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Items: 1 to 50 of 158

1.

In Vitro Pharmacological Characterization of Buprenorphine, Samidorphan, and Combinations Being Developed as an Adjunctive Treatment of Major Depressive Disorder.

Bidlack JM, Knapp BI, Deaver DR, Plotnikava M, Arnelle D, Wonsey AM, Fern Toh M, Pin SS, Namchuk MN.

J Pharmacol Exp Ther. 2018 Nov;367(2):267-281. doi: 10.1124/jpet.118.249839. Epub 2018 Aug 14.

PMID:
30108159
2.

Antidepressant-like effects of 3-carboxamido seco-nalmefene (3CS-nalmefene), a novel opioid receptor modulator, in a rat IFN-α-induced depression model.

Callaghan CK, Rouine J, Dean RL, Knapp BI, Bidlack JM, Deaver DR, O'Mara SM.

Brain Behav Immun. 2018 Jan;67:152-162. doi: 10.1016/j.bbi.2017.08.016. Epub 2017 Aug 24.

PMID:
28844812
3.

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.

PMID:
26125201
4.

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.

5.

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.

PMID:
24484983
6.

Preliminary pharmacological evaluation of enantiomeric morphinans.

Sromek AW, Provencher BA, Russell S, Chartoff E, Knapp BI, Bidlack JM, Neumeyer JL.

ACS Chem Neurosci. 2014 Feb 19;5(2):93-9. doi: 10.1021/cn400205z. Epub 2014 Jan 8.

7.

Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.

Provencher BA, Sromek AW, Li W, Russell S, Chartoff E, Knapp BI, Bidlack JM, Neumeyer JL.

J Med Chem. 2013 Nov 14;56(21):8872-8. doi: 10.1021/jm401290y. Epub 2013 Oct 29.

8.

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.

VanAlstine MA, Wentland MP, Alvarez J, Cao Q, Cohen DJ, Knapp BI, Bidlack JM.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2128-33. doi: 10.1016/j.bmcl.2013.01.117. Epub 2013 Feb 8.

9.

Inhibition of Gβγ-subunit signaling potentiates morphine-induced antinociception but not respiratory depression, constipation, locomotion, and reward.

Hoot MR, Sypek EI, Reilley KJ, Carey AN, Bidlack JM, McLaughlin JP.

Behav Pharmacol. 2013 Apr;24(2):144-52. doi: 10.1097/FBP.0b013e32835f3d2f.

PMID:
23412114
10.

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.

Wentland MP, Jo S, Gargano JM, VanAlstine MA, Cohen DJ, Bidlack JM.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7340-4. doi: 10.1016/j.bmcl.2012.10.081. Epub 2012 Oct 27.

11.

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. Epub 2012 Apr 4.

12.

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.

13.

Effects of oral loperamide on efficacy of naltrexone, baclofen and AM-251 in blocking ethanol self-administration in rats.

Dean RL, Eyerman D, Todtenkopf MS, Turncliff RZ, Bidlack JM, Deaver DR.

Pharmacol Biochem Behav. 2012 Jan;100(3):530-7. doi: 10.1016/j.pbb.2011.10.019. Epub 2011 Oct 25.

PMID:
22056608
14.

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.

15.

Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.

Zhang B, Zhang T, Sromek AW, Scrimale T, Bidlack JM, Neumeyer JL.

Bioorg Med Chem. 2011 May 1;19(9):2808-16. doi: 10.1016/j.bmc.2011.03.052. Epub 2011 Mar 26.

16.

Aminothiazolomorphinans with mixed κ and μ opioid activity.

Zhang T, Yan Z, Sromek A, Knapp BI, Scrimale T, Bidlack JM, Neumeyer JL.

J Med Chem. 2011 Mar 24;54(6):1903-13. doi: 10.1021/jm101542c. Epub 2011 Feb 25.

17.

Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic.

Hough LB, Nalwalk JW, Yang J, Conroy JL, VanAlstine MA, Yang W, Gargano J, Shan Z, Zhang SZ, Wentland MP, Phillips JG, Knapp BI, Bidlack JM, Zuiderveld OP, Leurs R, Ding X.

Pain. 2011 Apr;152(4):878-87. doi: 10.1016/j.pain.2011.01.001.

18.

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

Balboni G, Salvadori S, Marczak ED, Knapp BI, Bidlack JM, Lazarus LH, Peng X, Si YG, Neumeyer JL.

Eur J Med Chem. 2011 Feb;46(2):799-803. doi: 10.1016/j.ejmech.2010.12.001. Epub 2010 Dec 8.

19.

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.

20.

Evolution of the Bifunctional Lead μ Agonist / δ Antagonist Containing the Dmt-Tic Opioid Pharmacophore.

Balboni G, Salvadori S, Trapella C, Knapp BI, Bidlack JM, Lazarus LH, Peng X, Neumeyer JL.

ACS Chem Neurosci. 2010 Feb 17;1(2):155-164.

21.

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

Fulton BS, Knapp BL, Bidlack JM, Neumeyer JL.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. doi: 10.1016/j.bmcl.2010.01.101. Epub 2010 Jan 25.

22.

Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling.

Conroy JL, Fang C, Gu J, Zeitlin SO, Yang W, Yang J, VanAlstine MA, Nalwalk JW, Albrecht PJ, Mazurkiewicz JE, Snyder-Keller A, Shan Z, Zhang SZ, Wentland MP, Behr M, Knapp BI, Bidlack JM, Zuiderveld OP, Leurs R, Ding X, Hough LB.

