Literature DB >> 20795648

Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.

Michele Melchiorre1, Martina Del Lungo, Luca Guandalini, Elisabetta Martini, Silvia Dei, Dina Manetti, Serena Scapecchi, Elisabetta Teodori, Laura Sartiani, Alessandro Mugelli, Elisabetta Cerbai, Maria Novella Romanelli.   

Abstract

New I(f) blockers have been designed and tested on HEK293 cells stably expressing the HCN1, HCN2, and HCN4 channels to find compounds able to discriminate among the channel isoforms. Among the synthesized compounds, the cis-butene derivative (R)-5 shows some preference for HCN2 while the pseudodimeric product (R)-6 shows selectivity for HCN1. These compounds can be important pharmacological tools to study the channels in native tissues and may be useful to design safe drugs.

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Year:  2010        PMID： 20795648     DOI： 10.1021/jm1006758

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

Review 1.  Exploring HCN channels as novel drug targets.

Authors:  Otilia Postea; Martin Biel
Journal:  Nat Rev Drug Discov       Date:  2011-11-18       Impact factor: 84.694

2.  EC18 as a Tool To Understand the Role of HCN4 Channels in Mediating Hyperpolarization-Activated Current in Tissues.

Authors:  Maria Novella Romanelli; Martina Del Lungo; Luca Guandalini; Mehrnoush Zobeiri; András Gyökeres; Tamás Árpádffy-Lovas; Istvan Koncz; Laura Sartiani; Gianluca Bartolucci; Silvia Dei; Dina Manetti; Elisabetta Teodori; Thomas Budde; Elisabetta Cerbai
Journal:  ACS Med Chem Lett       Date:  2019-02-06       Impact factor: 4.345

3.  Identification and characterization of a series of novel HCN channel inhibitors.

Authors:  Shu-Jun Chen; Yao Xu; Ye-Mei Liang; Ying Cao; Jin-Yan Lv; Jian-Xin Pang; Ping-Zheng Zhou
Journal:  Acta Pharmacol Sin       Date:  2018-10-12       Impact factor: 6.150

4.  Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels by β-blocker carvedilol.

Authors:  Ying Cao; Shujun Chen; Yemei Liang; Ting Wu; Jianxin Pang; Shuwen Liu; Pingzheng Zhou
Journal:  Br J Pharmacol       Date:  2018-09-09       Impact factor: 8.739

5.  Novel blockers of hyperpolarization-activated current with isoform selectivity in recombinant cells and native tissue.

Authors:  Martina Del Lungo; Michele Melchiorre; Luca Guandalini; Laura Sartiani; Alessandro Mugelli; Istvan Koncz; Tamas Szel; Andras Varro; Maria Novella Romanelli; Elisabetta Cerbai
Journal:  Br J Pharmacol       Date:  2012-05       Impact factor: 8.739

6.  Seizures, behavioral deficits, and adverse drug responses in two new genetic mouse models of HCN1 epileptic encephalopathy.

Authors:  Andrea Merseburg; Jacquelin Kasemir; Eric W Buss; Felix Leroy; Tobias Bock; Alessandro Porro; Anastasia Barnett; Simon E Tröder; Birgit Engeland; Malte Stockebrand; Anna Moroni; Steven A Siegelbaum; Dirk Isbrandt; Bina Santoro
Journal:  Elife       Date:  2022-08-16       Impact factor: 8.713

Review 7.  Non-canonical Molecular Targets for Novel Analgesics: Intracellular Calcium and HCN Channels.

Authors:  Daniel C Cook; Peter A Goldstein
Journal:  Curr Neuropharmacol       Date:  2021       Impact factor: 7.708

Review 8.  Cardiac cAMP: production, hydrolysis, modulation and detection.

Authors:  Cédric Boularan; Céline Gales
Journal:  Front Pharmacol       Date:  2015-10-01       Impact factor: 5.810

9.  Ion channels and neuronal hyperexcitability in chemotherapy-induced peripheral neuropathy; cause and effect?

Authors:  Kelly Ann Aromolaran; Peter A Goldstein
Journal:  Mol Pain       Date:  2017 Jan-Dec       Impact factor: 3.395

Review 10.  HCN Channels Modulators: The Need for Selectivity.

Authors:  Maria Novella Romanelli; Laura Sartiani; Alessio Masi; Guido Mannaioni; Dina Manetti; Alessandro Mugelli; Elisabetta Cerbai
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295
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