Literature DB >> 10340620

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

P D Williams1, M G Bock, B E Evans, R M Freidinger, S N Gallicchio, M T Guidotti, M A Jacobson, M S Kuo, M R Levy, E V Lis, S R Michelson, J M Pawluczyk, D S Perlow, D J Pettibone, A G Quigley, D R Reiss, C Salvatore, K J Stauffer, C J Woyden.   

Abstract

Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; Ki = 1.4 nM).

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Year:  1999        PMID: 10340620     DOI: 10.1016/s0960-894x(99)00181-x

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


  4 in total

1.  Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.

Authors:  Cristiana Griffante; Andrew Green; Ornella Curcuruto; Carl P Haslam; Bryony A Dickinson; Roberto Arban
Journal:  Br J Pharmacol       Date:  2005-11       Impact factor: 8.739

2.  The 3D structure of the binding pocket of the human oxytocin receptor for benzoxazine antagonists, determined by molecular docking, scoring functions and 3D-QSAR methods.

Authors:  Balázs Jójárt; Tamás A Martinek; Arpád Márki
Journal:  J Comput Aided Mol Des       Date:  2005-05       Impact factor: 3.686

3.  Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.

Authors:  Aaron L Smith; Sara M Freeman; Jeffery S Stehouwer; Kiyoshi Inoue; Ronald J Voll; Larry J Young; Mark M Goodman
Journal:  Bioorg Med Chem       Date:  2012-02-25       Impact factor: 3.641

4.  Differential contributions of vasopressin V1A and oxytocin receptors in the amygdala to pain-related behaviors in rats.

Authors:  Bryce Cragg; Guangchen Ji; Volker Neugebauer
Journal:  Mol Pain       Date:  2016-11-11       Impact factor: 3.395

  4 in total

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