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Items: 1 to 50 of 343

1.

MP1104, a mixed kappa-delta opioid receptor agonist has anti-cocaine properties with reduced side-effects in rats.

Atigari DV, Uprety R, Pasternak GW, Majumdar S, Kivell BM.

Neuropharmacology. 2019 Feb 13. pii: S0028-3908(18)30757-3. doi: 10.1016/j.neuropharm.2019.02.010. [Epub ahead of print]

PMID:
30768946
2.

Kinetic and thermodynamic insights into sodium ion translocation through the μ-opioid receptor from molecular dynamics and machine learning analysis.

Hu X, Wang Y, Hunkele A, Provasi D, Pasternak GW, Filizola M.

PLoS Comput Biol. 2019 Jan 24;15(1):e1006689. doi: 10.1371/journal.pcbi.1006689. eCollection 2019 Jan.

3.

Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (σ1) receptor selective ligands.

Uprety R, Váradi A, Allaoa A, Redel-Traub GN, Palmer TC, Feinberg EN, Ferris AC, Pande VS, Pasternak GW, Majumdar S.

Eur J Med Chem. 2019 Feb 15;164:241-251. doi: 10.1016/j.ejmech.2018.12.048. Epub 2018 Dec 22.

PMID:
30597325
4.

σ1 Receptor ligand binding: an open-and-shut case.

Kim FJ, Pasternak GW.

Nat Struct Mol Biol. 2018 Nov;25(11):992-993. doi: 10.1038/s41594-018-0146-1. No abstract available.

PMID:
30310147
5.

Pharmacological Characterization of Levorphanol, a G-Protein Biased Opioid Analgesic.

Le Rouzic V, Narayan A, Hunkle A, Marrone GF, Lu Z, Majumdar S, Xu J, Pan YX, Pasternak GW.

Anesth Analg. 2019 Feb;128(2):365-373. doi: 10.1213/ANE.0000000000003360.

PMID:
29649035
6.

Mu Opioid Pharmacology: 40 Years to the Promised Land.

Pasternak GW.

Adv Pharmacol. 2018;82:261-291. doi: 10.1016/bs.apha.2017.09.006. Epub 2017 Nov 15.

PMID:
29413524
7.

Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor.

Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL.

Cell. 2018 Jan 11;172(1-2):55-67.e15. doi: 10.1016/j.cell.2017.12.011. Epub 2018 Jan 4.

8.

Fentanyl-related designer drugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo.

Huang XP, Che T, Mangano TJ, Le Rouzic V, Pan YX, Majumdar S, Cameron MD, Baumann MH, Pasternak GW, Roth BL.

JCI Insight. 2017 Nov 16;2(22). pii: 97222. doi: 10.1172/jci.insight.97222. [Epub ahead of print]

9.

Novel Synthetic Opioids and Overdose Deaths: Tip of the Iceberg?

Baumann MH, Pasternak GW.

Neuropsychopharmacology. 2018 Jan;43(1):216-217. doi: 10.1038/npp.2017.211. No abstract available.

10.

Truncated μ-Opioid Receptors With 6 Transmembrane Domains Are Essential for Opioid Analgesia.

Lu Z, Xu J, Xu M, Rossi GC, Majumdar S, Pasternak GW, Pan YX.

Anesth Analg. 2018 Mar;126(3):1050-1057. doi: 10.1213/ANE.0000000000002538.

PMID:
28991118
11.

Pharmacological characterization of novel synthetic opioids (NSO) found in the recreational drug marketplace.

Baumann MH, Majumdar S, Le Rouzic V, Hunkele A, Uprety R, Huang XP, Xu J, Roth BL, Pan YX, Pasternak GW.

Neuropharmacology. 2018 May 15;134(Pt A):101-107. doi: 10.1016/j.neuropharm.2017.08.016. Epub 2017 Aug 12.

PMID:
28807672
12.

Allosteric Modulation of Opioid G-Protein Coupled Receptors by Sigma1 Receptors.

Pasternak GW.

Handb Exp Pharmacol. 2017;244:163-175. doi: 10.1007/164_2017_34. Review.

PMID:
28667477
13.

Cloning the sigma2 receptor: Wandering 40 years to find an identity.

Kim FJ, Pasternak GW.

Proc Natl Acad Sci U S A. 2017 Jul 3;114(27):6888-6890. doi: 10.1073/pnas.1708155114. Epub 2017 Jun 23. No abstract available.

14.

Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.

