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A Cyclic Tetrapeptide (“Cyclodal”) and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9243-9254

2016

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‘Carba’-carfentanil (trans isomer): A μ opioid receptor (MOR) partial agonist with a distinct binding mode

Bioorganic & medicinal chemistry, 2014-09, Vol.22 (17), p.4581-4586

2014

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"Carba"-analogues of fentanyl are opioid receptor agonists

Journal of medicinal chemistry, 2010-04, Vol.53 (7), p.2875-2881

2010

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An enzymatically stable kyotorphin analog induces pain in subattomol doses

Peptides (New York, N.Y. : 1980), 2000-05, Vol.21 (5), p.717-722

2000

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N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile

Bioorganic & medicinal chemistry letters, 2013-09, Vol.23 (18), p.5082-5085

2013

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The Opioid μ Agonist/δ Antagonist DIPP-NH2[Ψ] Produces a Potent Analgesic Effect, No Physical Dependence, and Less Tolerance than Morphine in Rats

Journal of medicinal chemistry, 1999-09, Vol.42 (18), p.3520-3526

1999

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Synthesis and in vitro opioid activity profiles of DALDA analogues

European journal of medicinal chemistry, 2000-10, Vol.35 (10), p.895-901

2000

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Equipotent enantiomers of cyclic opioid peptides at μ opioid receptor

Peptide science (Hoboken, N.J.), 2019-01, Vol.111 (1), p.n/a

2019

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[2‘,6‘-Dimethyltyrosine]Dynorphin A(1−11)-NH2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

Journal of medicinal chemistry, 2001-09, Vol.44 (19), p.3048-3053

2001

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“Carba”-Analogues of Fentanyl are Opioid Receptor Agonists ‡ Dedicated to the memory of Ralph F. Hirschmann

Journal of medicinal chemistry, 2010-04, Vol.53 (7), p.2875-2881

2010

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N-Methylated Cyclic Enkephalin Analogues Retain High Opioid Receptor Binding Affinity

Chemical biology & drug design, 2010-02, Vol.75 (2), p.182-188

2010

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Novel Opioid Peptide Derived Antagonists Containing (2S)-2-Methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic Acid [(2S)-Mdcp]

Journal of medicinal chemistry, 2008-09, Vol.51 (18), p.5866-5870

2008

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Stereoselective synthesis of (3S)- and (3R)-3-hydroxy-3-(2,6-dimethyl-4-hydroxyphenyl)propanoic acid and its incorporation into a cyclic enkephalin analogue

Advances in experimental medicine and biology, 2009, Vol.611, p.207

2009

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Attenuation of morphine tolerance and dependence with the highly selective δ-opioid receptor antagonist TIPP[ψ]

European journal of pharmacology, 1995-11, Vol.286 (1), p.105-108

1995

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The TIPP opioid peptide family: Development of δ antagonists, δ agonists, and mixed μ agonist/δ antagonists

BIOPOLYM, 1999, Vol.51 (6), p.411-425

1999

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Conformationally constrained opioid peptide analogs with novel activity profiles

International journal of peptide research and therapeutics, 1998-05, Vol.5 (2-3), p.209-214

1998

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Differential Stereochemical Requirements of μ vs. δ Opioid Receptors for Ligand Binding and Signal Transduction: Development of a Class of Potent and Highly δ-Selective Peptide Antagonists

Proceedings of the National Academy of Sciences - PNAS, 1992-12, Vol.89 (24), p.11871-11875

1992

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Potent Opioid Peptide Agonists Containing 4'-[N-((4'-phenyl)-phenethyl)carboxamido]phenylalanine (Bcp) in Place of Tyr

Chemical biology & drug design, 2008-11, Vol.72 (5), p.337-340

2008

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Conversion of δ-, κ- and μ-receptor selective opioid peptide agonists into δ-, κ- and μ-selective antagonists

Life sciences (1973), 2003-06, Vol.73 (6), p.691-698

2003

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A novel cyclic enkephalin analogue with potent opioid antagonist activity

