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Items: 1 to 50 of 500

1.

Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.

Yamamoto T, Nair P, Largent-Milnes TM, Jacobsen NE, Davis P, Ma SW, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.

J Med Chem. 2011 Apr 14;54(7):2029-38. doi: 10.1021/jm101023r. Epub 2011 Mar 2.

2.

Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.

Yamamoto T, Nair P, Jacobsen NE, Kulkarni V, Davis P, Ma SW, Navratilova E, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.

J Med Chem. 2010 Aug 12;53(15):5491-501. doi: 10.1021/jm100157m.

3.

Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.

Yamamoto T, Nair P, Jacobsen NE, Vagner J, Kulkarni V, Davis P, Ma SW, Navratilova E, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.

J Med Chem. 2009 Aug 27;52(16):5164-75. doi: 10.1021/jm900473p.

4.

Functional selectivity in cannabinoid signaling.

Varga EV, Georgieva T, Tumati S, Alves I, Salamon Z, Tollin G, Yamamura HI, Roeske WR.

Curr Mol Pharmacol. 2008 Nov;1(3):273-84. Review.

PMID:
20021440
5.

The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.

Yamamoto T, Nair P, Ma SW, Davis P, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.

Bioorg Med Chem. 2009 Oct 15;17(20):7337-43. doi: 10.1016/j.bmc.2009.08.035. Epub 2009 Aug 21.

6.

Sustained morphine treatment augments capsaicin-evoked calcitonin gene-related peptide release from primary sensory neurons in a protein kinase A- and Raf-1-dependent manner.

Tumati S, Yamamura HI, Vanderah TW, Roeske WR, Varga EV.

J Pharmacol Exp Ther. 2009 Sep;330(3):810-7. doi: 10.1124/jpet.109.151704. Epub 2009 Jun 2.

7.

Novel bifunctional peptides as opioid agonists and NK-1 antagonists.

Nair P, Yamamoto T, Kulkarni V, Moye S, Navratilova E, Davis P, Largent T, Ma SW, Yamamura HI, Vanderah T, Lai J, Porreca F, Hruby VJ.

Adv Exp Med Biol. 2009;611:537-8. No abstract available.

8.

Sustained cannabinoid agonist treatment augments CGRP release in a PKA-dependent manner.

Tumati S, Yamamura HI, St John PA, Vanderah TW, Roeske WR, Varga EV.

Neuroreport. 2009 May 27;20(8):815-9. doi: 10.1097/WNR.0b013e32832be50b.

PMID:
19387418
9.

Constitutive activity at the cannabinoid CB1 receptor is required for behavioral response to noxious chemical stimulation of TRPV1: antinociceptive actions of CB1 inverse agonists.

Fioravanti B, De Felice M, Stucky CL, Medler KA, Luo MC, Gardell LR, Ibrahim M, Malan TP Jr, Yamamura HI, Ossipov MH, King T, Lai J, Porreca F, Vanderah TW.

J Neurosci. 2008 Nov 5;28(45):11593-602. doi: 10.1523/JNEUROSCI.3322-08.2008.

10.

Intrathecal Raf-1-selective siRNA attenuates sustained morphine-mediated thermal hyperalgesia.

Tumati S, Milnes TL, Yamamura HI, Vanderah TW, Roeske WR, Varga EV.

Eur J Pharmacol. 2008 Dec 28;601(1-3):207-8. doi: 10.1016/j.ejphar.2008.10.033. Epub 2008 Oct 21.

11.

The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.

Yamamoto T, Nair P, Jacobsen NE, Davis P, Ma SW, Navratilova E, Moye S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.

J Med Chem. 2008 Oct 23;51(20):6334-47. doi: 10.1021/jm800389v. Epub 2008 Sep 27.

12.

Sustained morphine treatment augments basal CGRP release from cultured primary sensory neurons in a Raf-1 dependent manner.

Yue X, Tumati S, Navratilova E, Strop D, St John PA, Vanderah TW, Roeske WR, Yamamura HI, Varga EV.

Eur J Pharmacol. 2008 Apr 28;584(2-3):272-7. doi: 10.1016/j.ejphar.2008.02.013. Epub 2008 Feb 14.

