PMID
Data
Article Title
Organization
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.

Clinical Research Institute of Montreal
[Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.

Nanjing Medical University
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.

Vrije Universiteit Brussel
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.

Vrije Universiteit Brussel
'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.

Clinical Research Institute of Montreal
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.

Vrije Universiteit Brussel
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt

Vrije Universiteit Brussel
[Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile.

Nanjing Medical University
Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at thed opioid receptor. Discovery of two highly potent and selectived opioid agonists.

Clinical Research Institute of Montreal
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.

Vrije Universiteit Brussel
"Carba"-analogues of fentanyl are opioid receptor agonists.

Clinical Research Institute of Montreal
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.

Vrije Universiteit Brussel
Structure-activity relationships of dynorphin a analogues modified in the address sequence.

University of California
Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.

University of Lausanne
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.

Clinical Research Institute of Montreal
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.

Clinical Research Institute of Montr£Al
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.

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

Vrije Universiteit Brussel
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.

Clinical Research Institute of Montreal
TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity.

Clinical Research Institute of Montreal
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.

Smith Kline and French Laboratories
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.

University of Minnesota
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.

TBA
Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.

TBA
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.

Vrije Universiteit Brussel
Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).

Clinical Research Institute of Montreal
Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].

National University of Singapore
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.

Medical University of Lodz
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.

Clinical Research Institute of Montreal
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).

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

Hungarian Academy of Sciences
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.

National University of Singapore
A new structural motif for mu-opioid antagonists.

Vrije Universiteit Brussel
A novel cyclic enkephalin analogue with potent opioid antagonist activity.

Clinical Research Institute of Montreal
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.

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

Clinical Research Institute of Montreal
The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.

Clinical Research Institute of Montreal
A topochemical approach to explain morphiceptin bioactivity.

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

Clinical Research Institute of Montreal
Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.

University of Montpellier
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.

Clinical Research Institute of Montreal
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity.

Clinical Research Institute of Montreal
χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.

Vrije Universiteit Brussel
Chemical space screening around Phe

Vrije Universiteit Brussel
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.

Clinical Research Institute of Montreal
Conformationally restricted deltorphin analogues.

Clinical Research Institute of Montreal
Structural basis for selective inhibition of Src family kinases by PP1.

Princeton University
Ultrasensitive in situ visualization of active glucocerebrosidase molecules.

Leiden University
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.

Novartis