Literature DB >> 21316226

Pyridyl amides as potent inhibitors of T-type calcium channels.

Thomas S Reger1, Zhi-Qiang Yang, Kelly-Ann S Schlegel, Youheng Shu, Christa Mattern, Rowena Cube, Kenneth E Rittle, Georgia B McGaughey, George D Hartman, Cuyue Tang, Jeanine Ballard, Yuhsin Kuo, Thomayant Prueksaritanont, Cindy E Nuss, Scott M Doran, Steven V Fox, Susan L Garson, Yuxing Li, Richard L Kraus, Victor N Uebele, John J Renger, James C Barrow.   

Abstract

A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21316226     DOI: 10.1016/j.bmcl.2011.01.089

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

1.  The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Authors:  Zixiu Xiang; Analisa D Thompson; John T Brogan; Michael L Schulte; Bruce J Melancon; Debbie Mi; L Michelle Lewis; Bende Zou; Liya Yang; Ryan Morrison; Tammy Santomango; Frank Byers; Katrina Brewer; Jonathan S Aldrich; Haibo Yu; Eric S Dawson; Min Li; Owen McManus; Carrie K Jones; J Scott Daniels; Corey R Hopkins; Ximin Simon Xie; P Jeffrey Conn; C David Weaver; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-12-21       Impact factor: 4.418

Review 2.  T-type calcium channel blockers as neuroprotective agents.

Authors:  Benjamin J Kopecky; Ruqiang Liang; Jianxin Bao
Journal:  Pflugers Arch       Date:  2014-02-25       Impact factor: 3.657

Review 3.  Modulation of T-type calcium channels by bioactive lipids.

Authors:  Jean Chemin; Magali Cazade; Philippe Lory
Journal:  Pflugers Arch       Date:  2014-02-16       Impact factor: 3.657

4.  Inhibition of human N- and T-type calcium channels by an ortho-phenoxyanilide derivative, MONIRO-1.

Authors:  Jeffrey R McArthur; Leonid Motin; Ellen C Gleeson; Sandro Spiller; Richard J Lewis; Peter J Duggan; Kellie L Tuck; David J Adams
Journal:  Br J Pharmacol       Date:  2017-07-21       Impact factor: 8.739

5.  β-Arrestin-Dependent Dopaminergic Regulation of Calcium Channel Activity in the Axon Initial Segment.

Authors:  Sungchil Yang; Roy Ben-Shalom; Misol Ahn; Alayna T Liptak; Richard M van Rijn; Jennifer L Whistler; Kevin J Bender
Journal:  Cell Rep       Date:  2016-07-21       Impact factor: 9.423

6.  Evaluation of anticonvulsant effect of two novels 4-[1-(4-fluorobenzyl)- 5-imidazolyl] dihydropyridine derivatives in mice.

Authors:  F Hadizadeh; B Rahimi; E Taghiabadi; M Razavi; G Karimi
Journal:  Res Pharm Sci       Date:  2013-04

7.  Pharmacological Inhibition of Voltage-gated Ca(2+) Channels for Chronic Pain Relief.

Authors:  Seungkyu Lee
Journal:  Curr Neuropharmacol       Date:  2013-12       Impact factor: 7.363

8.  T-type calcium channels contribute to NMDA receptor independent synaptic plasticity in hippocampal regular-spiking oriens-alveus interneurons.

Authors:  Elizabeth Nicholson; Dimitri M Kullmann
Journal:  J Physiol       Date:  2017-03-22       Impact factor: 5.182

9.  Adjuvant role of a T-type calcium channel blocker, TTA-A2, in lung cancer treatment with paclitaxel.

Authors:  Neema Kumari; Pravin Shankar Giri; Subha Narayan Rath
Journal:  Cancer Drug Resist       Date:  2021-11-14
  9 in total

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