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Peripherally Acting µ-Opioid Receptor Antagonists for the Treatment of Opioid-Related Side Effects: Mechanism of Action and Clinical Implications.

Streicher JM, Bilsky EJ.

J Pharm Pract. 2017 Sep 25:897190017732263. doi: 10.1177/0897190017732263. [Epub ahead of print]


Long-term morphine delivery via slow release morphine pellets or osmotic pumps: Plasma concentration, analgesia, and naloxone-precipitated withdrawal.

McLane VD, Bergquist I, Cormier J, Barlow DJ, Houseknecht KL, Bilsky EJ, Cao L.

Life Sci. 2017 Sep 15;185:1-7. doi: 10.1016/j.lfs.2017.07.016. Epub 2017 Jul 16.


Exercise reverses pain-related weight asymmetry and differentially modulates trabecular bone microarchitecture in a rat model of osteoarthritis.

Cormier J, Cone K, Lanpher J, Kinens A, Henderson T, Liaw L, Bilsky EJ, King T, Rosen CJ, Stevenson GW.

Life Sci. 2017 Jul 1;180:51-59. doi: 10.1016/j.lfs.2017.05.011. Epub 2017 May 11.


Heat-shock protein 90 (Hsp90) promotes opioid-induced anti-nociception by an ERK mitogen-activated protein kinase (MAPK) mechanism in mouse brain.

Lei W, Mullen N, McCarthy S, Brann C, Richard P, Cormier J, Edwards K, Bilsky EJ, Streicher JM.

J Biol Chem. 2017 Jun 23;292(25):10414-10428. doi: 10.1074/jbc.M116.769489. Epub 2017 Apr 27.


FAAH inhibitor OL-135 disrupts contextual, but not auditory, fear conditioning in rats.

Burman MA, Szolusha K, Bind R, Kerney K, Boger DL, Bilsky EJ.

Behav Brain Res. 2016 Jul 15;308:1-5. doi: 10.1016/j.bbr.2016.04.014. Epub 2016 Apr 13.


17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-(4'-pyridylcarboxamido)morphinan (NAP) Modulating the Mu Opioid Receptor in a Biased Fashion.

Zhang Y, Williams DA, Zaidi SA, Yuan Y, Braithwaite A, Bilsky EJ, Dewey WL, Akbarali HI, Streicher JM, Selley DE.

ACS Chem Neurosci. 2016 Mar 16;7(3):297-304. doi: 10.1021/acschemneuro.5b00245. Epub 2016 Jan 8.


Evaluation of a Postoperative Pain-Like State on Motivated Behavior in Rats: Effects of Plantar Incision on Progressive-Ratio Food-Maintained Responding.

Warner E, Krivitsky R, Cone K, Atherton P, Pitre T, Lanpher J, Giuvelis D, Bergquist I, King T, Bilsky EJ, Stevenson GW.

Drug Dev Res. 2015 Dec;76(8):432-41. doi: 10.1002/ddr.21284. Epub 2015 Oct 23.


Structural Requirements for CNS Active Opioid Glycopeptides.

Lefever M, Li Y, Anglin B, Muthu D, Giuvelis D, Lowery JJ, Knapp BI, Bidlack JM, Bilsky EJ, Polt R.

J Med Chem. 2015 Aug 13;58(15):5728-41. doi: 10.1021/acs.jmedchem.5b00014. Epub 2015 Jul 23.


The mixed-action delta/mu opioid agonist MMP-2200 does not produce conditioned place preference but does maintain drug self-administration in rats, and induces in vitro markers of tolerance and dependence.

Stevenson GW, Luginbuhl A, Dunbar C, LaVigne J, Dutra J, Atherton P, Bell B, Cone K, Giuvelis D, Polt R, Streicher JM, Bilsky EJ.

Pharmacol Biochem Behav. 2015 May;132:49-55. doi: 10.1016/j.pbb.2015.02.022. Epub 2015 Feb 28.


K-12 Neuroscience Education Outreach Program: Interactive Activities for Educating Students about Neuroscience.

Deal AL, Erickson KJ, Bilsky EJ, Hillman SJ, Burman MA.

J Undergrad Neurosci Educ. 2014 Oct 15;13(1):A8-A20. eCollection 2014 Fall.


