Literature DB >> 23131342

Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.

Hazel J Hunt1, Nicholas C Ray, George Hynd, Jon Sutton, Mohammed Sajad, Elizabeth O'Connor, Shahadat Ahmed, Peter Lockey, Steve Daly, Gerry Buckley, Robin D Clark, Robert Roe, Christine Blasey, Joe Belanoff.   

Abstract

We report the optimization of a series of non-steroidal GR antagonists that led to the identification of compound 7. This compound is efficacious when dosed orally in an olanzapine-induced weight gain model in rats.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 23131342     DOI： 10.1016/j.bmcl.2012.10.074

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


  10 in total

Review 1.  Corticosteroid Action in the Brain: The Potential of Selective Receptor Modulation.

Authors:  Eva M G Viho; Jacobus C Buurstede; Ahmed Mahfouz; Lisa L Koorneef; Lisa T C M van Weert; René Houtman; Hazel J Hunt; Jan Kroon; Onno C Meijer
Journal:  Neuroendocrinology       Date:  2019-03-19       Impact factor: 4.914

2.  Selective Glucocorticoid Receptor Modulators (SGRMs) Delay Castrate-Resistant Prostate Cancer Growth.

Authors:  Jacob Kach; Tiha M Long; Phillip Selman; Eva Y Tonsing-Carter; Maria A Bacalao; Ricardo R Lastra; Larischa de Wet; Shane Comiskey; Marc Gillard; Calvin VanOpstall; Diana C West; Wen-Ching Chan; Donald Vander Griend; Suzanne D Conzen; Russell Z Szmulewitz
Journal:  Mol Cancer Ther       Date:  2017-04-20       Impact factor: 6.261

3.  A mixed glucocorticoid/mineralocorticoid receptor modulator dampens endocrine and hippocampal stress responsivity in male rats.

Authors:  Elizabeth T Nguyen; Joshua Streicher; Sarah Berman; Jody L Caldwell; Valentina Ghisays; Christina M Estrada; Aynara C Wulsin; Matia B Solomon
Journal:  Physiol Behav       Date:  2017-01-14

4.  Psychosocial Stress, Glucocorticoid Signaling, and Prostate Cancer Health Disparities in African American Men.

Authors:  Leanne Woods-Burnham; Laura Stiel; Shannalee R Martinez; Evelyn S Sanchez-Hernandez; Herbert C Ruckle; Frankis G Almaguel; Mariana C Stern; Lisa R Roberts; David R Williams; Susanne Montgomery; Carlos A Casiano
Journal:  Cancer Health Disparities       Date:  2020

5.  Discovery of a Glucocorticoid Receptor (GR) Activity Signature Using Selective GR Antagonism in ER-Negative Breast Cancer.

Authors:  Diana C West; Masha Kocherginsky; Eva Y Tonsing-Carter; D Nesli Dolcen; David J Hosfield; Ricardo R Lastra; Jason P Sinnwell; Kevin J Thompson; Kathleen R Bowie; Ryan V Harkless; Maxwell N Skor; Charles F Pierce; Sarah C Styke; Caroline R Kim; Larischa de Wet; Geoffrey L Greene; Judy C Boughey; Matthew P Goetz; Krishna R Kalari; Liewei Wang; Gini F Fleming; Balázs Györffy; Suzanne D Conzen
Journal:  Clin Cancer Res       Date:  2018-04-10       Impact factor: 12.531

6.  A novel combined glucocorticoid-mineralocorticoid receptor selective modulator markedly prevents weight gain and fat mass expansion in mice fed a high-fat diet.

Authors:  C Mammi; V Marzolla; A Armani; A Feraco; A Antelmi; E Maslak; S Chlopicki; F Cinti; H Hunt; A Fabbri; M Caprio
Journal:  Int J Obes (Lond)       Date:  2016-02-02       Impact factor: 5.095

7.  Glucocorticoid receptor modulators decrease alcohol self-administration in male rats.

Authors:  M Adrienne McGinn; Brendan J Tunstall; Joel E Schlosburg; Adriana Gregory-Flores; Olivier George; Giordano de Guglielmo; Barbara J Mason; Hazel J Hunt; George F Koob; Leandro F Vendruscolo
Journal:  Neuropharmacology       Date:  2021-02-26       Impact factor: 5.250

8.  ETS Proteins Bind with Glucocorticoid Receptors: Relevance for Treatment of Ewing Sarcoma.

Authors:  Swati Srivastava; Nishanth Belugali Nataraj; Arunachalam Sekar; Soma Ghosh; Chamutal Bornstein; Diana Drago-Garcia; Lee Roth; Donatella Romaniello; Ilaria Marrocco; Eyal David; Yuval Gilad; Mattia Lauriola; Ron Rotkopf; Adi Kimchi; Yuya Haga; Yasuo Tsutsumi; Olivier Mirabeau; Didier Surdez; Andrei Zinovyev; Olivier Delattre; Heinrich Kovar; Ido Amit; Yosef Yarden
Journal:  Cell Rep       Date:  2019-10-01       Impact factor: 9.423

9.  The infralimbic mineralocorticoid blockage prevents the stress-induced impairment of aversive memory extinction in rats.

Authors:  Kairo Alan Albernaz-Mariano; Carolina Demarchi Munhoz
Journal:  Transl Psychiatry       Date:  2022-08-24       Impact factor: 7.989

10.  Effect of Miricorilant, a Selective Glucocorticoid Receptor Modulator, on Olanzapine-Associated Weight Gain in Healthy Subjects: A Proof-of-Concept Study.

Authors:  Hazel J Hunt; Kirsteen Donaldson; Mark Strem; Iulia Cristina Tudor; Suzanne Sweet-Smith; Sharan Sidhu
Journal:  J Clin Psychopharmacol       Date:  2021 Nov-Dec 01       Impact factor: 3.153
  10 in total

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