Literature DB >> 15808478

Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.

Mark P Wentland1, Qun Lu, Rongliang Lou, Yigong Bu, Brian I Knapp, Jean M Bidlack.   

Abstract

Very high affinity for opioid receptors (e.g., K(i)=0.052nM for mu) has been observed in the rationally designed naltrexone analogue 5. SAR and physical data supports the hypothesis that the 4-OH group of 5 stabilizes the 3-carboxamido group in the putative bioactive conformation.

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Year:  2005        PMID： 15808478     DOI： 10.1016/j.bmcl.2005.02.032

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


  6 in total

Review 1.  Targeting opioid dysregulation in depression for the development of novel therapeutics.

Authors:  Caroline A Browne; Irwin Lucki
Journal:  Pharmacol Ther       Date:  2019-04-30       Impact factor: 12.310

2.  Syntheses of novel high affinity ligands for opioid receptors.

Authors:  Mark P Wentland; Rongliang Lou; Qun Lu; Yigong Bu; Christoph Denhardt; Jin Jin; Rakesh Ganorkar; Melissa A VanAlstine; Chengyun Guo; Dana J Cohen; Jean M Bidlack
Journal:  Bioorg Med Chem Lett       Date:  2009-02-25       Impact factor: 2.823

3.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.

Authors:  Mark P Wentland; Xufeng Sun; Dana J Cohen; Jean M Bidlack
Journal:  Bioorg Med Chem       Date:  2008-03-30       Impact factor: 3.641

4.  Evaluation of opioid modulation in major depressive disorder.

Authors:  Elliot Ehrich; Ryan Turncliff; Yangchun Du; Richard Leigh-Pemberton; Emilio Fernandez; Reese Jones; Maurizio Fava
Journal:  Neuropsychopharmacology       Date:  2014-12-18       Impact factor: 7.853

5.  Samidorphan mitigates olanzapine-induced weight gain and metabolic dysfunction in rats and non-human primates.

Authors:  Jacobi I Cunningham; David J Eyerman; Mark S Todtenkopf; Reginald L Dean; Daniel R Deaver; Connie Sanchez; Mark Namchuk
Journal:  J Psychopharmacol       Date:  2019-07-11       Impact factor: 4.153

6.  Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age.

Authors:  Vipul Kumar; Hong Lu; Marjie Hard; Lisa von Moltke
Journal:  Drugs R D       Date:  2019-09
  6 in total

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