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Orvinols with mixed kappa/mu opioid receptor agonist activity.

Greedy BM, Bradbury F, Thomas MP, Grivas K, Cami-Kobeci G, Archambeau A, Bosse K, Clark MJ, Aceto M, Lewis JW, Traynor JR, Husbands SM.

J Med Chem. 2013 Apr 25;56(8):3207-16. doi: 10.1021/jm301543e.


Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.

Harland AA, Yeomans L, Griggs NW, Anand JP, Pogozheva ID, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2015 Nov 25;58(22):8952-69. doi: 10.1021/acs.jmedchem.5b01270.


Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines.

Cami-Kobeci G, Neal AP, Bradbury FA, Purington LC, Aceto MD, Harris LS, Lewis JW, Traynor JR, Husbands SM.

J Med Chem. 2009 Mar 26;52(6):1546-52. doi: 10.1021/jm8015552.


Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.

Neumeyer JL, Zhang B, Zhang T, Sromek AW, Knapp BI, Cohen DJ, Bidlack JM.

J Med Chem. 2012 Apr 26;55(8):3878-90. doi: 10.1021/jm3001086.


Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting.

Zhou L, Stahl EL, Lovell KM, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:131-41. doi: 10.1016/j.neuropharm.2015.07.001.


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

Mathews JL, Peng X, Xiong W, Zhang A, Negus SS, Neumeyer JL, Bidlack JM.

J Pharmacol Exp Ther. 2005 Nov;315(2):821-7.


Mixed κ/μ partial opioid agonists as potential treatments for cocaine dependence.

Bidlack JM.

Adv Pharmacol. 2014;69:387-418. doi: 10.1016/B978-0-12-420118-7.00010-X. Review.


Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.

Chauvignac C, Miller CN, Srivastava SK, Lewis JW, Husbands SM, Traynor JR.

J Med Chem. 2005 Mar 10;48(5):1676-9.


Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

Li G, Aschenbach LC, Chen J, Cassidy MP, Stevens DL, Gabra BH, Selley DE, Dewey WL, Westkaemper RB, Zhang Y.

J Med Chem. 2009 Mar 12;52(5):1416-27. doi: 10.1021/jm801272c.


LPK-26, a novel kappa-opioid receptor agonist with potent antinociceptive effects and low dependence potential.

Tao YM, Li QL, Zhang CF, Xu XJ, Chen J, Ju YW, Chi ZQ, Long YQ, Liu JG.

Eur J Pharmacol. 2008 Apr 28;584(2-3):306-11. doi: 10.1016/j.ejphar.2008.02.028.


Design of high affinity cyclic pentapeptide ligands for kappa-opioid receptors.

Przydzial MJ, Pogozheva ID, Ho JC, Bosse KE, Sawyer E, Traynor JR, Mosberg HI.

J Pept Res. 2005 Nov;66(5):255-62.


C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.

Cueva JP, Roche C, Ostovar M, Kumar V, Clark MJ, Hillhouse TM, Lewis JW, Traynor JR, Husbands SM.

J Med Chem. 2015 May 28;58(10):4242-9. doi: 10.1021/acs.jmedchem.5b00130.


Characterization of the binding of [3H][Dmt1]H-Dmt-D-Arg-Phe-Lys-NH2, a highly potent opioid peptide.

Neilan CL, Janvey AJ, Bolan E, Berezowska I, Nguyen TM, Schiller PW, Pasternak GW.

J Pharmacol Exp Ther. 2003 Aug;306(2):430-6.


Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.

Cheng MF, Ou LC, Chen SC, Chang WT, Law PY, Loh HH, Chao YS, Shih C, Yeh SH, Ueng SH.

Bioorg Med Chem. 2014 Sep 1;22(17):4694-703. doi: 10.1016/j.bmc.2014.07.012.


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