Literature DB >> 11909730

The synthesis and structure-activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel opener targeted for urge urinary incontinence.

Piyasena Hewawasam1, Matthew Erway, George Thalody, Harvey Weiner, Christopher G Boissard, Valentin K Gribkoff, Nicholas A Meanwell, Nicholas Lodge, John E Starrett.   

Abstract

A series of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones was prepared and shown by electrophysiological analysis to activate a cloned maxi-K channel mSlo (or hSlo) expressed in Xenopus laevis oocytes. The effects of these structurally novel maxi-K channel openers on bladder contractile function were studied in vitro using isolated rat bladder strips pre-contracted with carbachol. Several 1,3-diaryl 1,2,4-(4H)-triazol-5-one derivatives were found to be potent smooth muscle relaxants but this activity did not completely correlate with maxi-K channel opening.

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Year:  2002        PMID： 11909730     DOI： 10.1016/s0960-894x(02)00099-9

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle.

Authors:  John Malysz; Steven A Buckner; Anthony V Daza; Ivan Milicic; Arturo Perez-Medrano; Murali Gopalakrishnan
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2004-04-17       Impact factor: 3.000

2.  BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle.

Authors:  Jeffrey J Layne; Bernhard Nausch; Søren-Peter Olesen; Mark T Nelson
Journal:  Am J Physiol Regul Integr Comp Physiol       Date:  2009-11-18       Impact factor: 3.619

3.  Suppression of human detrusor smooth muscle excitability and contractility via pharmacological activation of large conductance Ca2+-activated K+ channels.

Authors:  Kiril L Hristov; Shankar P Parajuli; Rupal P Soder; Qiuping Cheng; Eric S Rovner; Georgi V Petkov
Journal:  Am J Physiol Cell Physiol       Date:  2012-03-14       Impact factor: 4.249

Review 4.  Regulator of G-protein signaling (RGS) proteins as drug targets: Progress and future potentials.

Authors:  Joseph B O'Brien; Joshua C Wilkinson; David L Roman
Journal:  J Biol Chem       Date:  2019-10-21       Impact factor: 5.157

Review 5.  Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and beta-adrenoceptors.

Authors:  Elfaridah P Frazier; Stephan L M Peters; Alan S Braverman; Michael R Ruggieri; Martin C Michel
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2007-12-04       Impact factor: 3.000

6.  Inducible knockout mutagenesis reveals compensatory mechanisms elicited by constitutive BK channel deficiency in overactive murine bladder.

Authors:  Franz Sprossmann; Patrick Pankert; Ulrike Sausbier; Angela Wirth; Xiao-Bo Zhou; Johannes Madlung; Hong Zhao; Iancu Bucurenciu; Andreas Jakob; Tobias Lamkemeyer; Winfried Neuhuber; Stefan Offermanns; Michael J Shipston; Michael Korth; Alfred Nordheim; Peter Ruth; Matthias Sausbier
Journal:  FEBS J       Date:  2008-02-12       Impact factor: 5.542

7.  Urinary bladder instability induced by selective suppression of the murine small conductance calcium-activated potassium (SK3) channel.

Authors:  Gerald M Herrera; Maria J Pozo; Peter Zvara; Georgi V Petkov; Chris T Bond; John P Adelman; Mark T Nelson
Journal:  J Physiol       Date:  2003-06-17       Impact factor: 5.182

Review 8.  RGS proteins as targets in the treatment of intestinal inflammation and visceral pain: New insights and future perspectives.

Authors:  Maciej Salaga; Martin Storr; Kirill A Martemyanov; Jakub Fichna
Journal:  Bioessays       Date:  2016-01-28       Impact factor: 4.345

9.  Chemical genetics reveals an RGS/G-protein role in the action of a compound.

Authors:  Kevin Fitzgerald; Svetlana Tertyshnikova; Lisa Moore; Lynn Bjerke; Ben Burley; Jian Cao; Pamela Carroll; Robert Choy; Steve Doberstein; Yves Dubaquie; Yvonne Franke; Jenny Kopczynski; Hendrik Korswagen; Stanley R Krystek; Nicholas J Lodge; Ronald Plasterk; John Starrett; Terry Stouch; George Thalody; Honey Wayne; Alexander van der Linden; Yongmei Zhang; Stephen G Walker; Mark Cockett; Judi Wardwell-Swanson; Petra Ross-Macdonald; Rachel M Kindt
Journal:  PLoS Genet       Date:  2006-04-21       Impact factor: 5.917
  9 in total

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