Format
Sort by
Items per page

Send to

Choose Destination

Links from PubMed

Items: 1 to 20 of 82

1.

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J.

ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. Epub 2012 Jan 20.

2.

Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor.

Zheng Z, Huang XP, Mangano TJ, Zou R, Chen X, Zaidi SA, Roth BL, Stevens RC, Katritch V.

J Med Chem. 2017 Apr 13;60(7):3070-3081. doi: 10.1021/acs.jmedchem.7b00109. Epub 2017 Apr 3.

3.
4.

Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting.

Zhou L, Stahl EL, Lovell KM, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:131-41. doi: 10.1016/j.neuropharm.2015.07.001. Epub 2015 Jul 6.

5.

Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.

Ananthan S, Johnson CA, Carter RL, Clayton SD, Rice KC, Xu H, Davis P, Porreca F, Rothman RB.

J Med Chem. 1998 Jul 16;41(15):2872-81.

PMID:
9667975
6.

6'-Guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.

Rives ML, Rossillo M, Liu-Chen LY, Javitch JA.

J Biol Chem. 2012 Aug 3;287(32):27050-4. doi: 10.1074/jbc.C112.387332. Epub 2012 Jun 26.

7.

Pharmacological characterization of 2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a high-affinity antagonist selective for κ-opioid receptors.

Grimwood S, Lu Y, Schmidt AW, Vanase-Frawley MA, Sawant-Basak A, Miller E, McLean S, Freeman J, Wong S, McLaughlin JP, Verhoest PR.

J Pharmacol Exp Ther. 2011 Nov;339(2):555-66. doi: 10.1124/jpet.111.185108. Epub 2011 Aug 5.

8.

N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy.

Béguin C, Potter DN, Dinieri JA, Munro TA, Richards MR, Paine TA, Berry L, Zhao Z, Roth BL, Xu W, Liu-Chen LY, Carlezon WA Jr, Cohen BM.

J Pharmacol Exp Ther. 2008 Jan;324(1):188-95. Epub 2007 Oct 19.

9.

Bioactivity of new mu and delta opioid peptides.

Capasso A.

Med Chem. 2007 Sep;3(5):480-7.

PMID:
17897075
10.

Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.

Schmitt S, Colloc'h N, Perrio C.

Eur J Med Chem. 2015 Jan 27;90:742-50. doi: 10.1016/j.ejmech.2014.12.016. Epub 2014 Dec 11.

PMID:
25513968
11.

Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.

Polepally PR, Huben K, Vardy E, Setola V, Mosier PD, Roth BL, Zjawiony JK.

Eur J Med Chem. 2014 Oct 6;85:818-29. doi: 10.1016/j.ejmech.2014.07.077. Epub 2014 Aug 23.

12.

N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing κ-Opioid Receptor Ligands.

Frankowski KJ, Ghosh P, Setola V, Tran TB, Roth BL, Aubé J.

ACS Med Chem Lett. 2010 Aug 12;1(5):189-193.

13.

The effects of kappa-opioid receptor ligands on prepulse inhibition and CRF-induced prepulse inhibition deficits in the rat.

Tejeda HA, Chefer VI, Zapata A, Shippenberg TS.

Psychopharmacology (Berl). 2010 Jun;210(2):231-40. doi: 10.1007/s00213-010-1799-6. Epub 2010 Mar 16.

14.

Selective KOP Receptor Agonists: Probe 1 & Probe 2.

Hedrick MP, Gosalia P, Frankowski K, Shi S, Prisinzano TE, Schoenen F, Aubé J, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Ghosh P, Milan L, Heynen-Genel S, Chung TDY, Dad S, Caron M, Bohn LM, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 28 [updated 2010 Oct 4].

15.

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.

16.

Use of the mouse vas deferens to determine mu, delta, and kappa receptor affinities of opioid antagonists.

Cohen ML, Mendelsohn LG, Mitch CH, Zimmerman DM.

Receptor. 1994 Spring;4(1):43-53.

PMID:
8038706
17.

Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.

Schiller PW, Berezowska I, Nguyen TM, Schmidt R, Lemieux C, Chung NN, Falcone-Hindley ML, Yao W, Liu J, Iwama S, Smith AB 3rd, Hirschmann R.

J Med Chem. 2000 Feb 24;43(4):551-9.

PMID:
10691681
18.

Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

Li G, Aschenbach LC, Chen J, Cassidy MP, Stevens DL, Gabra BH, Selley DE, Dewey WL, Westkaemper RB, Zhang Y.

J Med Chem. 2009 Mar 12;52(5):1416-27. doi: 10.1021/jm801272c.

19.

Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective mu/kappa antagonist in the [35S]-GTP-gamma-S functional binding assay.

Romero DV, Partilla JS, Zheng QX, Heyliger SO, Ni Q, Rice KC, Lai J, Rothman RB.

Synapse. 1999 Nov;34(2):83-94.

PMID:
10502307
20.

Kappa-opioid agonists directly inhibit midbrain dopaminergic neurons.

Margolis EB, Hjelmstad GO, Bonci A, Fields HL.

J Neurosci. 2003 Nov 5;23(31):9981-6.

Supplemental Content

Support Center