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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.


Effects of the novel, selective and low-efficacy mu opioid receptor ligand NAQ on intracranial self-stimulation in rats.

Altarifi AA, Yuan Y, Zhang Y, Selley DE, Negus SS.

Psychopharmacology (Berl). 2015 Feb;232(4):815-24. doi: 10.1007/s00213-014-3719-7. Epub 2014 Sep 3.


Identification of selective agonists and positive allosteric modulators for µ- and δ-opioid receptors from a single high-throughput screen.

Burford NT, Wehrman T, Bassoni D, O'Connell J, Banks M, Zhang L, Alt A.

J Biomol Screen. 2014 Oct;19(9):1255-65. doi: 10.1177/1087057114542975. Epub 2014 Jul 21.


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.


Characterization of BU09059: a novel potent selective κ-receptor antagonist.

Casal-Dominguez JJ, Furkert D, Ostovar M, Teintang L, Clark MJ, Traynor JR, Husbands SM, Bailey SJ.

ACS Chem Neurosci. 2014 Mar 19;5(3):177-84. doi: 10.1021/cn4001507. Epub 2014 Jan 28.


Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.

Bender AM, Clark MJ, Agius MP, Traynor JR, Mosberg HI.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):548-51. doi: 10.1016/j.bmcl.2013.12.021. Epub 2013 Dec 11.


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.


Synthesis, modeling, and pharmacological evaluation of UMB 425, a mixed μ agonist/δ antagonist opioid analgesic with reduced tolerance liabilities.

Healy JR, Bezawada P, Shim J, Jones JW, Kane MA, MacKerell AD Jr, Coop A, Matsumoto RR.

ACS Chem Neurosci. 2013 Sep 18;4(9):1256-66. doi: 10.1021/cn4000428. Epub 2013 Jun 11.


Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.

Iyer MR, Rothman RB, Dersch CM, Jacobson AE, Rice KC.

Bioorg Med Chem. 2013 Jun 1;21(11):3298-309. doi: 10.1016/j.bmc.2013.02.060. Epub 2013 Apr 3.


The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist.

Tsuruda PR, Vickery RG, Long DD, Armstrong SR, Beattie DT.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91. doi: 10.1007/s00210-013-0850-7. Epub 2013 Apr 4.


The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.

Nemoto T, Yamamoto N, Wada N, Harada Y, Tomatsu M, Ishihara M, Hirayama S, Iwai T, Fujii H, Nagase H.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):268-72. doi: 10.1016/j.bmcl.2012.10.100. Epub 2012 Oct 30.


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.


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.


The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.

Mollica A, Pinnen F, Stefanucci A, Feliciani F, Campestre C, Mannina L, Sobolev AP, Lucente G, Davis P, Lai J, Ma SW, Porreca F, Hruby VJ.

J Med Chem. 2012 Apr 12;55(7):3027-35. doi: 10.1021/jm201402v. Epub 2012 Mar 22.


Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity.

Iyer MR, Lee YS, Deschamps JR, Dersch CM, Rothman RB, Jacobson AE, Rice KC.

Eur J Med Chem. 2012 Apr;50:44-54. doi: 10.1016/j.ejmech.2012.01.025. Epub 2012 Jan 20.


Pharmacological characterization of the bifunctional opioid ligand H-Dmt-Tic-Gly-NH-Bzl (UFP-505).

Dietis N, McDonald J, Molinari S, Calo G, Guerrini R, Rowbotham DJ, Lambert DG.

Br J Anaesth. 2012 Feb;108(2):262-70. doi: 10.1093/bja/aer377. Epub 2011 Dec 22.


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.


Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.

Yuan Y, Elbegdorj O, Chen J, Akubathini SK, Beletskaya IO, Selley DE, Zhang Y.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5625-9. doi: 10.1016/j.bmcl.2011.06.135. Epub 2011 Jul 18.


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.


Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.

Cheng K, Lee YS, Rothman RB, Dersch CM, Bittman RW, Jacobson AE, Rice KC.

J Med Chem. 2011 Feb 24;54(4):957-69. doi: 10.1021/jm1011676. Epub 2011 Jan 19.

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