Behavioral and cellular pharmacology characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) as a mu opioid receptor selective ligand.

Zhang Y, Braithwaite A, Yuan Y, Streicher JM, Bilsky EJ.

Eur J Pharmacol. 2014 Aug 5;736:124-30. doi: 10.1016/j.ejphar.2014.04.041. Epub 2014 May 8.


Can amphipathic helices influence the CNS antinociceptive activity of glycopeptides related to β-endorphin?

Li Y, St Louis L, Knapp BI, Muthu D, Anglin B, Giuvelis D, Bidlack JM, Bilsky EJ, Polt R.

J Med Chem. 2014 Mar 27;57(6):2237-46. doi: 10.1021/jm400879w. Epub 2014 Mar 7.


Novel fentanyl-based dual μ/δ-opioid agonists for the treatment of acute and chronic pain.

Podolsky AT, Sandweiss A, Hu J, Bilsky EJ, Cain JP, Kumirov VK, Lee YS, Hruby VJ, Vardanyan RS, Vanderah TW.

Life Sci. 2013 Dec 18;93(25-26):1010-6. doi: 10.1016/j.lfs.2013.09.016. Epub 2013 Sep 29.


Building a better analgesic: multifunctional compounds that address injury-induced pathology to enhance analgesic efficacy while eliminating unwanted side effects.

Largent-Milnes TM, Brookshire SW, Skinner DP Jr, Hanlon KE, Giuvelis D, Yamamoto T, Davis P, Campos CR, Nair P, Deekonda S, Bilsky EJ, Porreca F, Hruby VJ, Vanderah TW.

J Pharmacol Exp Ther. 2013 Oct;347(1):7-19. doi: 10.1124/jpet.113.205245. Epub 2013 Jul 16.


14-Alkoxy- and 14-acyloxypyridomorphinans: μ agonist/δ antagonist opioid analgesics with diminished tolerance and dependence side effects.

Ananthan S, Saini SK, Dersch CM, Xu H, McGlinchey N, Giuvelis D, Bilsky EJ, Rothman RB.

J Med Chem. 2012 Oct 11;55(19):8350-63. doi: 10.1021/jm300686p. Epub 2012 Sep 27.


6β-N-heterocyclic substituted naltrexamine derivative NAP as a potential lead to develop peripheral mu opioid receptor selective antagonists.

Yuan Y, Stevens DL, Braithwaite A, Scoggins KL, Bilsky EJ, Akbarali HI, Dewey WL, Zhang Y.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4731-4. doi: 10.1016/j.bmcl.2012.05.075. Epub 2012 May 26.


Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins.

Li Y, Lefever MR, Muthu D, Bidlack JM, Bilsky EJ, Polt R.

Future Med Chem. 2012 Feb;4(2):205-26. doi: 10.4155/fmc.11.195. Review.


Phosphorylation of enkephalins: NMR and CD studies in aqueous and membrane-mimicking environments.

Yeomans L, Muthu D, Lowery JJ, Martinez HN, Abrell L, Lin G, Strom K, Knapp BI, Bidlack JM, Bilsky EJ, Polt R.

Chem Biol Drug Des. 2011 Nov;78(5):749-56. doi: 10.1111/j.1747-0285.2011.01203.x. Epub 2011 Sep 26.


Selective ablation of mu-opioid receptor expressing neurons in the rostral ventromedial medulla attenuates stress-induced mechanical hypersensitivity.

Reynolds J, Bilsky EJ, Meng ID.

Life Sci. 2011 Aug 29;89(9-10):313-9. doi: 10.1016/j.lfs.2011.06.024. Epub 2011 Jul 6.


Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics.

Ezzili C, Mileni M, McGlinchey N, Long JZ, Kinsey SG, Hochstatter DG, Stevens RC, Lichtman AH, Cravatt BF, Bilsky EJ, Boger DL.

J Med Chem. 2011 Apr 28;54(8):2805-22. doi: 10.1021/jm101597x. Epub 2011 Mar 23.


Monosodium iodoacetate-induced osteoarthritis produces pain-depressed wheel running in rats: implications for preclinical behavioral assessment of chronic pain.

