Structure–Activity Relationship Studies on Oxazolo[3,4-a]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent In Vivo Activity

Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis

(2019) Mathieu Rappas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor

(2018) Zhenlin Yang et al.   NATURE

Orthosteric and allosteric action of the C5a receptor antagonists

(2018) Heng Liu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Orthosteric and allosteric action of the C5a receptor antagonists

(2018) Heng Liu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An Efficient One-Pot Synthesis of Chiral N-Protected 3-Substituted (Diketo)piperazines via Ugi-4CR/De-Boc/Cyclization Process

(2018) Mouhamad Jida et al.   ChemistrySelect

Structural insights into the subtype-selective antagonist binding to the M2 muscarinic receptor

(2018) Ryoji Suno et al.   Nature Chemical Biology

X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog

(2017) Wataru Shihoya et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog

(2017) Wataru Shihoya et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Neuropeptide S receptor ligands: a patent review (2005-2016)

(2016) Chiara Ruzza et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

(2016) Jie Yin et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure of the Angiotensin Receptor Revealed by Serial Femtosecond Crystallography

(2015) Haitao Zhang et al.   CELL

Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor

(2015) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

OPLS3: A Force Field Providing Broad Coverage of Drug-like Small Molecules and Proteins

(2015) Edward Harder et al.   Journal of Chemical Theory and Computation

Like-Charge Guanidinium Pairing between Ligand and Receptor: An Unusual Interaction for Drug Discovery and Design?

(2015) Yang Yang et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Neuropeptide S reduces mouse aggressiveness in the resident/intruder test through selective activation of the neuropeptide S receptor

(2015) Chiara Ruzza et al.   NEUROPHARMACOLOGY

Neuropeptide S Increases locomotion activity through corticotropin-releasing factor receptor 1 in substantia nigra of mice

(2015) M.S. Li et al.   PEPTIDES

Identification of Neuropeptide S Antagonists: Structure–Activity Relationship Studies, X-ray Crystallography, and in Vivo Evaluation

(2014) Carla Hassler et al.   ACS Chemical Neuroscience

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Biological activities of guanidine compounds, 2008 – 2012 update

(2013) Franciszek Sączewski et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Neuropeptide S enhances memory and mitigates memory impairment induced by MK801, scopolamine or Aβ1–42 in mice novel object and object location recognition tasks

(2013) Ren-Wen Han et al.   NEUROPHARMACOLOGY

In vitro and in vivo pharmacological characterization of the novel neuropeptide S receptor ligands QA1 and PI1

(2013) V. Camarda et al.   PEPTIDES

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

Behavioural phenotypic characterization of CD-1 mice lacking the neuropeptide S receptor

(2012) C. Ruzza et al.   NEUROPHARMACOLOGY

[tBu-d-Gly5]NPS, a pure and potent antagonist of the neuropeptide S receptor: In vitro and in vivo studies

(2012) C. Ruzza et al.   PEPTIDES

Antagonism of the neuropeptide S receptor with RTI-118 decreases cocaine self-administration and cocaine-seeking behavior in rats

(2012) Christopher D. Schmoutz et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Anatomical characterization of the neuropeptide S system in the mouse brain by in situ hybridization and immunohistochemistry

(2011) Stewart D. Clark et al.   JOURNAL OF COMPARATIVE NEUROLOGY

Synthesis and Separation of the Enantiomers of the Neuropeptide S Receptor Antagonist (9R/S)-3-Oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic Acid 4-Fluoro-benzylamide (SHA 68)

(2011) Claudio Trapella et al.   JOURNAL OF MEDICINAL CHEMISTRY

Animal research: Reporting in vivo experiments: The ARRIVE guidelines

(2010) Carol Kilkenny et al.   BRITISH JOURNAL OF PHARMACOLOGY

Molecular Modeling Studies on the Human Neuropeptide S Receptor and Its Antagonists

(2010) Diego Dal Ben et al.   ChemMedChem

Lipophilicity in drug discovery

(2010) Michael J Waring   Expert Opinion on Drug Discovery

Neuropeptide S Enhances Memory During the Consolidation Phase and Interacts with Noradrenergic Systems in the Brain

(2010) Naoe Okamura et al.   NEUROPSYCHOPHARMACOLOGY

Further studies on the pharmacological profile of the neuropeptide S receptor antagonist SHA 68

(2010) Chiara Ruzza et al.   PEPTIDES

Neuropeptide S facilitates cue-induced relapse to cocaine seeking through activation of the hypothalamic hypocretin system

(2010) M. Kallupi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Abnormal response to stress and impaired NPS-induced hyperlocomotion, anxiolytic effect and corticosterone increase in mice lacking NPSR1

(2010) Hongyan Zhu et al.   PSYCHONEUROENDOCRINOLOGY

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Behavioral phenotyping of Neuropeptide S receptor knockout mice

(2009) Dee M. Duangdao et al.   BEHAVIOURAL BRAIN RESEARCH

Biological activities of guanidine compounds

(2009) Franciszek Saczewski et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Neuropeptide S Reinstates Cocaine-Seeking Behavior and Increases Locomotor Activity through Corticotropin-Releasing Factor Receptor 1 in Mice

(2009) C. Paneda et al.   JOURNAL OF NEUROSCIENCE

Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptor

(2009) Remo Guerrini et al.   MEDICINAL RESEARCH REVIEWS

Persistent Increase of Alcohol-Seeking Evoked by Neuropeptide S: an Effect Mediated by the Hypothalamic Hypocretin System

(2009) Nazzareno Cannella et al.   NEUROPSYCHOPHARMACOLOGY

A Role for a Specific Cholesterol Interaction in Stabilizing the Apo Configuration of the Human A 2A Adenosine Receptor

(2009) Edward Lyman et al.   STRUCTURE

A facile and practical one-pot ‘catch and release’ synthesis of substituted guanidines

(2009) Ying Wang et al.   TETRAHEDRON LETTERS

Identifying structural features on 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones critical for Neuropeptide S antagonist activity

(2008) Yanan Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Biological Activity of Human Neuropeptide S Analogues Modified in Position 5: Identification of Potent and Pure Neuropeptide S Receptor Antagonists

(2008) Remo Guerrini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Pharmacological in Vitro and in Vivo Profile of 3-Oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic Acid 4-Fluoro-benzylamide (SHA 68), a Selective Antagonist of the Neuropeptide S Receptor

(2008) N. Okamura et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Synthesis and Structure of 1,4-Dipiperazino Benzenes:  Chiral Terphenyl-type Peptide Helix Mimetics

(2008) Prantik Maity et al.   ORGANIC LETTERS