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (18), p.4731-4733

2004

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Replacement of the N-terminal Tyrosine Residue in Opioid Peptides with 3-(2,6-Dimethyl-4-carbamoylphenyl)propanoic Acid (Dcp) Results in Novel Opioid Antagonists

Journal of medicinal chemistry, 2006-08, Vol.49 (17), p.5382-5385

2006

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TIPP[.psi.]: a highly potent and stable pseudopeptide .delta. opioid receptor antagonist with extraordinary .delta. selectivity

Journal of medicinal chemistry, 1993-10, Vol.36 (21), p.3182-3187

1993

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Stereospecific synthesis of (2S)-2-methyl-3-(2', 6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide

Bioorganic & medicinal chemistry letters, 2001-02, Vol.11 (3), p.323-325

2001

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[2‘,6‘-Dimethyltyrosine]Dynorphin A(1−11)-NH 2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

Journal of medicinal chemistry, 2001-09, Vol.44 (19), p.3048-3053

2001

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Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analog: effects on receptor selectivity and stereospecificity

Journal of medicinal chemistry, 1991-10, Vol.34 (10), p.3125-3132

1991

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A Cyclic Tetrapeptide (“Cyclodal”) and Its Mirror-Image Isomer Are Both High-Affinity μ Opioid Receptor Antagonists

‘Carba’-carfentanil (trans isomer): A μ opioid receptor (MOR) partial agonist with a distinct binding mode

"Carba"-analogues of fentanyl are opioid receptor agonists

An enzymatically stable kyotorphin analog induces pain in subattomol doses

N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile

The Opioid μ Agonist/δ Antagonist DIPP-NH2[Ψ] Produces a Potent Analgesic Effect, No Physical Dependence, and Less Tolerance than Morphine in Rats

Synthesis and in vitro opioid activity profiles of DALDA analogues

Equipotent enantiomers of cyclic opioid peptides at μ opioid receptor

[2‘,6‘-Dimethyltyrosine]Dynorphin A(1−11)-NH2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

“Carba”-Analogues of Fentanyl are Opioid Receptor Agonists ‡ Dedicated to the memory of Ralph F. Hirschmann

N-Methylated Cyclic Enkephalin Analogues Retain High Opioid Receptor Binding Affinity

Novel Opioid Peptide Derived Antagonists Containing (2S)-2-Methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic Acid [(2S)-Mdcp]

Stereoselective synthesis of (3S)- and (3R)-3-hydroxy-3-(2,6-dimethyl-4-hydroxyphenyl)propanoic acid and its incorporation into a cyclic enkephalin analogue

Attenuation of morphine tolerance and dependence with the highly selective δ-opioid receptor antagonist TIPP[ψ]

The TIPP opioid peptide family: Development of δ antagonists, δ agonists, and mixed μ agonist/δ antagonists

Conformationally constrained opioid peptide analogs with novel activity profiles

Differential Stereochemical Requirements of μ vs. δ Opioid Receptors for Ligand Binding and Signal Transduction: Development of a Class of Potent and Highly δ-Selective Peptide Antagonists

Potent Opioid Peptide Agonists Containing 4'-[N-((4'-phenyl)-phenethyl)carboxamido]phenylalanine (Bcp) in Place of Tyr

Conversion of δ-, κ- and μ-receptor selective opioid peptide agonists into δ-, κ- and μ-selective antagonists

A novel cyclic enkephalin analogue with potent opioid antagonist activity

Replacement of the N-terminal Tyrosine Residue in Opioid Peptides with 3-(2,6-Dimethyl-4-carbamoylphenyl)propanoic Acid (Dcp) Results in Novel Opioid Antagonists

TIPP[.psi.]: a highly potent and stable pseudopeptide .delta. opioid receptor antagonist with extraordinary .delta. selectivity

Stereospecific synthesis of (2S)-2-methyl-3-(2', 6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide

[2‘,6‘-Dimethyltyrosine]Dynorphin A(1−11)-NH 2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analog: effects on receptor selectivity and stereospecificity

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