Literature DB >> 26101568

Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.

Sharan K Bagal1, Peter J Bungay2, Stephen M Denton3, Karl R Gibson3, Melanie S Glossop3, Tanya L Hay3, Mark I Kemp3, Charlotte A L Lane3, Mark L Lewis3, Graham N Maw3, William A Million3, C Elizabeth Payne2, Cedric Poinsard3, David J Rawson3, Blanda L Stammen3, Edward B Stevens2, Lisa R Thompson3.   

Abstract

Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemical matter that is efficacious in preclinical models of neuropathic and inflammatory pain.

Entities:  

Keywords:  Nav1.8; SCN10A; TTX-R; Voltage-gated sodium channels; sodium channel drugs

Year:  2015        PMID： 26101568      PMCID： PMC4468395          DOI： 10.1021/acsmedchemlett.5b00059

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  18 in total

1.  MMP-Cliffs: systematic identification of activity cliffs on the basis of matched molecular pairs.

Authors:  Xiaoying Hu; Ye Hu; Martin Vogt; Dagmar Stumpfe; Jürgen Bajorath
Journal:  J Chem Inf Model       Date:  2012-04-17       Impact factor: 4.956

2.  Lipophilic efficiency: the most important efficiency metric in medicinal chemistry.

Authors:  Kevin D Freeman-Cook; Robert L Hoffman; Ted W Johnson
Journal:  Future Med Chem       Date:  2013-02       Impact factor: 3.808

3.  PGE2 modulates the tetrodotoxin-resistant sodium current in neonatal rat dorsal root ganglion neurones via the cyclic AMP-protein kinase A cascade.

Authors:  S England; S Bevan; R J Docherty
Journal:  J Physiol       Date:  1996-09-01       Impact factor: 5.182

4.  The tetrodotoxin-resistant sodium channel SNS has a specialized function in pain pathways.

Authors:  A N Akopian; V Souslova; S England; K Okuse; N Ogata; J Ure; A Smith; B J Kerr; S B McMahon; S Boyce; R Hill; L C Stanfa; A H Dickenson; J N Wood
Journal:  Nat Neurosci       Date:  1999-06       Impact factor: 24.884

5.  Diversity of expression of the sensory neuron-specific TTX-resistant voltage-gated sodium ion channels SNS and SNS2.

Authors:  F Amaya; I Decosterd; T A Samad; C Plumpton; S Tate; R J Mannion; M Costigan; C J Woolf
Journal:  Mol Cell Neurosci       Date:  2000-04       Impact factor: 4.314

6.  Allometric scaling of pharmacokinetic parameters in drug discovery: can human CL, Vss and t1/2 be predicted from in-vivo rat data?

Authors:  Gary W Caldwell; John A Masucci; Zhengyin Yan; William Hageman
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2004 Apr-Jun       Impact factor: 2.441

7.  Gain-of-function Nav1.8 mutations in painful neuropathy.

Authors:  Catharina G Faber; Giuseppe Lauria; Ingemar S J Merkies; Xiaoyang Cheng; Chongyang Han; Hye-Sook Ahn; Anna-Karin Persson; Janneke G J Hoeijmakers; Monique M Gerrits; Tiziana Pierro; Raffaella Lombardi; Dimos Kapetis; Sulayman D Dib-Hajj; Stephen G Waxman
Journal:  Proc Natl Acad Sci U S A       Date:  2012-10-31       Impact factor: 11.205

8.  A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.

Authors:  Claire Elizabeth Payne; Adam R Brown; Jonathon W Theile; Alexandre J C Loucif; Aristos J Alexandrou; Mathew D Fuller; John H Mahoney; Brett M Antonio; Aaron C Gerlach; David M Printzenhoff; Rebecca L Prime; Gillian Stockbridge; Anthony J Kirkup; Anthony W Bannon; Steve England; Mark L Chapman; Sharan Bagal; Rosemarie Roeloffs; Uma Anand; Praveen Anand; Peter J Bungay; Mark Kemp; Richard P Butt; Edward B Stevens
Journal:  Br J Pharmacol       Date:  2015-04-10       Impact factor: 8.739

9.  Neuropathic pain develops normally in mice lacking both Na(v)1.7 and Na(v)1.8.

Authors:  Mohammed A Nassar; Alessandra Levato; L Caroline Stirling; John N Wood
Journal:  Mol Pain       Date:  2005-08-22       Impact factor: 3.395

10.  Pain without nociceptors? Nav1.7-independent pain mechanisms.

Authors:  Michael S Minett; Sarah Falk; Sonia Santana-Varela; Yury D Bogdanov; Mohammed A Nassar; Anne-Marie Heegaard; John N Wood
Journal:  Cell Rep       Date:  2014-01-16       Impact factor: 9.423
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  11 in total

1.  PF-06526290 can both enhance and inhibit conduction through voltage-gated sodium channels.

Authors:  Lingxin Wang; Shannon G Zellmer; David M Printzenhoff; Neil A Castle
Journal:  Br J Pharmacol       Date:  2018-06-03       Impact factor: 8.739

2.  The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.

Authors:  D C Pryde; N A Swain; P A Stupple; C W West; B Marron; C J Markworth; D Printzenhoff; Z Lin; P J Cox; R Suzuki; S McMurray; G J Waldron; C E Payne; J S Warmus; M L Chapman
Journal:  Medchemcomm       Date:  2017-04-28       Impact factor: 3.597

Review 3.  Voltage-gated Sodium Channels and Blockers: An Overview and Where Will They Go?

Authors:  Zhi-Mei Li; Li-Xia Chen; Hua Li
Journal:  Curr Med Sci       Date:  2019-12-16

Review 4.  Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform NaV1.7.

Authors:  John V Mulcahy; Hassan Pajouhesh; Jacob T Beckley; Anton Delwig; J Du Bois; John C Hunter
Journal:  J Med Chem       Date:  2019-05-07       Impact factor: 7.446

Review 5.  Status of peripheral sodium channel blockers for non-addictive pain treatment.

Authors:  Matthew Alsaloum; Grant P Higerd; Philip R Effraim; Stephen G Waxman
Journal:  Nat Rev Neurol       Date:  2020-10-27       Impact factor: 42.937

Review 6.  Evaluation of Nav1.8 as a therapeutic target for Pitt Hopkins Syndrome.

Authors:  Keri Martinowich; Debamitra Das; Srinidhi Rao Sripathy; Yishan Mai; Rakaia F Kenney; Brady J Maher
Journal:  Mol Psychiatry       Date:  2022-10-12       Impact factor: 13.437

Review 7.  Inhibition of NaV1.7: the possibility of ideal analgesics.

Authors:  Yutaka Kitano; Tsuyoshi Shinozuka
Journal:  RSC Med Chem       Date:  2022-08-01

Review 8.  Voltage gated sodium channels as drug discovery targets.

Authors:  Sharan K Bagal; Brian E Marron; Robert M Owen; R Ian Storer; Nigel A Swain
Journal:  Channels (Austin)       Date:  2015       Impact factor: 2.581

Review 9.  Managing Neuropathic Pain in Dogs.

Authors:  Sarah A Moore
Journal:  Front Vet Sci       Date:  2016-02-22

Review 10.  Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief.

Authors:  Edward C Emery; Ana Paula Luiz; John N Wood
Journal:  Expert Opin Ther Targets       Date:  2016-04-12       Impact factor: 6.902
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