Literature DB >> 15771431

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.

Devin M Swanson1, Adrienne E Dubin, Chandra Shah, Nadia Nasser, Leon Chang, Scott L Dax, Michele Jetter, J Guy Breitenbucher, Changlu Liu, Curt Mazur, Brian Lord, Lisa Gonzales, Kenway Hoey, Michele Rizzolio, Michael Bogenstaetter, Ellen E Codd, Doo H Lee, Sui-Po Zhang, Sandra R Chaplan, Nicholas I Carruthers.   

Abstract

High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified the essential pharmacophoric elements for antagonism that permitted further optimization via targeted synthesis to provide a potent orally bioavailable and selective TRPV1 modulator 41 active in several in vivo models.

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Year:  2005        PMID： 15771431     DOI： 10.1021/jm0495071

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


  40 in total

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Review 4.  Calcium signals that determine vascular resistance.

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5.  Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials.

Authors:  Ahmed A Othman; Wolfram Nothaft; Walid M Awni; Sandeep Dutta
Journal:  Br J Clin Pharmacol       Date:  2013-04       Impact factor: 4.335

6.  Altered pharmacology of native rodent spinal cord TRPV1 after phosphorylation.

Authors:  A J Mogg; C E J Mill; E A Folly; R E Beattie; M J Blanco; J P Beck; L M Broad
Journal:  Br J Pharmacol       Date:  2013-02       Impact factor: 8.739

7.  Jellyfish and other cnidarian envenomations cause pain by affecting TRPV1 channels.

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Review 8.  Update: the search for the human cough receptor.

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Review 9.  The cannabinoid system and pain.

Authors:  Stephen G Woodhams; Victoria Chapman; David P Finn; Andrea G Hohmann; Volker Neugebauer
Journal:  Neuropharmacology       Date:  2017-06-15       Impact factor: 5.250

10.  Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).

Authors:  Douglas S Johnson; Kay Ahn; Suzanne Kesten; Scott E Lazerwith; Yuntao Song; Mark Morris; Lorraine Fay; Tracy Gregory; Cory Stiff; James B Dunbar; Marya Liimatta; David Beidler; Sarah Smith; Tyzoon K Nomanbhoy; Benjamin F Cravatt
Journal:  Bioorg Med Chem Lett       Date:  2009-03-24       Impact factor: 2.823
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