Urai Á, Váradi A, Szőcs L, Komjáti B, Le Rouzic V, Hunkele A, Pasternak GW, Majumdar S, Hosztafi S.

Medchemcomm. 2017 Jan 1;8(1):152-157. doi: 10.1039/C6MD00450D. Epub 2016 Oct 18.

15.

Isolation and characterization of alternatively spliced variants of the mouse sigma1 receptor gene, Sigmar1.

Pan L, Pasternak DA, Xu J, Xu M, Lu Z, Pasternak GW, Pan YX.

PLoS One. 2017 Mar 28;12(3):e0174694. doi: 10.1371/journal.pone.0174694. eCollection 2017.

16.

Genetic dissociation of morphine analgesia from hyperalgesia in mice.

Marrone GF, Le Rouzic V, Varadi A, Xu J, Rajadhyaksha AM, Majumdar S, Pan YX, Pasternak GW.

Psychopharmacology (Berl). 2017 Jun;234(12):1891-1900. doi: 10.1007/s00213-017-4600-2. Epub 2017 Mar 25.

17.

Alternatively spliced mu opioid receptor C termini impact the diverse actions of morphine.

Xu J, Lu Z, Narayan A, Le Rouzic VP, Xu M, Hunkele A, Brown TG, Hoefer WF, Rossi GC, Rice RC, Martínez-Rivera A, Rajadhyaksha AM, Cartegni L, Bassoni DL, Pasternak GW, Pan YX.

J Clin Invest. 2017 Apr 3;127(4):1561-1573. doi: 10.1172/JCI88760. Epub 2017 Mar 20.

18.

Tetrapeptide Endomorphin Analogs Require Both Full Length and Truncated Splice Variants of the Mu Opioid Receptor Gene Oprm1 for Analgesia.

Marrone GF, Lu Z, Rossi G, Narayan A, Hunkele A, Marx S, Xu J, Pintar J, Majumdar S, Pan YX, Pasternak GW.

ACS Chem Neurosci. 2016 Dec 21;7(12):1717-1727. doi: 10.1021/acschemneuro.6b00240. Epub 2016 Oct 10.

19.

Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.

Váradi A, Marrone GF, Palmer TC, Narayan A, Szabó MR, Le Rouzic V, Grinnell SG, Subrath JJ, Warner E, Kalra S, Hunkele A, Pagirsky J, Eans SO, Medina JM, Xu J, Pan YX, Borics A, Pasternak GW, McLaughlin JP, Majumdar S.

J Med Chem. 2016 Sep 22;59(18):8381-97. doi: 10.1021/acs.jmedchem.6b00748. Epub 2016 Sep 2.

20.

Mediation of buprenorphine analgesia by a combination of traditional and truncated mu opioid receptor splice variants.

Grinnell SG, Ansonoff M, Marrone GF, Lu Z, Narayan A, Xu J, Rossi G, Majumdar S, Pan YX, Bassoni DL, Pintar J, Pasternak GW.

Synapse. 2016 Oct;70(10):395-407. doi: 10.1002/syn.21914. Epub 2016 Jul 12.

21.

Truncated mu opioid GPCR variant involvement in opioid-dependent and opioid-independent pain modulatory systems within the CNS.

Marrone GF, Grinnell SG, Lu Z, Rossi GC, Le Rouzic V, Xu J, Majumdar S, Pan YX, Pasternak GW.

Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):3663-8. doi: 10.1073/pnas.1523894113. Epub 2016 Mar 14.

22.

Synthesis and characterization of a dual kappa-delta opioid receptor agonist analgesic blocking cocaine reward behavior.

Váradi A, Marrone GF, Eans SO, Ganno ML, Subrath JJ, Le Rouzic V, Hunkele A, Pasternak GW, McLaughlin JP, Majumdar S.

ACS Chem Neurosci. 2015 Nov 18;6(11):1813-24. doi: 10.1021/acschemneuro.5b00153. Epub 2015 Sep 14.

23.

Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target.

Marrone GF, Majumdar S, Pasternak GW.

Methods Mol Biol. 2015;1335:241-9. doi: 10.1007/978-1-4939-2914-6_16.

PMID:
26260605
24.

Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction.

Váradi A, Palmer TC, Haselton N, Afonin D, Subrath JJ, Le Rouzic V, Hunkele A, Pasternak GW, Marrone GF, Borics A, Majumdar S.