Stevenson GW, Mercer H, Cormier J, Dunbar C, Benoit L, Adams C, Jezierski J, Luginbuhl A, Bilsky EJ.

Pharmacol Biochem Behav. 2011 Mar;98(1):35-42. doi: 10.1016/j.pbb.2010.12.009. Epub 2010 Dec 10.


In vivo characterization of MMP-2200, a mixed δ/μ opioid agonist, in mice.

Lowery JJ, Raymond TJ, Giuvelis D, Bidlack JM, Polt R, Bilsky EJ.

J Pharmacol Exp Ther. 2011 Mar;336(3):767-78. doi: 10.1124/jpet.110.172866. Epub 2010 Nov 30.


In vitro and in vivo assessment of mu opioid receptor constitutive activity.

Bilsky EJ, Giuvelis D, Osborn MD, Dersch CM, Xu H, Rothman RB.

Methods Enzymol. 2010;484:413-43. doi: 10.1016/B978-0-12-381298-8.00021-6.


Rationale and methods for assessment of pain-depressed behavior in preclinical assays of pain and analgesia.

Negus SS, Bilsky EJ, Do Carmo GP, Stevenson GW.

Methods Mol Biol. 2010;617:79-91. doi: 10.1007/978-1-60327-323-7_7.


In vivo characterization of the opioid antagonist nalmefene in mice.

Osborn MD, Lowery JJ, Skorput AG, Giuvelis D, Bilsky EJ.

Life Sci. 2010 Apr 10;86(15-16):624-30. doi: 10.1016/j.lfs.2010.02.013. Epub 2010 Feb 14.


Identification of a novel "almost neutral" micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptor.

Sally EJ, Xu H, Dersch CM, Hsin LW, Chang LT, Prisinzano TE, Simpson DS, Giuvelis D, Rice KC, Jacobson AE, Cheng K, Bilsky EJ, Rothman RB.

Synapse. 2010 Apr;64(4):280-8. doi: 10.1002/syn.20723.


6beta-naltrexol preferentially antagonizes opioid effects on gastrointestinal transit compared to antinociception in mice.

Yancey-Wrona JE, Raymond TJ, Mercer HK, Sadée W, Bilsky EJ.

Life Sci. 2009 Sep 9;85(11-12):413-20. doi: 10.1016/j.lfs.2009.06.016. Epub 2009 Jul 5.


Targeting pain-depressed behaviors in preclinical assays of pain and analgesia: drug effects on acetic acid-depressed locomotor activity in ICR mice.

Stevenson GW, Cormier J, Mercer H, Adams C, Dunbar C, Negus SS, Bilsky EJ.

Life Sci. 2009 Aug 12;85(7-8):309-15. doi: 10.1016/j.lfs.2009.06.006. Epub 2009 Jun 24.


Glycosyl-enkephalins: synthesis and binding at the mu, delta & kappa opioid receptors. Antinociception in mice.

Keyari CM, Knapp BI, Bidlack JM, Lowey J, Bilsky EJ, Polt R.

Adv Exp Med Biol. 2009;611:495-6. No abstract available.


Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.

Pelotte AL, Smith RM, Ayestas M, Dersch CM, Bilsky EJ, Rothman RB, Deveau AM.

Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. doi: 10.1016/j.bmcl.2009.03.095. Epub 2009 Mar 26.


Behavioral pharmacology of the mu/delta opioid glycopeptide MMP2200 in rhesus monkeys.

Do Carmo GP, Polt R, Bilsky EJ, Rice KC, Negus SS.

J Pharmacol Exp Ther. 2008 Sep;326(3):939-48. doi: 10.1124/jpet.108.138180. Epub 2008 May 29.


Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a micro-agonist delta-antagonist and delta-inverse agonists.

Cheng K, Kim IJ, Lee MJ, Adah SA, Raymond TJ, Bilsky EJ, Aceto MD, May EL, Harris LS, Coop A, Dersch CM, Rothman RB, Jacobson AE, Rice KC.

Org Biomol Chem. 2007 Apr 21;5(8):1177-1190. doi: 10.1039/b618875c. Epub 2007 Mar 1.


Glycosylation improves the central effects of DAMGO.

Lowery JJ, Yeomans L, Keyari CM, Davis P, Porreca F, Knapp BI, Bidlack JM, Bilsky EJ, Polt R.

