Literature DB >> 28664409

Surfen is a broad-spectrum calcium channel inhibitor with analgesic properties in mouse models of acute and chronic inflammatory pain.

Paula Rivas-Ramirez1, Vinicius M Gadotti2, Gerald W Zamponi2, Norbert Weiss3.   

Abstract

Multiple voltage-gated calcium channels (VGCCs) contribute to the processing of nociceptive signals in primary afferent fibers. In addition, alteration of calcium channel activity is associated with a number of chronic pain conditions. Therefore, VGCCs have emerged as prime target for the management of either neuropathic or inflammatory pain, and selective calcium channel blockers have been shown to have efficacy in animal models and in the clinic. However, considering that multiple calcium channels contribute pain afferent signaling, broad-spectrum inhibitors of several channel isoforms may offer a net advantage in modulating pain. Here, we have analyzed the ability of the compound surfen to modulate calcium channels, and assessed its analgesic potential. We show that surfen is an equipotent blocker of both low- and high-voltage-activated calcium channels. Furthermore, spinal (intrathecal) delivery of surfen to mice produces sustained analgesia against both acute and chronic pain. Collectively, our data establish surfen as a broad-spectrum calcium channel inhibitor with analgesic potential, and raise the possibility of using surfen-derived compounds for the development of new pain-relieving drugs.

Entities:  

Keywords:  Calcium channel; Calcium channel blocker; DRG neuron; Inflammatory pain; Pain; Surfen

Mesh:

Substances:

Year:  2017        PMID: 28664409     DOI: 10.1007/s00424-017-2017-8

Source DB:  PubMed          Journal:  Pflugers Arch        ISSN: 0031-6768            Impact factor:   3.657


  65 in total

1.  Suppression of inflammatory and neuropathic pain symptoms in mice lacking the N-type Ca2+ channel.

Authors:  H Saegusa; T Kurihara; S Zong; A Kazuno ; Y Matsuda; T Nonaka; W Han; H Toriyama; T Tanabe
Journal:  EMBO J       Date:  2001-05-15       Impact factor: 11.598

2.  Distribution and regulation of L-type calcium channels in deep dorsal horn neurons after sciatic nerve injury in rats.

Authors:  E Dobremez; R Bouali-Benazzouz; P Fossat; L Monteils; J Dulluc; F Nagy; M Landry
Journal:  Eur J Neurosci       Date:  2005-06       Impact factor: 3.386

3.  Silencing of the Cav3.2 T-type calcium channel gene in sensory neurons demonstrates its major role in nociception.

Authors:  Emmanuel Bourinet; Abdelkrim Alloui; Arnaud Monteil; Christian Barrère; Brigitte Couette; Olivier Poirot; Anne Pages; John McRory; Terrance P Snutch; Alain Eschalier; Joël Nargeot
Journal:  EMBO J       Date:  2004-12-16       Impact factor: 11.598

4.  Distribution of calcium channel Ca(V)1.3 immunoreactivity in the rat spinal cord and brain stem.

Authors:  N Sukiasyan; H Hultborn; M Zhang
Journal:  Neuroscience       Date:  2008-12-14       Impact factor: 3.590

Review 5.  T-type voltage-gated calcium channels as targets for the development of novel pain therapies.

Authors:  Slobodan M Todorovic; Vesna Jevtovic-Todorovic
Journal:  Br J Pharmacol       Date:  2011-06       Impact factor: 8.739

6.  Z944: a first in class T-type calcium channel modulator for the treatment of pain.

Authors:  M Lee
Journal:  J Peripher Nerv Syst       Date:  2014-10       Impact factor: 3.494

7.  Synthesis and biological evaluation of novel N3-substituted dihydropyrimidine derivatives as T-type calcium channel blockers and their efficacy as analgesics in mouse models of inflammatory pain.

Authors:  Mohamed Teleb; Fang-Xiong Zhang; Junting Huang; Vinicius M Gadotti; Ahmed M Farghaly; Omaima M AboulWafa; Gerald W Zamponi; Hesham Fahmy
Journal:  Bioorg Med Chem       Date:  2017-02-13       Impact factor: 3.641

8.  N- and L-type calcium channels blocker cilnidipine ameliorates neuropathic pain.

Authors:  Shohei Yamamoto; Yuma Suzuki; Hideki Ono; Kazuhiko Kume; Masahiro Ohsawa
Journal:  Eur J Pharmacol       Date:  2016-11-05       Impact factor: 4.432

9.  Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.

Authors:  T J Lanza; P L Durette; T Rollins; S Siciliano; D N Cianciarulo; S V Kobayashi; C G Caldwell; M S Springer; W K Hagmann
Journal:  J Med Chem       Date:  1992-01-24       Impact factor: 7.446

10.  Pain sensitivity in mice lacking the Ca(v)2.1alpha1 subunit of P/Q-type Ca2+ channels.

Authors:  S Luvisetto; S Marinelli; M S Panasiti; F R D'Amato; C F Fletcher; F Pavone; D Pietrobon
Journal:  Neuroscience       Date:  2006-08-04       Impact factor: 3.590

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  1 in total

1.  Surfen and oxalyl surfen decrease tau hyperphosphorylation and mitigate neuron deficits in vivo in a zebrafish model of tauopathy.

Authors:  Seyedeh Maryam Alavi Naini; Constantin Yanicostas; Rahma Hassan-Abdi; Sébastien Blondeel; Mohamed Bennis; Ryan J Weiss; Yitzhak Tor; Jeffrey D Esko; Nadia Soussi-Yanicostas
Journal:  Transl Neurodegener       Date:  2018-03-16       Impact factor: 8.014

  1 in total

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