PMID
Data
Article Title
Organization
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.

University of Arizona
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.

University of Arizona
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.

University of Arizona
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.

Vrije Universiteit Brussel
Novel cyclic biphalin analogue with improved antinociceptive properties.

D'Annunzio University of Chieti���Pescara
Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.

University of Arizona
Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.

D'Annunzio University of Chieti���Pescara
Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine.

Neuraxon
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.

D'Annunzio University of Chieti���Pescara
1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.

Neuraxon
The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.

D'Annunzio University of Chieti���Pescara
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.

Neuraxon
Structure-activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors.

Zalicus Pharmaceuticals
Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS).

Neuraxon
Discovery of N-(3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a selective inhibitor of human neuronal nitric oxide synthase (nNOS) for the treatment of pain.

Neuraxon
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.

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

University of Arizona
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).

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

University of Arizona
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.

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

Southern Research Institute
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.

National Institute of Diabetes and Digestive and Kidney Diseases
Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.

University of Northern Colorado
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.

National Institute of Diabetes
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.

National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.

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

Southern Research Institute
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r

National Institute of Diabetes and Digestive and Kidney Diseases
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.

University of Arizona
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.

National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.

National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.

National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.

National Institute of Diabetes and Digestive and Kidney Diseases
Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.

University of Arizona
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.

University of Arizona
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.

University of Arizona
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.

Southern Research Institute
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.

University of Louisville
3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors.

Neuraxon
Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.

Neuraxon
Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.

Neuraxon
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.

University of Arizona
1,6-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.

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

University of Arizona
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.

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

University of Arizona
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.

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

University of Arizona
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.

University of Arizona
Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.

Sapienza University of Rome
The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-Tic

TBA
A new approach to enhance bioavailability of biologically active peptides: conjugation of a δ opioid agonist to β-cyclodextrin

TBA
Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ
1
TBA
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.

University of Arizona
Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.

Northeastern University
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.

University of Arizona
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.

University of Arizona
Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.

University of Arizona
Synthesis and biological activity of the first cyclic biphalin analogues.

University of Arizona
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.

University of The Punjab
Structure-Activity Relationships of [des-Arg

University of Arizona
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.

National Institute of Diabetes and Digestive and Kidney Diseases
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).

The Scripps Research Institute
Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.

University of Arizona
Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.

The University of Arizona
Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.

University of Louisville
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.

University of Arizona
Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.

University of Arizona
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.

The University of Arizona
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.

University of Arizona
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.

University of Arizona
Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.

University of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.

University of Arizona
Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.

University of Arizona
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.

University of Arizona
Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).

University of Michigan
Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).

University of Michigan
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.

University of Arizona
Chiral Effect of a Phe Residue in Position 3 of the Dmt

University of Arizona
Effect of anchoring 4-anilidopiperidines to opioid peptides.

University of Arizona
Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.

University of Arizona
Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.

University of Arizona
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.

Neuromed Pharmaceuticals
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors.

University of Arizona
Immunomodulators

Bristol-Myers Squibb
Pyrrolobenzodiazepines and conjugates thereof

Mersana Therapeutics
Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication

Viiv Healthcare UK (NO.5)
Triazolopyridines and triazolopyrazines as LSD1 inhibitors

Incyte
3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).

Smithkline Beecham Pharmaceuticals