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Items: 39


Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.

Kamakolanu UG, Meyer ME, Yasuda D, Polgar WE, Marti M, Mercatelli D, Pisanò CA, Brugnoli A, Morari M, Zaveri NT.

J Med Chem. 2020 Feb 3. doi: 10.1021/acs.jmedchem.9b02134. [Epub ahead of print]


Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile.

Kumar V, Polgar WE, Cami-Kobeci G, Thomas MP, Khroyan TV, Toll L, Husbands SM.

Front Psychiatry. 2018 Sep 19;9:430. doi: 10.3389/fpsyt.2018.00430. eCollection 2018.


A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates.

Ding H, Kiguchi N, Yasuda D, Daga PR, Polgar WE, Lu JJ, Czoty PW, Kishioka S, Zaveri NT, Ko MC.

Sci Transl Med. 2018 Aug 29;10(456). pii: eaar3483. doi: 10.1126/scitranslmed.aar3483.


Anti-Parkinsonian and anti-dyskinetic profiles of two novel potent and selective nociceptin/orphanin FQ receptor agonists.

Arcuri L, Novello S, Frassineti M, Mercatelli D, Pisanò CA, Morella I, Fasano S, Journigan BV, Meyer ME, Polgar WE, Brambilla R, Zaveri NT, Morari M.

Br J Pharmacol. 2018 Mar;175(5):782-796. doi: 10.1111/bph.14123. Epub 2018 Jan 31.


Probing ligand recognition of the opioid pan antagonist AT-076 at nociceptin, kappa, mu, and delta opioid receptors through structure-activity relationships.

Journigan VB, Polgar WE, Tuan EW, Lu J, Daga PR, Zaveri NT.

Sci Rep. 2017 Oct 16;7(1):13255. doi: 10.1038/s41598-017-13129-1.


In Vitro and In Vivo Profile of PPL-101 and PPL-103: Mixed Opioid Partial Agonist Analgesics with Low Abuse Potential.

Khroyan TV, Cippitelli A, Toll N, Lawson JA, Crossman W, Polgar WE, Toll L.

Front Psychiatry. 2017 Apr 12;8:52. doi: 10.3389/fpsyt.2017.00052. eCollection 2017.


In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations.

Ferrari F, Cerlesi MC, Malfacini D, Asth L, Gavioli EC, Journigan BV, Kamakolanu UG, Meyer ME, Yasuda D, Polgar WE, Rizzi A, Guerrini R, Ruzza C, Zaveri NT, Calo G.

Eur J Pharmacol. 2016 Dec 15;793:1-13. doi: 10.1016/j.ejphar.2016.10.025. Epub 2016 Oct 22.


High affinity α3β4 nicotinic acetylcholine receptor ligands AT-1001 and AT-1012 attenuate cocaine-induced conditioned place preference and behavioral sensitization in mice.

Khroyan TV, Yasuda D, Toll L, Polgar WE, Zaveri NT.

Biochem Pharmacol. 2015 Oct 15;97(4):531-541. doi: 10.1016/j.bcp.2015.08.083. Epub 2015 Aug 7.


Discovery of the first small-molecule opioid pan antagonist with nanomolar affinity at mu, delta, kappa, and nociceptin opioid receptors.

Zaveri NT, Journigan VB, Polgar WE.

ACS Chem Neurosci. 2015 Apr 15;6(4):646-57. doi: 10.1021/cn500367b. Epub 2015 Feb 18.


Structure-based virtual screening of the nociceptin receptor: hybrid docking and shape-based approaches for improved hit identification.

Daga PR, Polgar WE, Zaveri NT.

J Chem Inf Model. 2014 Oct 27;54(10):2732-43. doi: 10.1021/ci500291a. Epub 2014 Sep 17.


BU08073 a buprenorphine analogue with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice.

Khroyan TV, Wu J, Polgar WE, Cami-Kobeci G, Fotaki N, Husbands SM, Toll L.

Br J Pharmacol. 2015 Jan;172(2):668-80. doi: 10.1111/bph.12796. Epub 2014 Nov 5.


Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.

Journigan VB, Polgar WE, Khroyan TV, Zaveri NT.

Bioorg Med Chem. 2014 Apr 15;22(8):2508-16. doi: 10.1016/j.bmc.2014.02.047. Epub 2014 Mar 5.


[¹²⁵I]AT-1012, a new high affinity radioligand for the α3β4 nicotinic acetylcholine receptors.

Wu J, Perry DC, Bupp JE, Jiang F, Polgar WE, Toll L, Zaveri NT.

Neuropharmacology. 2014 Feb;77:193-9. doi: 10.1016/j.neuropharm.2013.09.023. Epub 2013 Oct 3.


Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.

Zaveri NT, Jiang F, Olsen C, Polgar WE, Toll L.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3308-13. doi: 10.1016/j.bmcl.2013.03.101. Epub 2013 Apr 4.


AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats.

Toll L, Zaveri NT, Polgar WE, Jiang F, Khroyan TV, Zhou W, Xie XS, Stauber GB, Costello MR, Leslie FM.

Neuropsychopharmacology. 2012 May;37(6):1367-76. doi: 10.1038/npp.2011.322. Epub 2012 Jan 25.


Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.

Cami-Kobeci G, Polgar WE, Khroyan TV, Toll L, Husbands SM.

J Med Chem. 2011 Oct 13;54(19):6531-7. doi: 10.1021/jm2003238. Epub 2011 Sep 7.


Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice.

Khroyan TV, Polgar WE, Orduna J, Montenegro J, Jiang F, Zaveri NT, Toll L.

J Pharmacol Exp Ther. 2011 Nov;339(2):687-93. doi: 10.1124/jpet.111.184663. Epub 2011 Aug 22.


Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications.

Toll L, Khroyan TV, Polgar WE, Jiang F, Olsen C, Zaveri NT.

J Pharmacol Exp Ther. 2009 Dec;331(3):954-64. doi: 10.1124/jpet.109.157446. Epub 2009 Sep 22.


Nociceptin/orphanin FQ receptor activation attenuates antinociception induced by mixed nociceptin/orphanin FQ/mu-opioid receptor agonists.

Khroyan TV, Polgar WE, Jiang F, Zaveri NT, Toll L.

J Pharmacol Exp Ther. 2009 Dec;331(3):946-53. doi: 10.1124/jpet.109.156711. Epub 2009 Aug 27.


Activity of new NOP receptor ligands in a rat peripheral mononeuropathy model: potentiation of morphine anti-allodynic activity by NOP receptor antagonists.

Khroyan TV, Polgar WE, Orduna J, Jiang F, Olsen C, Toll L, Zaveri NT.

Eur J Pharmacol. 2009 May 21;610(1-3):49-54. doi: 10.1016/j.ejphar.2009.03.019. Epub 2009 Mar 12.


Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.

Ghirmai S, Azar MR, Polgar WE, Berzetei-Gurske I, Cashman JR.

J Med Chem. 2008 Mar 27;51(6):1913-24. doi: 10.1021/jm701060e. Epub 2008 Feb 26.


Activities of mixed NOP and mu-opioid receptor ligands.

Spagnolo B, Calo G, Polgar WE, Jiang F, Olsen CM, Berzetei-Gurske I, Khroyan TV, Husbands SM, Lewis JW, Toll L, Zaveri NT.

Br J Pharmacol. 2008 Feb;153(3):609-19. Epub 2007 Dec 3.


Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors.

Madrid PB, Polgar WE, Toll L, Tanga MJ.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3014-7. Epub 2007 Mar 24.


Anti-nociceptive and anti-allodynic effects of a high affinity NOP hexapeptide [Ac-RY(3-Cl)YRWR-NH2] (Syn 1020) in rodents.

Khroyan TV, Polgar WE, Orduna J, Zaveri NT, Judd AK, Tuttle DJ, Sanchez A, Toll L.

Eur J Pharmacol. 2007 Mar 29;560(1):29-35. Epub 2007 Jan 17.


SR 16435 [1-(1-(bicyclo[3.3.1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice.

Khroyan TV, Zaveri NT, Polgar WE, Orduna J, Olsen C, Jiang F, Toll L.

J Pharmacol Exp Ther. 2007 Feb;320(2):934-43. Epub 2006 Nov 28.


Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.

MacDougall JM, Zhang XD, Polgar WE, Khroyan TV, Toll L, Cashman JR.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.


Design, chemical synthesis, and biological evaluation of thiosaccharide analogues of morphine- and codeine-6-glucuronide.

MacDougall JM, Zhang XD, Polgar WE, Khroyan TV, Toll L, Cashman JR.

J Med Chem. 2004 Nov 4;47(23):5809-15.


Synthesis and biological evaluation of some 6-arylamidomorphines as analogues of morphine-6-glucuronide.

Macdougall JM, Zhang XD, Polgar WE, Khroyan TV, Toll L, Cashman JR.

Bioorg Med Chem. 2004 Nov 15;12(22):5983-90.


Regulation of transcription of the human prepronociceptin gene by Sp1.

Zaveri NT, Green CJ, Polgar WE, Huynh N, Toll L.

Gene. 2002 May 15;290(1-2):45-52.


Characterization of opiates, neuroleptics, and synthetic analogs at ORL1 and opioid receptors.

Zaveri N, Polgar WE, Olsen CM, Kelson AB, Grundt P, Lewis JW, Toll L.

Eur J Pharmacol. 2001 Sep 28;428(1):29-36.


Ovarian sex steroid-dependent plasticity of nociceptin/orphanin FQ and opioid modulation of spinal dynorphin release.

Gupta DS, Kelson AB, Polgar WE, Toll L, Szücs M, Gintzler AR.

J Pharmacol Exp Ther. 2001 Sep;298(3):1213-20.


Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.

Toll L, Berzetei-Gurske IP, Polgar WE, Brandt SR, Adapa ID, Rodriguez L, Schwartz RW, Haggart D, O'Brien A, White A, Kennedy JM, Craymer K, Farrington L, Auh JS.

NIDA Res Monogr. 1998 Mar;178:440-66. No abstract available.


Characterization of the delta-opioid receptor found in SH-SY5Y neuroblastoma cells.

Toll L, Polgar WE, Auh JS.

Eur J Pharmacol. 1997 Apr 4;323(2-3):261-7.


Desensitization of melanotropin receptors in COS-7 cells.

Polgar WE, Bitler CM, Toll L.

Life Sci. 1996;58(15):1223-9.


Comparison of kappa 2-opioid receptors in guinea pig brain and guinea pig ileum membranes.

Webster JL, Polgar WE, Brandt SR, Berzetei-Gurske IP, Toll L.

Eur J Pharmacol. 1993 Feb 9;231(2):251-8.


Paralytic activity of (des-Glu1)conotoxin GI analogs in the mouse diaphragm.

Almquist RG, Kadambi SR, Yasuda DM, Weitl FL, Polgar WE, Toll LR.

Int J Pept Protein Res. 1989 Dec;34(6):455-62.


Novel mu-selective Met-enkephalinamide analogs with antagonist activity. Synthesis, receptor binding, analgesic properties and conformational studies.

Judd AK, Lawson JA, Olsen CM, Toll LR, Polgar WE, Uyeno ET, Keys CJ, Loew GH.

Int J Pept Protein Res. 1987 Sep;30(3):299-317.


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