Chem Biol Drug Des. 2007 Jan;69(1):41-7.


Preclinical assessment of candidate analgesic drugs: recent advances and future challenges.

Negus SS, Vanderah TW, Brandt MR, Bilsky EJ, Becerra L, Borsook D.

J Pharmacol Exp Ther. 2006 Nov;319(2):507-14. Epub 2006 Jun 2. Review.


Spinal L-type calcium channel blockade abolishes opioid-induced sensory hypersensitivity and antinociceptive tolerance.

Dogrul A, Bilsky EJ, Ossipov MH, Lai J, Porreca F.

Anesth Analg. 2005 Dec;101(6):1730-5.


Chronic morphine up-regulates G alpha12 and cytoskeletal proteins in Chinese hamster ovary cells expressing the cloned mu opioid receptor.

Xu H, Wang X, Zimmerman D, Boja ES, Wang J, Bilsky EJ, Rothman RB.

J Pharmacol Exp Ther. 2005 Oct;315(1):248-55. Epub 2005 Jun 29.


Glycopeptides related to beta-endorphin adopt helical amphipathic conformations in the presence of lipid bilayers.

Dhanasekaran M, Palian MM, Alves I, Yeomans L, Keyari CM, Davis P, Bilsky EJ, Egleton RD, Yamamura HI, Jacobsen NE, Tollin G, Hruby VJ, Porreca F, Polt R.

J Am Chem Soc. 2005 Apr 20;127(15):5435-48.


In vivo characterization of 6beta-naltrexol, an opioid ligand with less inverse agonist activity compared with naltrexone and naloxone in opioid-dependent mice.

Raehal KM, Lowery JJ, Bhamidipati CM, Paolino RM, Blair JR, Wang D, Sadée W, Bilsky EJ.

J Pharmacol Exp Ther. 2005 Jun;313(3):1150-62. Epub 2005 Feb 16.


Basal opioid receptor activity, neutral antagonists, and therapeutic opportunities.

Sadée W, Wang D, Bilsky EJ.

Life Sci. 2005 Feb 11;76(13):1427-37. Epub 2004 Dec 8. Review.


Antinociceptive structure-activity studies with enkephalin-based opioid glycopeptides.

Elmagbari NO, Egleton RD, Palian MM, Lowery JJ, Schmid WR, Davis P, Navratilova E, Dhanasekaran M, Keyari CM, Yamamura HI, Porreca F, Hruby VJ, Polt R, Bilsky EJ.

J Pharmacol Exp Ther. 2004 Oct;311(1):290-7. Epub 2004 May 27.


Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].

Ananthan S, Khare NK, Saini SK, Seitz LE, Bartlett JL, Davis P, Dersch CM, Porreca F, Rothman RB, Bilsky EJ.

J Med Chem. 2004 Mar 11;47(6):1400-12. Erratum in: J Med Chem. 2004 May 6;47(10):2716.


Basal signaling activity of mu opioid receptor in mouse brain: role in narcotic dependence.

Wang D, Raehal KM, Lin ET, Lowery JJ, Kieffer BL, Bilsky EJ, Sadée W.

J Pharmacol Exp Ther. 2004 Feb;308(2):512-20. Epub 2003 Nov 4.


Differential effects of MK-801 on cerebrocortical neuronal injury in C57BL/6J, NSA, and ICR mice.

Brosnan-Watters G, Ogimi T, Ford D, Tatekawa L, Gilliam D, Bilsky EJ, Nash D.

Prog Neuropsychopharmacol Biol Psychiatry. 2000 Aug;24(6):925-38.


Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.

Bilsky EJ, Egleton RD, Mitchell SA, Palian MM, Davis P, Huber JD, Jones H, Yamamura HI, Janders J, Davis TP, Porreca F, Hruby VJ, Polt R.

J Med Chem. 2000 Jun 29;43(13):2586-90.


Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.

Ananthan S, Kezar HS 3rd, Carter RL, Saini SK, Rice KC, Wells JL, Davis P, Xu H, Dersch CM, Bilsky EJ, Porreca F, Rothman RB.

J Med Chem. 1999 Sep 9;42(18):3527-38.


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