Literature DB >> 20144870

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.

Brian S Fulton1, Brian L Knapp, Jean M Bidlack, John L Neumeyer.   

Abstract

A series of bivalent hydroxy ether butorphan ligands were prepared and their binding affinities at the opioid receptors determined. Addition of a hydroxy group to a hydrocarbon chain can potentiate binding affinity up to 27- and 86-fold at the mu and kappa opioid receptors, respectively. Two bivalent ligands with sub-nanomolar binding affinity at the mu and kappa opioid receptors were discovered. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20144870      PMCID： PMC2834170          DOI： 10.1016/j.bmcl.2010.01.101

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


  11 in total

1.  Effects of mixed-action kappa/mu opioids on cocaine self-administration and cocaine discrimination by rhesus monkeys.

Authors:  Carrie A Bowen; S Stevens Negus; Rushi Zong; John L Neumeyer; Jean M Bidlack; Nancy K Mello
Journal:  Neuropsychopharmacology       Date:  2003-03-05       Impact factor: 7.853

2.  A role for heterodimerization of mu and delta opiate receptors in enhancing morphine analgesia.

Authors:  Ivone Gomes; Achla Gupta; Julija Filipovska; Hazel H Szeto; John E Pintar; Lakshmi A Devi
Journal:  Proc Natl Acad Sci U S A       Date:  2004-03-24       Impact factor: 11.205

3.  Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.

Authors:  John L Neumeyer; Ao Zhang; Wennan Xiong; Xiao-Hui Gu; James E Hilbert; Brian I Knapp; S Stevens Negus; Nancy K Mello; Jean M Bidlack
Journal:  J Med Chem       Date:  2003-11-20       Impact factor: 7.446

4.  Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.

Authors:  J L Neumeyer; J M Bidlack; R Zong; V Bakthavachalam; P Gao; D J Cohen; S S Negus; N K Mello
Journal:  J Med Chem       Date:  2000-01-13       Impact factor: 7.446

5.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.

Authors:  Mark P Wentland; Melissa VanAlstine; Robert Kucejko; Rongliang Lou; Dana J Cohen; Amy L Parkhill; Jean M Bidlack
Journal:  J Med Chem       Date:  2006-09-07       Impact factor: 7.446

6.  Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.

Authors:  Brian S Fulton; Brian I Knapp; Jean M Bidlack; John L Neumeyer
Journal:  Bioorg Med Chem Lett       Date:  2008-07-17       Impact factor: 2.823

7.  Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.

Authors:  Michael Decker; Brian S Fulton; Bin Zhang; Brian I Knapp; Jean M Bidlack; John L Neumeyer
Journal:  J Med Chem       Date:  2009-12-10       Impact factor: 7.446

8.  Identity of the putative delta1-opioid receptor as a delta-kappa heteromer in the mouse spinal cord.

Authors:  Philip S Portoghese; Mary M Lunzer
Journal:  Eur J Pharmacol       Date:  2003-04-25       Impact factor: 4.432

9.  Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.

Authors:  Jennifer L Mathews; Xuemei Peng; Wennan Xiong; Ao Zhang; S Stevens Negus; John L Neumeyer; Jean M Bidlack
Journal:  J Pharmacol Exp Ther       Date:  2005-08-02       Impact factor: 4.030

10.  In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: isomeric, bivalent ligands with mu/kappa agonist properties.

Authors:  Jennifer L Mathews; Brian S Fulton; S Stevens Negus; John L Neumeyer; Jean M Bidlack
Journal:  Neurochem Res       Date:  2008-06-05       Impact factor: 3.996
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  4 in total

1.  Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.

Authors:  Gianfranco Balboni; Severo Salvadori; Ewa D Marczak; Brian I Knapp; Jean M Bidlack; Lawrence H Lazarus; Xuemei Peng; Yu Gui Si; John L Neumeyer
Journal:  Eur J Med Chem       Date:  2010-12-08       Impact factor: 6.514

Review 2.  An Update on Non-CB1, Non-CB2 Cannabinoid Related G-Protein-Coupled Receptors.

Authors:  Paula Morales; Patricia H Reggio
Journal:  Cannabis Cannabinoid Res       Date:  2017-10-01

Review 3.  Biased, Bitopic, Opioid-Adrenergic Tethered Compounds May Improve Specificity, Lower Dosage and Enhance Agonist or Antagonist Function with Reduced Risk of Tolerance and Addiction.

Authors:  Robert Root-Bernstein
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-10

Review 4.  Targeting Cannabinoid CB2 Receptors in the Central Nervous System. Medicinal Chemistry Approaches with Focus on Neurodegenerative Disorders.

Authors:  Gemma Navarro; Paula Morales; Carmen Rodríguez-Cueto; Javier Fernández-Ruiz; Nadine Jagerovic; Rafael Franco
Journal:  Front Neurosci       Date:  2016-09-13       Impact factor: 4.677
  4 in total

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