Design of Potent, Orally Available Antagonists of the Transient Receptor Potential Vanilloid 1. Structure−Activity Relationships of 2-Piperazin-1-yl-1H-benzimidazoles

Vassil I. Ognyanov; Chenera Balan; Anthony W. Bannon; Yunxin Bo; Celia Dominguez; Christopher Fotsch; Vijay K. Gore; Lana Klionsky; Vu V. Ma; Yi-Xin Qian; Rami Tamir; Xianghong Wang; Ning Xi; Shimin Xu; Dawn Zhu; Narender R. Gavva; James J. S. Treanor; Mark H. Norman

doi:10.1021/jm060065y

Design of Potent, Orally Available Antagonists of the Transient Receptor Potential Vanilloid 1. Structure−Activity Relationships of 2-Piperazin-1-yl-1H-benzimidazoles

Journal of Medicinal Chemistry ◽

10.1021/jm060065y ◽

2006 ◽

Vol 49 (12) ◽

pp. 3719-3742 ◽

Cited By ~ 55

Author(s):

Vassil I. Ognyanov ◽

Chenera Balan ◽

Anthony W. Bannon ◽

Yunxin Bo ◽

Celia Dominguez ◽

...

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Structure Activity Relationships ◽

Structure Activity ◽

Transient Receptor

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Novel Transient Receptor Potential Vanilloid 1 Receptor Antagonists for the Treatment of Pain: Structure−Activity Relationships for Ureas with Quinoline, Isoquinoline, Quinazoline, Phthalazine, Quinoxaline, and Cinnoline Moieties

Journal of Medicinal Chemistry ◽

10.1021/jm0492958 ◽

2005 ◽

Vol 48 (3) ◽

pp. 744-752 ◽

Cited By ~ 111

Author(s):

Arthur Gomtsyan ◽

Erol K. Bayburt ◽

Robert G. Schmidt ◽

Guo Zhu Zheng ◽

Richard J. Perner ◽

...

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Transient Receptor

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2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as Potent Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonists: Structure–Activity Relationships of 2-Amino Derivatives in the N-(6-Trifluoromethylpyridin-3-ylmethyl) C-Region

Journal of Medicinal Chemistry ◽

10.1021/jm300780p ◽

2012 ◽

Vol 55 (19) ◽

pp. 8392-8408 ◽

Cited By ~ 29

Author(s):

Myeong Seop Kim ◽

HyungChul Ryu ◽

Dong Wook Kang ◽

Seong-Hee Cho ◽

Sejin Seo ◽

...

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Structure Activity Relationships ◽

Structure Activity ◽

Amino Derivatives ◽

Transient Receptor

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Modulation of the Transient Receptor Potential Vanilloid Channel TRPV4 by 4α-Phorbol Esters: A Structure−Activity Study

Journal of Medicinal Chemistry ◽

10.1021/jm9001007 ◽

2009 ◽

Vol 52 (9) ◽

pp. 2933-2939 ◽

Cited By ~ 47

Author(s):

Thomas Kjær Klausen ◽

Alberto Pagani ◽

Alberto Minassi ◽

Abdellah Ech-Chahad ◽

Jean Prenen ◽

...

Keyword(s):

Transient Receptor Potential ◽

Phorbol Esters ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Structure Activity ◽

Transient Receptor

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Structure-Activity Relationship of Capsaicin Analogs and Transient Receptor Potential Vanilloid 1-Mediated Human Lung Epithelial Cell Toxicity

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.110.178491 ◽

2011 ◽

Vol 337 (2) ◽

pp. 400-410 ◽

Cited By ~ 27

Author(s):

Karen C. Thomas ◽

Manivannan Ethirajan ◽

Kiumars Shahrokh ◽

Hao Sun ◽

Jeewoo Lee ◽

...

Keyword(s):

Transient Receptor Potential ◽

Human Lung ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Cell Toxicity ◽

Human Lung Epithelial Cell ◽

Structure Activity ◽

Lung Epithelial ◽

Transient Receptor ◽

Relationship Of

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In Vitro Structure−Activity Relationship and In Vivo Characterization of 1-(Aryl)-3-(4-(amino)benzyl)urea Transient Receptor Potential Vanilloid 1 Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm070276i ◽

2007 ◽

Vol 50 (15) ◽

pp. 3651-3660 ◽

Cited By ~ 19

Author(s):

Richard J. Perner ◽

Stanley DiDomenico ◽

John R. Koenig ◽

Arthur Gomtsyan ◽

Erol K. Bayburt ◽

...

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Activity Relationship ◽

Transient Receptor Potential Vanilloid ◽

Structure Activity ◽

Transient Receptor ◽

In Vivo Characterization

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Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management

Journal of Medicinal Chemistry ◽

10.1021/jm500818a ◽

2014 ◽

Vol 57 (15) ◽

pp. 6781-6794 ◽

Cited By ~ 16

Author(s):

Laykea Tafesse ◽

Toshiyuki Kanemasa ◽

Noriyuki Kurose ◽

Jianming Yu ◽

Toshiyuki Asaki ◽

...

Keyword(s):

Pain Management ◽

Transient Receptor Potential ◽

Receptor Potential ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Transient Receptor Potential Vanilloid ◽

Structure Activity ◽

Trpv1 Antagonist ◽

Transient Receptor ◽

Clinical Candidate

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Faculty Opinions recommendation of Transient receptor potential vanilloid 1 is required for intrinsic osmoreception in organum vasculosum lamina terminalis neurons and for normal thirst responses to systemic hyperosmolality.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1047186.497222 ◽

2006 ◽

Author(s):

Alastair Ferguson

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Lamina Terminalis ◽

Organum Vasculosum Lamina Terminalis ◽

Organum Vasculosum ◽

Transient Receptor

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Faculty Opinions recommendation of Transient receptor potential vanilloid 1 is required for intrinsic osmoreception in organum vasculosum lamina terminalis neurons and for normal thirst responses to systemic hyperosmolality.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1047186.497108 ◽

2006 ◽

Author(s):

Bernd Nilius

Keyword(s):

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Lamina Terminalis ◽

Organum Vasculosum Lamina Terminalis ◽

Organum Vasculosum ◽

Transient Receptor

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Faculty Opinions recommendation of Somatostatin modulates the transient receptor potential vanilloid 1 (TRPV1) ion channel.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1052995.504951 ◽

2006 ◽

Author(s):

Marcos Milla

Keyword(s):

Ion Channel ◽

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Transient Receptor

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Faculty Opinions recommendation of A specific subset of transient receptor potential vanilloid-type channel subunits in Caenorhabditis elegans endocrine cells function as mixed heteromers to promote neurotransmitter release.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1063770.516694 ◽

2007 ◽

Author(s):

Oliver Hobert

Keyword(s):

Caenorhabditis Elegans ◽

Neurotransmitter Release ◽

Endocrine Cells ◽

Transient Receptor Potential ◽

Receptor Potential ◽

Transient Receptor Potential Vanilloid ◽

Specific Subset ◽

Transient Receptor

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