ACS Chem Neurosci. 2015 Sep 16;6(9):1570-7. doi: 10.1021/acschemneuro.5b00137. Epub 2015 Jul 21.

25.

Mediation of opioid analgesia by a truncated 6-transmembrane GPCR.

Lu Z, Xu J, Rossi GC, Majumdar S, Pasternak GW, Pan YX.

J Clin Invest. 2015 Jul 1;125(7):2626-30. doi: 10.1172/JCI81070. Epub 2015 May 26.

26.

Synthesis and pharmacology of halogenated δ-opioid-selective [d-Ala(2)]deltorphin II peptide analogues.

Pescatore R, Marrone GF, Sedberry S, Vinton D, Finkelstein N, Katlowitz YE, Pasternak GW, Wilson KR, Majumdar S.

ACS Chem Neurosci. 2015 Jun 17;6(6):905-10. doi: 10.1021/acschemneuro.5b00060. Epub 2015 Apr 14.

27.

Mild, Pd-catalyzed stannylation of radioiodination targets.

Pickett JE, Váradi A, Palmer TC, Grinnell SG, Schrock JM, Pasternak GW, Karimov RR, Majumdar S.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1761-1764. doi: 10.1016/j.bmcl.2015.02.055. Epub 2015 Mar 2.

28.

Stabilization of morphine tolerance with long-term dosing: association with selective upregulation of mu-opioid receptor splice variant mRNAs.

Xu J, Faskowitz AJ, Rossi GC, Xu M, Lu Z, Pan YX, Pasternak GW.

Proc Natl Acad Sci U S A. 2015 Jan 6;112(1):279-84. doi: 10.1073/pnas.1419183112. Epub 2014 Dec 22.

29.

Differential expressions of the alternatively spliced variant mRNAs of the µ opioid receptor gene, OPRM1, in brain regions of four inbred mouse strains.

Xu J, Lu Z, Xu M, Rossi GC, Kest B, Waxman AR, Pasternak GW, Pan YX.

PLoS One. 2014 Oct 24;9(10):e111267. doi: 10.1371/journal.pone.0111267. eCollection 2014.

30.

A heroin addiction severity-associated intronic single nucleotide polymorphism modulates alternative pre-mRNA splicing of the μ opioid receptor gene OPRM1 via hnRNPH interactions.

Xu J, Lu Z, Xu M, Pan L, Deng Y, Xie X, Liu H, Ding S, Hurd YL, Pasternak GW, Klein RJ, Cartegni L, Zhou W, Pan YX.

J Neurosci. 2014 Aug 13;34(33):11048-66. doi: 10.1523/JNEUROSCI.3986-13.2014.

31.

Broad-spectrum analgesic efficacy of IBNtxA is mediated by exon 11-associated splice variants of the mu-opioid receptor gene.

Wieskopf JS, Pan YX, Marcovitz J, Tuttle AH, Majumdar S, Pidakala J, Pasternak GW, Mogil JS.

Pain. 2014 Oct;155(10):2063-70. doi: 10.1016/j.pain.2014.07.014. Epub 2014 Aug 2.

32.

Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions.

Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M.

Biochemistry. 2014 Aug 12;53(31):5140-9. doi: 10.1021/bi5006915. Epub 2014 Jul 29.

33.

Pharmacologic characterization in the rat of a potent analgesic lacking respiratory depression, IBNtxA.

Grinnell SG, Majumdar S, Narayan A, Le Rouzic V, Ansonoff M, Pintar JE, Pasternak GW.

J Pharmacol Exp Ther. 2014 Sep;350(3):710-8. doi: 10.1124/jpet.114.213199. Epub 2014 Jun 26.

34.

Opiate pharmacology and relief of pain.

Pasternak GW.

J Clin Oncol. 2014 Jun 1;32(16):1655-61. doi: 10.1200/JCO.2013.53.1079. Epub 2014 May 5. Review.

35.

Three-component coupling approach for the synthesis of diverse heterocycles utilizing reactive nitrilium trapping.

Váradi A, Palmer TC, Notis PR, Redel-Traub GN, Afonin D, Subrath JJ, Pasternak GW, Hu C, Sharma I, Majumdar S.

Org Lett. 2014 Mar 21;16(6):1668-71. doi: 10.1021/ol500328t. Epub 2014 Feb 28.

36.

Isolating and characterizing three alternatively spliced mu opioid receptor variants: mMOR-1A, mMOR-1O, and mMOR-1P.

Xu J, Xu M, Bolan E, Gilbert AK, Pasternak GW, Pan YX.

