Surfen is a broad-spectrum calcium channel inhibitor with analgesic properties in mouse models of acute and chronic inflammatory pain
Jazyk angličtina Země Německo Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
15-13556S
Grantová Agentura České Republiky - International
Canadian Institutes of Health Research - International
PubMed
28664409
DOI
10.1007/s00424-017-2017-8
PII: 10.1007/s00424-017-2017-8
Knihovny.cz E-zdroje
- Klíčová slova
- Calcium channel, Calcium channel blocker, DRG neuron, Inflammatory pain, Pain, Surfen,
- MeSH
- analgetika farmakologie MeSH
- blokátory kalciových kanálů farmakologie MeSH
- chronická bolest farmakoterapie MeSH
- chronická nemoc farmakoterapie MeSH
- lidé MeSH
- modely nemocí na zvířatech MeSH
- myši inbrední C57BL MeSH
- neuralgie farmakoterapie MeSH
- vápník metabolismus MeSH
- vápníková signalizace účinky léků MeSH
- zánět farmakoterapie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- analgetika MeSH
- blokátory kalciových kanálů MeSH
- vápník MeSH
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.
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Eur J Neurosci. 2005 Jun;21(12):3321-33 PubMed
Neuroscience. 2006 Oct 27;142(3):823-32 PubMed
EMBO J. 2005 Jan 26;24(2):315-24 PubMed
Eur J Pharmacol. 2016 Dec 15;793:66-75 PubMed
EMBO J. 2001 May 15;20(10):2349-56 PubMed
Bioorg Med Chem. 2017 Mar 15;25(6):1926-1938 PubMed
Br J Pharmacol. 2011 Jun;163(3):484-95 PubMed
J Med Chem. 1992 Jan 24;35(2):252-8 PubMed
Neuroscience. 2009 Mar 3;159(1):217-35 PubMed
J Peripher Nerv Syst. 2014 Oct;19 Suppl 2:S11-2 PubMed
Brain Res. 1996 Mar 18;712(2):265-73 PubMed
Neurosci Lett. 1990 Jul 3;114(2):203-6 PubMed
Pain. 2002 Mar;96(1-2):119-27 PubMed
Pain. 2010 Dec;151(3):633-43 PubMed
Nat Struct Mol Biol. 2004 Jan;11(1):67-72 PubMed
Physiol Rev. 2014 Jan;94(1):81-140 PubMed
Chem Sci. 2015 Oct 1;6(10 ):5984-5993 PubMed
Nat Neurosci. 2014 Feb;17(2):153-63 PubMed
J Med Chem. 2012 Nov 26;55(22):9847-55 PubMed
Sci Rep. 2013;3:1777 PubMed
Pflugers Arch. 2011 Nov;462(5):709-22 PubMed
PLoS One. 2014 Apr 04;9(4):e91467 PubMed
CNS Drugs. 2013 Nov;27(11):989-1002 PubMed
Cell Rep. 2015 Jan 14;:null PubMed
Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):13075-80 PubMed
Neuron. 2014 Sep 3;83(5):1144-58 PubMed
Mol Pharmacol. 2015 Jun;87(6):890-906 PubMed
Neuropharmacology. 2013 Dec;75:1-8 PubMed
Neuron. 2007 Aug 2;55(3):353-64 PubMed
Neuroscience. 2013 Oct 10;250:263-74 PubMed
Neurotherapeutics. 2009 Oct;6(4):679-92 PubMed
Mol Pain. 2015 Mar 14;11:12 PubMed
Biochim Biophys Acta. 2013 Jul;1828(7):1579-86 PubMed
JAMA. 2004 Jan 7;291(1):63-70 PubMed
Mol Pain. 2016 Apr 06;12 :null PubMed
Neurosci Lett. 2001 Sep 28;311(2):137-41 PubMed
J Physiol. 1992 Jan;445:639-58 PubMed
Expert Opin Investig Drugs. 2011 Sep;20(9):1277-84 PubMed
J Neurosci. 2012 Jul 4;32(27):9374-82 PubMed
Neuroscience. 2009 Apr 21;160(1):165-73 PubMed
Exp Neurol. 2015 Dec;274(Pt B):156-65 PubMed
Brain Res. 2004 Oct 22;1024(1-2):122-9 PubMed
Eur J Pharmacol. 1980 Oct 17;67(2-3):313-6 PubMed
Eur J Neurosci. 2007 Jun;25(12):3561-9 PubMed
Pflugers Arch. 2016 Nov;468(11-12):1837-1851 PubMed
Expert Opin Ther Targets. 2015 Jan;19(1):25-35 PubMed
Nat Rev Drug Discov. 2016 Jan;15(1):19-34 PubMed
Eur J Neurosci. 1997 Oct;9(10):2193-201 PubMed
J Biol Chem. 2014 Jun 20;289(25):17791-801 PubMed
BMJ Open. 2016 Dec 16;6(12 ):e013530 PubMed
Cereb Cortex. 2017 Feb 1;27(2):903-918 PubMed
J Neurosci Methods. 1985 Jun;14(1):69-76 PubMed
Mol Pain. 2016 Apr 29;12 :null PubMed
Trends Neurosci. 1988 Oct;11(10):431-8 PubMed
Nephrol Dial Transplant. 2003 Nov;18(11):2240-7 PubMed
Neuroscience. 2016 Dec 3;338:183-206 PubMed
Mol Pain. 2013 Jul 01;9:32 PubMed
Pain. 2011 Apr;152(4):833-43 PubMed
J Biol Chem. 2012 Jan 20;287(4):2810-8 PubMed
Br J Pharmacol. 2012 Nov;167(5):970-89 PubMed
Cell Calcium. 2006 Aug;40(2):165-74 PubMed
Neurosci Lett. 1992 Mar 2;136(2):161-4 PubMed
J Physiol. 2016 Nov 15;594(22):6607-6626 PubMed
Acta Pharmacol Sin. 2006 Dec;27(12):1547-52 PubMed
Mol Pain. 2013 Dec 26;9:67 PubMed
