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Items: 1 to 50 of 59

1.

Unveiling 7-Hydroxymitragynine as the Key Active Metabolite of Mitragynine and the Promise for Creating Novel Pain Relievers.

Spetea M, Schmidhammer H.

ACS Cent Sci. 2019 Jun 26;5(6):936-938. doi: 10.1021/acscentsci.9b00462. Epub 2019 May 29. No abstract available.

2.

Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.

Spetea M, Rief SB, Haddou TB, Fink M, Kristeva E, Mittendorfer H, Haas S, Hummer N, Follia V, Guerrieri E, Asim MF, Sturm S, Schmidhammer H.

J Med Chem. 2019 Jan 24;62(2):641-653. doi: 10.1021/acs.jmedchem.8b01327. Epub 2019 Jan 3.

3.

Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.

Martin C, Dumitrascuta M, Mannes M, Lantero A, Bucher D, Walker K, Van Wanseele Y, Oyen E, Hernot S, Van Eeckhaut A, Madder A, Hoogenboom R, Spetea M, Ballet S.

J Med Chem. 2018 Nov 8;61(21):9784-9789. doi: 10.1021/acs.jmedchem.8b01282. Epub 2018 Oct 26.

PMID:
30351003
4.

In vitro and in vivo Pharmacological Activities of 14-O-Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice.

Lattanzi R, Rief S, Schmidhammer H, Negri L, Spetea M.

Front Pharmacol. 2018 Aug 31;9:1002. doi: 10.3389/fphar.2018.01002. eCollection 2018.

5.

In vivo brain GPCR signaling elucidated by phosphoproteomics.

Liu JJ, Sharma K, Zangrandi L, Chen C, Humphrey SJ, Chiu YT, Spetea M, Liu-Chen LY, Schwarzer C, Mann M.

Science. 2018 Jun 22;360(6395). pii: eaao4927. doi: 10.1126/science.aao4927.

6.

A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects.

Drieu la Rochelle A, Guillemyn K, Dumitrascuta M, Martin C, Utard V, Quillet R, Schneider S, Daubeuf F, Willemse T, Mampuys P, Maes BUW, Frossard N, Bihel F, Spetea M, Simonin F, Ballet S.

Pain. 2018 Sep;159(9):1705-1718. doi: 10.1097/j.pain.0000000000001262.

PMID:
29708942
7.

Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists.

Dumitrascuta M, Ben Haddou T, Guerrieri E, Noha SM, Schläfer L, Schmidhammer H, Spetea M.

J Med Chem. 2017 Nov 22;60(22):9407-9412. doi: 10.1021/acs.jmedchem.7b01363. Epub 2017 Nov 3.

8.

Highly Potent and Selective New Diphenethylamines Interacting with the κ-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.

Erli F, Guerrieri E, Ben Haddou T, Lantero A, Mairegger M, Schmidhammer H, Spetea M.

J Med Chem. 2017 Sep 14;60(17):7579-7590. doi: 10.1021/acs.jmedchem.7b00981. Epub 2017 Aug 30.

9.

Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice.

Spetea M, Eans SO, Ganno ML, Lantero A, Mairegger M, Toll L, Schmidhammer H, McLaughlin JP.

Br J Pharmacol. 2017 Aug;174(15):2444-2456. doi: 10.1111/bph.13854. Epub 2017 Jun 27.

10.

Bifunctional peptide-based opioid agonist/nociceptin antagonist ligand for dual treatment of nociceptive and neuropathic pain.

Lagard C, Chevillard L, Guillemyn K, Risède P, Laplanche JL, Spetea M, Ballet S, Mégarbane B.

Pain. 2017 Mar;158(3):505-515. doi: 10.1097/j.pain.0000000000000790.

11.

Molecular Docking, Molecular Dynamics, and Structure-Activity Relationship Explorations of 14-Oxygenated N-Methylmorphinan-6-ones as Potent μ-Opioid Receptor Agonists.

Noha SM, Schmidhammer H, Spetea M.

ACS Chem Neurosci. 2017 Jun 21;8(6):1327-1337. doi: 10.1021/acschemneuro.6b00460. Epub 2017 Feb 9.

12.

Structural determinants of diphenethylamines for interaction with the κ opioid receptor: Synthesis, pharmacology and molecular modeling studies.

Guerrieri E, Bermudez M, Wolber G, Berzetei-Gurske IP, Schmidhammer H, Spetea M.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4769-4774. doi: 10.1016/j.bmcl.2016.08.031. Epub 2016 Aug 12.

PMID:
27567368
13.

μ Opioid receptor: novel antagonists and structural modeling.

Kaserer T, Lantero A, Schmidhammer H, Spetea M, Schuster D.

Sci Rep. 2016 Feb 18;6:21548. doi: 10.1038/srep21548.

14.

Anti-inflammatory effect of dual nociceptin and opioid receptor agonist, BU08070, in experimental colitis in mice.

Zielińska M, Ben Haddou T, Cami-Kobeci G, Sałaga M, Jarmuż A, Padysz M, Kordek R, Spetea M, Husbands SM, Fichna J.

