Literature DB >> 28892388

Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).

Larry V Pearce1, Jihyae Ann2, Aeran Jung2, Shivaji A Thorat2, Brienna K A Herold1, Amelework D Habtemichael1, Peter M Blumberg1, Jeewoo Lee2.   

Abstract

Transient receptor potential vanilloid 1 (TRPV1) has emerged as a promising therapeutic target. While radiolabeled resiniferatoxin (RTX) has provided a powerful tool for characterization of vanilloid binding to TRPV1, TRPV1 shows 20-fold weaker binding to the human TRPV1 than to the rodent TRPV1. We now describe a tritium radiolabeled synthetic vanilloid antagonist, 1-((2-(4-(methyl-[3H])piperidin-1-yl-4-[3H])-6-(trifluoromethyl)pyridin-3-yl)methyl)-3-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)urea ([3H]MPOU), that embodies improved absolute affinity for human TRPV1 and improved synthetic accessibility.

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Year:  2017        PMID： 28892388      PMCID： PMC6959550          DOI： 10.1021/acs.jmedchem.7b00859

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


  29 in total

1.  The capsaicin receptor: a heat-activated ion channel in the pain pathway.

Authors:  M J Caterina; M A Schumacher; M Tominaga; T A Rosen; J D Levine; D Julius
Journal:  Nature       Date:  1997-10-23       Impact factor: 49.962

Review 2.  Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014).

Authors:  Yoonji Lee; Sunhye Hong; Minghua Cui; Pankaz K Sharma; Jeewoo Lee; Sun Choi
Journal:  Expert Opin Ther Pat       Date:  2015-03       Impact factor: 6.674

Review 3.  Recent progress in the development of selective TRPV1 antagonists for pain.

Authors:  Lisa M Broad; Stacy J Keding; Maria-Jesus Blanco
Journal:  Curr Top Med Chem       Date:  2008       Impact factor: 3.295

4.  N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Authors:  Kenneth J Valenzano; Elfrida R Grant; Gang Wu; Mohamed Hachicha; Lori Schmid; Laykea Tafesse; Qun Sun; Yakov Rotshteyn; Joseph Francis; James Limberis; Shiazah Malik; Edward R Whittemore; Dianne Hodges
Journal:  J Pharmacol Exp Ther       Date:  2003-04-29       Impact factor: 4.030

5.  [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.

Authors:  Bruce R Bianchi; Rachid El Kouhen; Torben R Neelands; Chih-Hung Lee; Arthur Gomtsyan; Shirish N Raja; Sriajan N Vaidyanathan; Bruce Surber; Heath A McDonald; Carol S Surowy; Connie R Faltynek; Robert B Moreland; Michael F Jarvis; Pamela S Puttfarcken
Journal:  J Pharmacol Exp Ther       Date:  2007-07-27       Impact factor: 4.030

6.  Molecular determinants of vanilloid sensitivity in TRPV1.

Authors:  Narender R Gavva; Lana Klionsky; Yusheng Qu; Licheng Shi; Rami Tamir; Steve Edenson; T J Zhang; Vellarkad N Viswanadhan; Attila Toth; Larry V Pearce; Todd W Vanderah; Frank Porreca; Peter M Blumberg; Jack Lile; Yax Sun; Ken Wild; Jean-Claude Louis; James J S Treanor
Journal:  J Biol Chem       Date:  2004-03-02       Impact factor: 5.157

7.  Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper.

Authors:  A Szallasi; P M Blumberg
Journal:  Neuroscience       Date:  1989       Impact factor: 3.590

8.  Multi-Functional Diarylurea Small Molecule Inhibitors of TRPV1 with Therapeutic Potential for Neuroinflammation.

Authors:  Zhiwei Feng; Larry V Pearce; Yu Zhang; Changrui Xing; Brienna K A Herold; Shifan Ma; Ziheng Hu; Noe A Turcios; Peng Yang; Qin Tong; Anna K McCall; Peter M Blumberg; Xiang-Qun Xie
Journal:  AAPS J       Date:  2016-03-21       Impact factor: 4.009

9.  Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.

Authors:  Jihyae Ann; Wei Sun; Xing Zhou; Aeran Jung; Jisoo Baek; Sunho Lee; Changhoon Kim; Suyoung Yoon; Sunhye Hong; Sun Choi; Noe A Turcios; Brienna K A Herold; Timothy E Esch; Nancy E Lewin; Adelle Abramovitz; Larry V Pearce; Peter M Blumberg; Jeewoo Lee
Journal:  Bioorg Med Chem Lett       Date:  2016-06-07       Impact factor: 2.823

10.  Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia.

Authors:  Andras Garami; Yury P Shimansky; Eszter Pakai; Daniela L Oliveira; Narender R Gavva; Andrej A Romanovsky
Journal:  J Neurosci       Date:  2010-01-27       Impact factor: 6.167
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  1 in total

1.  Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.

Authors:  Hobin Lee; Songyeon Ahn; Jihyae Ann; Heejin Ha; Young Dong Yoo; Young Ho Kim; Ji-Young Hwang; Kwang-Hyun Hur; Choon-Gon Jang; Larry V Pearce; Timothy E Esch; Nancy E Lewin; Peter M Blumberg; Jeewoo Lee
Journal:  Eur J Med Chem       Date:  2019-08-21       Impact factor: 6.514
  1 in total

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