13.

A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.

Yamamoto T, Nair P, Vagner J, Largent-Milnes T, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.

J Med Chem. 2008 Mar 13;51(5):1369-76. doi: 10.1021/jm070332f. Epub 2008 Feb 12.

14.

Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling.

Georgieva T, Devanathan S, Stropova D, Park CK, Salamon Z, Tollin G, Hruby VJ, Roeske WR, Yamamura HI, Varga E.

Eur J Pharmacol. 2008 Feb 26;581(1-2):19-29. Epub 2007 Nov 28.

15.

Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.

Yamamoto T, Nair P, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Vanderah TW, Yamamura HI, Porreca F, Hruby VJ.

J Med Chem. 2007 Jun 14;50(12):2779-86. Epub 2007 May 22.

16.

A red clover (Trifolium pratense) phase II clinical extract possesses opiate activity.

Nissan HP, Lu J, Booth NL, Yamamura HI, Farnsworth NR, Wang ZJ.

J Ethnopharmacol. 2007 May 30;112(1):207-10. Epub 2007 Feb 11.

PMID:
17350196
17.

Quantitative evaluation of human delta opioid receptor desensitization using the operational model of drug action.

Navratilova E, Waite S, Stropova D, Eaton MC, Alves ID, Hruby VJ, Roeske WR, Yamamura HI, Varga EV.

Mol Pharmacol. 2007 May;71(5):1416-26. Epub 2007 Feb 22.

PMID:
17322005
18.
19.

New paradigms and tools in drug design for pain and addiction.

Hruby VJ, Porreca F, Yamamura HI, Tollin G, Agnes RS, Lee YS, Cai M, Alves I, Cowell S, Varga E, Davis P, Salamon Z, Roeske W, Vanderah T, Lai J.

AAPS J. 2006 Jul 14;8(3):E450-60. Review.

20.

Chronic morphine-mediated adenylyl cyclase superactivation is attenuated by the Raf-1 inhibitor, GW5074.

Yue X, Varga EV, Stropova D, Vanderah TW, Yamamura HI, Roeske WR.

Eur J Pharmacol. 2006 Jul 1;540(1-3):57-9. Epub 2006 May 3.

PMID:
16750187
21.

Characterization of muscarinic receptor binding and inhibition of salivation after oral administration of tolterodine in mice.

Oki T, Maruyama S, Takagi Y, Yamamura HI, Yamada S.

Eur J Pharmacol. 2006 Jan 4;529(1-3):157-63. Epub 2005 Nov 28.

PMID:
16316647
22.

Lipid bilayers on polyacrylamide brushes for inclusion of membrane proteins.

Smith EA, Coym JW, Cowell SM, Tokimoto T, Hruby VJ, Yamamura HI, Wirth MJ.

Langmuir. 2005 Oct 11;21(21):9644-50.

23.

Morphine promotes phosphorylation of the human delta-opioid receptor at serine 363.

Navratilova E, Eaton MC, Stropova D, Varga EV, Vanderah TW, Roeske WR, Yamamura HI.

Eur J Pharmacol. 2005 Sep 20;519(3):212-4.

PMID:
16135360
24.

Development of a lanthanide-based assay for detection of receptor-ligand interactions at the delta-opioid receptor.

Handl HL, Vagner J, Yamamura HI, Hruby VJ, Gillies RJ.

Anal Biochem. 2005 Aug 15;343(2):299-307.

PMID:
16004955
25.

Glycopeptides related to beta-endorphin adopt helical amphipathic conformations in the presence of lipid bilayers.

Dhanasekaran M, Palian MM, Alves I, Yeomans L, Keyari CM, Davis P, Bilsky EJ, Egleton RD, Yamamura HI, Jacobsen NE, Tollin G, Hruby VJ, Porreca F, Polt R.

J Am Chem Soc. 2005 Apr 20;127(15):5435-48.

PMID:
15826181
26.

Antinociception depends on the presence of G protein gamma2-subunits in brain.

