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Items: 1 to 20 of 287

1.

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.

2.

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.

3.

Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.

Agnes RS, Lee YS, Davis P, Ma SW, Badghisi H, Porreca F, Lai J, Hruby VJ.

J Med Chem. 2006 May 18;49(10):2868-75.

4.

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.

5.

Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.

Salvadori S, Balboni G, Guerrini R, Tomatis R, Bianchi C, Bryant SD, Cooper PS, Lazarus LH.

J Med Chem. 1997 Sep 12;40(19):3100-8.

PMID:
9301674
6.

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
7.

Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.

Lee YS, Agnes RS, Badghisi H, Davis P, Ma SW, Lai J, Porreca F, Hruby VJ.

J Med Chem. 2006 Mar 9;49(5):1773-80.

8.

Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.

Fujita Y, Tsuda Y, Li T, Motoyama T, Takahashi M, Shimizu Y, Yokoi T, Sasaki Y, Ambo A, Kita A, Jinsmaa Y, Bryant SD, Lazarus LH, Okada Y.

J Med Chem. 2004 Jul 1;47(14):3591-9.

PMID:
15214786
9.

Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.

Tóth G, Ioja E, Tömböly C, Ballet S, Tourwé D, Péter A, Martinek T, Chung NN, Schiller PW, Benyhe S, Borsodi A.

J Med Chem. 2007 Jan 25;50(2):328-33.

PMID:
17228874
10.

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
11.

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.

Lee YS, Petrov R, Park CK, Ma SW, Davis P, Lai J, Porreca F, Vardanyan R, Hruby VJ.

J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.

12.

Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.

Tourwé D, Mannekens E, Diem TN, Verheyden P, Jaspers H, Tóth G, Péter A, Kertész I, Török G, Chung NN, Schiller PW.

J Med Chem. 1998 Dec 17;41(26):5167-76.

PMID:
9857087
13.

Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.

Balboni G, Salvadori S, Guerrini R, Negri L, Giannini E, Bryant SD, Jinsmaa Y, Lazarus LH.

J Med Chem. 2004 Jul 29;47(16):4066-71.

PMID:
15267245
14.

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.

15.

Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.

Salvadori S, Guerrini R, Balboni G, Bianchi C, Bryant SD, Cooper PS, Lazarus LH.

J Med Chem. 1999 Dec 2;42(24):5010-9.

PMID:
10585210
16.

From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.

Balboni G, Cocco MT, Salvadori S, Romagnoli R, Sasaki Y, Okada Y, Bryant SD, Jinsmaa Y, Lazarus LH.

J Med Chem. 2005 Aug 25;48(17):5608-11.

PMID:
16107162
17.

Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.

Li T, Shiotani K, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Lazarus LH, Okada Y.

J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.

19.

Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].

Ananthan S, Khare NK, Saini SK, Seitz LE, Bartlett JL, Davis P, Dersch CM, Porreca F, Rothman RB, Bilsky EJ.

J Med Chem. 2004 Mar 11;47(6):1400-12. Erratum in: J Med Chem. 2004 May 6;47(10):2716.

PMID:
14998329
20.

Development of potent μ and δ opioid agonists with high lipophilicity.

Lee YS, Kulkarani V, Cowell SM, Ma SW, Davis P, Hanlon KE, Vanderah TW, Lai J, Porreca F, Vardanyan R, Hruby VJ.

J Med Chem. 2011 Jan 13;54(1):382-6. doi: 10.1021/jm100982d. Epub 2010 Dec 3.

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