of Ih blockers has also been implicated in epilepsy therapy [3].

Our new Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Blocker library (672 compounds in total) was designed as a special screening library containing compounds with predicted HCN channels blocking activity and selectivity. The compounds have been selected by pharmacophore screening of OTAVAchemicals's Drug-like Green Collection against two ligand-based pharmacophore models. The models were built based on known HCN channel blockers.

This library comprises drug-like compounds only and provides an excellent basis for antianginal, antiarrhythmic, neuropathic research and drug discovery projects.

 

All compounds are in stock, cherry-picking is available.

 

The library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.

 


 

1. DiFrancesco D, The role of the funny current in pacemaker activity, Circ Res – 2010 – 106 – pp. 255–271.
2. Jiang YQ, Sun Q, Tu HY et al, Characteristics of HCN channels and their participation in neuropathic pain, Neurochem Res – 2008 –  33 – pp. 1979–1989.
3. Kitayama M, Miyata H, Yano M et al, Ih blockers have a potential of antiepileptic effects, Epilepsia – 2003 – 44 – pp. 20–24.
 

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