Eur J Pharmacol. 2015 Oct 15;765:582-90. doi: 10.1016/j.ejphar.2015.09.021. Epub 2015 Sep 25.

15.

Synthesis and pharmacological evaluation of [(3)H]HS665, a novel, highly selective radioligand for the kappa opioid receptor.

Guerrieri E, Mallareddy JR, Tóth G, Schmidhammer H, Spetea M.

ACS Chem Neurosci. 2015 Mar 18;6(3):456-63. doi: 10.1021/cn5002792. Epub 2014 Dec 24.

PMID:
25496417
16.

Exploring pharmacological activities and signaling of morphinans substituted in position 6 as potent agonists interacting with the μ opioid receptor.

Ben Haddou T, Malfacini D, Calo G, Aceto MD, Harris LS, Traynor JR, Coop A, Schmidhammer H, Spetea M.

Mol Pain. 2014 Jul 24;10:48. doi: 10.1186/1744-8069-10-48.

17.

Pharmacological investigations of N-substituent variation in morphine and oxymorphone: opioid receptor binding, signaling and antinociceptive activity.

Ben Haddou T, Béni S, Hosztafi S, Malfacini D, Calo G, Schmidhammer H, Spetea M.

PLoS One. 2014 Jun 11;9(6):e99231. doi: 10.1371/journal.pone.0099231. eCollection 2014.

18.
19.

The µ opioid receptor and ligands acting at the µ opioid receptor, as therapeutics and potential therapeutics.

Spetea M, Asim MF, Wolber G, Schmidhammer H.

Curr Pharm Des. 2013;19(42):7415-34. Review.

PMID:
23448479
20.

Functionalization of the carbonyl group in position 6 of morphinan-6-ones. Development of novel 6-amino and 6-guanidino substituted 14-alkoxymorphinans.

Schmidhammer H, Spetea M, Windisch P, Schütz J, Riba P, Al-Khrasani M, Furst S.

Curr Pharm Des. 2013;19(42):7391-9. Review.

PMID:
23448473
21.
22.

Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.

Spetea M, Berzetei-Gurske IP, Guerrieri E, Schmidhammer H.

J Med Chem. 2012 Nov 26;55(22):10302-6. doi: 10.1021/jm301258w. Epub 2012 Nov 7.

PMID:
23134120
23.

Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.

Novoa A, Van Dorpe S, Wynendaele E, Spetea M, Bracke N, Stalmans S, Betti C, Chung NN, Lemieux C, Zuegg J, Cooper MA, Tourwé D, De Spiegeleer B, Schiller PW, Ballet S.

J Med Chem. 2012 Nov 26;55(22):9549-61. doi: 10.1021/jm3008079. Epub 2012 Nov 12.

24.

Synthesis and characterization of thiazolo- and thiazinomorphinans and their intermediate products as novel opioid-active derivatives.

Sipos A, Follia V, Berényi S, Antus S, Schmidhammer H, Spetea M.

Arch Pharm (Weinheim). 2012 Nov;345(11):852-8. doi: 10.1002/ardp.201200176. Epub 2012 Aug 10.

PMID:
22886624
25.

Recent advances in the development of 14-alkoxy substituted morphinans as potent and safer opioid analgesics.

Spetea M, Schmidhammer H.

Curr Med Chem. 2012;19(15):2442-57. Review.

PMID:
22455592
26.

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist-neurokinin 1 receptor antagonist chimera.

Guillemyn K, Kleczkowska P, Novoa A, Vandormael B, Van den Eynde I, Kosson P, Asim MF, Schiller PW, Spetea M, Lipkowski AW, Tourwé D, Ballet S.

Mol Brain. 2012 Jan 30;5:4. doi: 10.1186/1756-6606-5-4.

27.

Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile.

Schmidhammer H, Spetea M.

Int J Med Chem. 2012;2012:208039. doi: 10.1155/2012/208039. Epub 2012 Jun 17. Review.

28.

Synthesis of 14-alkoxymorphinan derivatives and their pharmacological actions.

Schmidhammer H, Spetea M.

Top Curr Chem. 2011;299:63-91. Review.

PMID:
21630508
29.

Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.

Spetea M, Windisch P, Guo Y, Bileviciute-Ljungar I, Schütz J, Asim MF, Berzetei-Gurske IP, Riba P, Kiraly K, Fürst S, Al-Khrasani M, Schmidhammer H.

J Med Chem. 2011 Feb 24;54(4):980-8. doi: 10.1021/jm101211p. Epub 2011 Jan 14.

30.

In vitro and in vivo pharmacological profile of the 5-benzyl analogue of 14-methoxymetopon, a novel mu opioid analgesic with reduced propensity to alter motor function.

Spetea M, Bohotin CR, Asim MF, Stübegger K, Schmidhammer H.

Eur J Pharm Sci. 2010 Sep 11;41(1):125-35. doi: 10.1016/j.ejps.2010.05.018. Epub 2010 Jun 18.

31.

Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.

Schuster D, Spetea M, Music M, Rief S, Fink M, Kirchmair J, Schütz J, Wolber G, Langer T, Stuppner H, Schmidhammer H, Rollinger JM.