Varga EV, Hosohata K, Borys D, Navratilova E, Nylen A, Vanderah TW, Porreca F, Roeske WR, Yamamura HI.

Eur J Pharmacol. 2005 Jan 31;508(1-3):93-8. Epub 2005 Jan 12.

PMID:
15680258
27.

Parallel synthesis and biological evaluation of different sizes of bicyclo[2,3]-Leu-enkephalin analogues.

Gu X, Ying J, Min B, Cain JP, Davis P, Willey P, Navratilova E, Yamamura HI, Porreca F, Hruby VJ.

Biopolymers. 2005;80(2-3):151-63.

PMID:
15660379
28.

Agonist-specific regulation of the delta-opioid receptor.

Varga EV, Navratilova E, Stropova D, Jambrosic J, Roeske WR, Yamamura HI.

Life Sci. 2004 Dec 24;76(6):599-612. Review.

PMID:
15567186
29.

Novel design of bicyclic beta-turn dipeptides on solid-phase supports and synthesis of [3.3.0]-Bicyclo([2,3])-leu-enkephalin analogues.

Gu X, Ying J, Agnes RS, Navratilova E, Davis P, Stahl G, Porreca F, Yamamura HI, Hruby VJ.

Org Lett. 2004 Sep 16;6(19):3285-8.

PMID:
15355033
30.

Selectivity, cooperativity, and reciprocity in the interactions between the delta-opioid receptor, its ligands, and G-proteins.

Alves ID, Ciano KA, Boguslavski V, Varga E, Salamon Z, Yamamura HI, Hruby VJ, Tollin G.

J Biol Chem. 2004 Oct 22;279(43):44673-82. Epub 2004 Aug 17. Erratum in: J Biol Chem. 2005 Dec 2;280(48):40384.

31.

Lanthanide-based time-resolved fluorescence of in cyto ligand-receptor interactions.

Handl HL, Vagner J, Yamamura HI, Hruby VJ, Gillies RJ.

Anal Biochem. 2004 Jul 15;330(2):242-50.

PMID:
15203329
32.

Real time differentiation of G-protein coupled receptor (GPCR) agonist and antagonist by two photon fluorescence laser microscopy.

Cai M, Stankova M, Pond SJ, Mayorov AV, Perry JW, Yamamura HI, Trivedi D, Hruby VJ.

J Am Chem Soc. 2004 Jun 16;126(23):7160-1.

PMID:
15186137
33.

Antinociceptive structure-activity studies with enkephalin-based opioid glycopeptides.

Elmagbari NO, Egleton RD, Palian MM, Lowery JJ, Schmid WR, Davis P, Navratilova E, Dhanasekaran M, Keyari CM, Yamamura HI, Porreca F, Hruby VJ, Polt R, Bilsky EJ.

J Pharmacol Exp Ther. 2004 Oct;311(1):290-7. Epub 2004 May 27.

PMID:
15166257
34.

Mutation S363A in the human delta-opioid receptor selectively reduces down-regulation by a peptide agonist.

Navratilova E, Varga EV, Stropova D, Jambrosic JC, Roeske WR, Yamamura HI.

Eur J Pharmacol. 2004 Feb 6;485(1-3):341-3.

PMID:
14757159
35.

Molecular mechanisms of excitatory signaling upon chronic opioid agonist treatment.

Varga EV, Yamamura HI, Rubenzik MK, Stropova D, Navratilova E, Roeske WR.

Life Sci. 2003 Dec 5;74(2-3):299-311. Review.

PMID:
14607258
36.

Direct observation of G-protein binding to the human delta-opioid receptor using plasmon-waveguide resonance spectroscopy.

Alves ID, Salamon Z, Varga E, Yamamura HI, Tollin G, Hruby VJ.

J Biol Chem. 2003 Dec 5;278(49):48890-7. Epub 2003 Sep 30. Erratum in: J Biol Chem. 2005 Dec 30;280(52):43280.

37.

Converging protein kinase pathways mediate adenylyl cyclase superactivation upon chronic delta-opioid agonist treatment.

Varga EV, Rubenzik MK, Stropova D, Sugiyama M, Grife V, Hruby VJ, Rice KC, Roeske WR, Yamamura HI.