Nat Neurosci. 2010 Mar;13(3):284-6. doi: 10.1038/nn.2497. Epub 2010 Feb 7.

23.

Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.

Decker M, Si YG, Knapp BI, Bidlack JM, Neumeyer JL.

J Med Chem. 2010 Jan 14;53(1):402-18. doi: 10.1021/jm9013482.

24.

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

Decker M, Fulton BS, Zhang B, Knapp BI, Bidlack JM, Neumeyer JL.

J Med Chem. 2009 Dec 10;52(23):7389-96. doi: 10.1021/jm900379p.

25.

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.

PMID:
19400281
26.

Syntheses of novel high affinity ligands for opioid receptors.

Wentland MP, Lou R, Lu Q, Bu Y, Denhardt C, Jin J, Ganorkar R, VanAlstine MA, Guo C, Cohen DJ, Bidlack JM.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. doi: 10.1016/j.bmcl.2009.02.078. Epub 2009 Feb 25.

27.

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.

Wentland MP, Lu Q, Ganorkar R, Zhang SZ, Jo S, Cohen DJ, Bidlack JM.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. doi: 10.1016/j.bmcl.2008.11.076. Epub 2008 Nov 24.

PMID:
19091564
28.

Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.

Wentland MP, Lou R, Lu Q, Bu Y, VanAlstine MA, Cohen DJ, Bidlack JM.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. doi: 10.1016/j.bmcl.2008.10.134. Epub 2008 Nov 7.

PMID:
19027293
29.
30.

Phenobarbital withdrawal seizures may occur over several weeks before remitting: human data and hypothetical mechanism.

Bidlack JM, Morris HH 3rd.

Seizure. 2009 Jan;18(1):79-81. doi: 10.1016/j.seizure.2008.06.014. Epub 2008 Aug 3.

31.

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

Fulton BS, Knapp BI, Bidlack JM, Neumeyer JL.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4474-6. doi: 10.1016/j.bmcl.2008.07.054. Epub 2008 Jul 17.

32.

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

Mathews JL, Fulton BS, Negus SS, Neumeyer JL, Bidlack JM.

Neurochem Res. 2008 Oct;33(10):2142-50. doi: 10.1007/s11064-008-9752-3. Epub 2008 Jun 5.

33.

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

Wentland MP, Sun X, Cohen DJ, Bidlack JM.

Bioorg Med Chem. 2008 May 15;16(10):5653-64. doi: 10.1016/j.bmc.2008.03.066. Epub 2008 Mar 30.

34.

Extracellular biotransformation of beta-endorphin in rat striatum and cerebrospinal fluid.

Reed B, Bidlack JM, Chait BT, Kreek MJ.

J Neuroendocrinol. 2008 May;20(5):606-16. doi: 10.1111/j.1365-2826.2008.01705.x. Epub 2008 Mar 15.

35.

Opioid receptors and signaling on cells from the immune system.

Bidlack JM, Khimich M, Parkhill AL, Sumagin S, Sun B, Tipton CM.

J Neuroimmune Pharmacol. 2006 Sep;1(3):260-9. Epub 2006 Jul 8. Review.

PMID:
18040803
36.
37.

Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.

Zhang A, Li F, Ding C, Yao Q, Knapp BI, Bidlack JM, Neumeyer JL.

J Med Chem. 2007 May 31;50(11):2747-51. Epub 2007 May 9.

PMID:
17488103
38.

In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.

Peng X, Knapp BI, Bidlack JM, Neumeyer JL.

Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.

39.
40.

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.

PMID:
17313456
41.

High-affinity carbamate analogues of morphinan at opioid receptors.

Peng X, Knapp BI, Bidlack JM, Neumeyer JL.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.

42.

New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.

Neumeyer JL, Peng X, Knapp BI, Bidlack JM, Lazarus LH, Salvadori S, Trapella C, Balboni G.

J Med Chem. 2006 Sep 7;49(18):5640-3.

43.
44.

Reduction of lipopolysaccharide-induced interleukin-6 production by the kappa opioid U50,488 in a mouse monocyte-like cell line.

Parkhill AL, Bidlack JM.

Int Immunopharmacol. 2006 Jun;6(6):1013-9. Epub 2006 Feb 17.

PMID:
16644488
45.

Differential targeting of Gbetagamma-subunit signaling with small molecules.

Bonacci TM, Mathews JL, Yuan C, Lehmann DM, Malik S, Wu D, Font JL, Bidlack JM, Smrcka AV.

Science. 2006 Apr 21;312(5772):443-6.

46.

The expression of prodynorphin gene is down-regulated by activation with lipopolysaccharide in U-937 macrophage cells.

Sun B, Tipton CM, Bidlack JM.

J Neuroimmunol. 2006 May;174(1-2):52-62. Epub 2006 Feb 17.

PMID:
16483672
47.
48.
49.

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. Epub 2005 Aug 2.

PMID:
16076937
50.

Nalmefene induced elevation in serum prolactin in normal human volunteers: partial kappa opioid agonist activity?

Bart G, Schluger JH, Borg L, Ho A, Bidlack JM, Kreek MJ.

Neuropsychopharmacology. 2005 Dec;30(12):2254-62.

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