Bioorg Med Chem. 2010 Jul 15;18(14):5071-80. doi: 10.1016/j.bmc.2010.05.071. Epub 2010 Jun 2.

PMID:
20580236
32.

Novel approach to demonstrate high efficacy of mu opioids in the rat vas deferens: a simple model of predictive value.

Riba P, Friedmann T, Király KP, Al-Khrasani M, Sobor M, Asim MF, Spetea M, Schmidhammer H, Furst S.

Brain Res Bull. 2010 Jan 15;81(1):178-84. doi: 10.1016/j.brainresbull.2009.09.011.

PMID:
19800397
33.

Modulation of basal and stress-induced amygdaloid substance P release by the potent and selective NK1 receptor antagonist L-822429.

Singewald N, Chicchi GG, Thurner CC, Tsao KL, Spetea M, Schmidhammer H, Sreepathi HK, Ferraguti F, Singewald GM, Ebner K.

J Neurochem. 2008 Sep;106(6):2476-88. doi: 10.1111/j.1471-4159.2008.05596.x. Epub 2008 Jul 30.

34.

Non-peptidic delta-opioid receptor antagonists suppress mitogen-induced tryptophan degradation in peripheral blood mononuclear cells in vitro.

Jenny M, Winkler C, Spetea M, Schennach H, Schmidhammer H, Fuchs D.

Immunol Lett. 2008 Jun 15;118(1):82-7. doi: 10.1016/j.imlet.2008.03.006. Epub 2008 Apr 10.

PMID:
18440650
35.
36.

Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat.

Obara I, Makuch W, Spetea M, Schütz J, Schmidhammer H, Przewlocki R, Przewlocka B.

Eur J Pharmacol. 2007 Mar 8;558(1-3):60-7. Epub 2006 Nov 25.

PMID:
17204264
37.

Opioid peptides and receptors in joint tissues: study in the rat.

Bergström J, Ahmed M, Li J, Ahmad T, Kreicbergs A, Spetea M.

J Orthop Res. 2006 Jun;24(6):1193-9.

39.

Anti-inflammatory effects of contralateral administration of the kappa-opioid agonist U-50,488H in rats with unilaterally induced adjuvant arthritis.

Bileviciute-Ljungar I, Saxne T, Spetea M.

Rheumatology (Oxford). 2006 Mar;45(3):295-302. Epub 2005 Oct 25.

PMID:
16249243
40.

Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.

Spetea M, Greiner E, Aceto MD, Harris LS, Coop A, Schmidhammer H.

J Med Chem. 2005 Jul 28;48(15):5052-5.

PMID:
16033285
41.
42.

Peripheral versus central antinociceptive actions of 6-amino acid-substituted derivatives of 14-O-methyloxymorphone in acute and inflammatory pain in the rat.

Fürst S, Riba P, Friedmann T, Tímar J, Al-Khrasani M, Obara I, Makuch W, Spetea M, Schütz J, Przewlocki R, Przewlocka B, Schmidhammer H.

J Pharmacol Exp Ther. 2005 Feb;312(2):609-18. Epub 2004 Sep 21.

PMID:
15383636
43.
44.

Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.

Spetea M, Schüllner F, Moisa RC, Berzetei-Gurske IP, Schraml B, Dörfler C, Aceto MD, Harris LS, Coop A, Schmidhammer H.

J Med Chem. 2004 Jun 3;47(12):3242-7.

PMID:
15163203
45.

In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.

Spetea M, Friedmann T, Riba P, Schütz J, Wunder G, Langer T, Schmidhammer H, Fürst S.

Eur J Pharmacol. 2004 Jan 12;483(2-3):301-8.

PMID:
14729121
46.

Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.

Schütz J, Spetea M, Koch M, Aceto MD, Harris LS, Coop A, Schmidhammer H.

J Med Chem. 2003 Sep 11;46(19):4182-7.

PMID:
12954070
47.

Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist.

Spetea M, Tóth F, Schütz J, Otvös F, Tóth G, Benyhe S, Borsodi A, Schmidhammer H.

Eur J Neurosci. 2003 Jul;18(2):290-5.

PMID:
12887410
48.

Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.

Greiner E, Spetea M, Krassnig R, Schüllner F, Aceto M, Harris LS, Traynor JR, Woods JH, Coop A, Schmidhammer H.

J Med Chem. 2003 Apr 24;46(9):1758-63.

PMID:
12699394
49.

Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.

Schütz J, Dersch CM, Horel R, Spetea M, Koch M, Meditz R, Greiner E, Rothman RB, Schmidhammer H.

J Med Chem. 2002 Nov 21;45(24):5378-83.

PMID:
12431065
50.

Alteration in endogenous opioid systems due to chronic inflammatory pain conditions.

Spetea M, Rydelius G, Nylander I, Ahmed M, Bileviciute-Ljungar I, Lundeberg T, Svensson S, Kreicbergs A.

Eur J Pharmacol. 2002 Jan 25;435(2-3):245-52.

PMID:
11821033

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