Synapse. 2014 Apr;68(4):144-52. doi: 10.1002/syn.21727. Epub 2014 Jan 16.

37.

Morphine regulates expression of μ-opioid receptor MOR-1A, an intron-retention carboxyl terminal splice variant of the μ-opioid receptor (OPRM1) gene via miR-103/miR-107.

Lu Z, Xu J, Xu M, Pasternak GW, Pan YX.

Mol Pharmacol. 2014 Feb;85(2):368-80. doi: 10.1124/mol.113.089292. Epub 2013 Dec 3.

38.

Novel 6β-acylaminomorphinans with analgesic activity.

Váradi A, Hosztafi S, Le Rouzic V, Tóth G, Urai Á, Noszál B, Pasternak GW, Grinnell SG, Majumdar S.

Eur J Med Chem. 2013 Nov;69:786-9. doi: 10.1016/j.ejmech.2013.09.031. Epub 2013 Sep 22.

39.

Mu opioids and their receptors: evolution of a concept.

Pasternak GW, Pan YX.

Pharmacol Rev. 2013 Sep 27;65(4):1257-317. doi: 10.1124/pr.112.007138. Print 2013. Review.

40.

Sequential cytoprotective responses to Sigma1 ligand-induced endoplasmic reticulum stress.

Schrock JM, Spino CM, Longen CG, Stabler SM, Marino JC, Pasternak GW, Kim FJ.

Mol Pharmacol. 2013 Nov;84(5):751-62. doi: 10.1124/mol.113.087809. Epub 2013 Sep 4.

41.

Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin.

Pickett JE, Nagakura K, Pasternak AR, Grinnell SG, Majumdar S, Lewis JS, Pasternak GW.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4347-50. doi: 10.1016/j.bmcl.2013.05.090. Epub 2013 Jun 6.

42.

Stabilization of the μ-opioid receptor by truncated single transmembrane splice variants through a chaperone-like action.

Xu J, Xu M, Brown T, Rossi GC, Hurd YL, Inturrisi CE, Pasternak GW, Pan YX.

J Biol Chem. 2013 Jul 19;288(29):21211-27. doi: 10.1074/jbc.M113.458687. Epub 2013 Jun 11.

43.

Opioids and their receptors: Are we there yet?

Pasternak GW.

Neuropharmacology. 2014 Jan;76 Pt B:198-203. doi: 10.1016/j.neuropharm.2013.03.039. Epub 2013 Apr 26. Review.

44.

The role of multidrug resistance-associated protein in the blood-brain barrier and opioid analgesia.

Su W, Pasternak GW.

Synapse. 2013 Sep;67(9):609-19. doi: 10.1002/syn.21667. Epub 2013 May 2.

45.

Methadone-induced hypoglycemia.

Faskowitz AJ, Kramskiy VN, Pasternak GW.

Cell Mol Neurobiol. 2013 May;33(4):537-42. doi: 10.1007/s10571-013-9919-6. Epub 2013 Mar 7.

46.

Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression.

Kim FJ, Schrock JM, Spino CM, Marino JC, Pasternak GW.

Biochem Biophys Res Commun. 2012 Sep 21;426(2):177-82. doi: 10.1016/j.bbrc.2012.08.052. Epub 2012 Aug 17.

47.

Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants.

Majumdar S, Subrath J, Le Rouzic V, Polikar L, Burgman M, Nagakura K, Ocampo J, Haselton N, Pasternak AR, Grinnell S, Pan YX, Pasternak GW.

J Med Chem. 2012 Jul 26;55(14):6352-62. doi: 10.1021/jm300305c. Epub 2012 Jul 16.

48.

Preclinical pharmacology and opioid combinations.

Pasternak GW.

Pain Med. 2012 Mar;13 Suppl 1:S4-11. doi: 10.1111/j.1526-4637.2012.01335.x. Review.

49.

Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects.

Majumdar S, Grinnell S, Le Rouzic V, Burgman M, Polikar L, Ansonoff M, Pintar J, Pan YX, Pasternak GW.

Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19778-83. doi: 10.1073/pnas.1115231108. Epub 2011 Nov 21.

50.

Generation of novel radiolabeled opiates through site-selective iodination.

Majumdar S, Burgman M, Haselton N, Grinnell S, Ocampo J, Pasternak AR, Pasternak GW.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4001-4. doi: 10.1016/j.bmcl.2011.05.008. Epub 2011 May 8.

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