J Pharmacol Exp Ther. 2003 Jul;306(1):109-15. Epub 2003 Mar 26.

PMID:
12660310
38.

(2S,3R) beta-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinoline-3-carboxylic acid [(2S,3R)TMT-L-Tic-OH] is a potent, selective delta-opioid receptor antagonist in mouse brain.

Hosohata K, Varga EV, Alfaro-Lopez J, Tang X, Vanderah TW, Porreca F, Hruby VJ, Roeske WR, Yamamura HI.

J Pharmacol Exp Ther. 2003 Feb;304(2):683-8.

PMID:
12538822
39.

Agonist-specific down-regulation of the human delta-opioid receptor.

Okura T, Varga EV, Hosohata Y, Navratilova E, Cowell SM, Rice K, Nagase H, Hruby VJ, Roeske WR, Yamamura HI.

Eur J Pharmacol. 2003 Jan 10;459(1):9-16.

PMID:
12505529
40.

Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation.

Varga EV, Rubenzik M, Grife V, Sugiyama M, Stropova D, Roeske WR, Yamamura HI.

Eur J Pharmacol. 2002 Sep 6;451(1):101-2.

PMID:
12223234
41.

Cannabinoid CB(1) receptor expression, activation and detection of endogenous ligand in trabecular meshwork and ciliary process tissues.

Stamer WD, Golightly SF, Hosohata Y, Ryan EP, Porter AC, Varga E, Noecker RJ, Felder CC, Yamamura HI.

Eur J Pharmacol. 2001 Nov 23;431(3):277-86.

PMID:
11730719
43.

Pharmacodynamic and pharmacokinetic characterization of poly(ethylene glycol) conjugation to met-enkephalin analog [D-Pen2, D-Pen5]-enkephalin (DPDPE).

Witt KA, Huber JD, Egleton RD, Roberts MJ, Bentley MD, Guo L, Wei H, Yamamura HI, Davis TP.

J Pharmacol Exp Ther. 2001 Aug;298(2):848-56.

PMID:
11454951
44.

Mutation W284L of the human delta opioid receptor reveals agonist specific receptor conformations for G protein activation.

Hosohata Y, Varga EV, Stropova D, Li X, Knapp RJ, Hruby VJ, Rice KC, Nagase H, Roeske WR, Yamamura HI.

Life Sci. 2001 Apr 6;68(19-20):2233-42.

PMID:
11358332
45.

Synthesis, biology, NMR and conformation studies of the topographically constrained delta-opioid selective peptide analogs of [beta-iPrPhe(3)]deltorphin I.

Liao S, Shenderovich M, Kövér KE, Zhang Z, Hosohata K, Davis P, Porreca F, Yamamura HI, Hurby VJ.

J Pept Res. 2001 Apr;57(4):257-76.

PMID:
11328484
46.

Biological properties of Phe(o)-opioid peptide analogues.

Lipkowski AW, Misicka A, Hosohata K, Davis P, Yamamura HI, Porreca F, Hruby VJ.

Life Sci. 2001 Jan 12;68(8):969-72.

PMID:
11213367
47.
48.

Improved bioavailability to the brain of glycosylated Met-enkephalin analogs.

Egleton RD, Mitchell SA, Huber JD, Janders J, Stropova D, Polt R, Yamamura HI, Hruby VJ, Davis TP.

Brain Res. 2000 Oct 20;881(1):37-46.

PMID:
11033091
49.

Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.

Bilsky EJ, Egleton RD, Mitchell SA, Palian MM, Davis P, Huber JD, Jones H, Yamamura HI, Janders J, Davis TP, Porreca F, Hruby VJ, Polt R.

J Med Chem. 2000 Jun 29;43(13):2586-90.

PMID:
10891118
50.

Assessment of stereoselectivity of trimethylphenylalanine analogues of delta-opioid [D-Pen(2),D-Pen(5)]-enkephalin.

Witt KA, Slate CA, Egleton RD, Huber JD, Yamamura HI, Hruby VJ, Davis TP.

J Neurochem. 2000 Jul;75(1):424-35.

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