Synthesis and Characterization of New V1A Antagonist Compounds: The Separation of Four Atropisomeric Stereoisomers

Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder

(2020) Patrick Schnider et al.   JOURNAL OF MEDICINAL CHEMISTRY

Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation

(2020) Francesca Deflorian et al.   Journal of Chemical Information and Modeling

Discovery of New Heterocyclic Ring Systems as Novel and Potent V1A Receptor Antagonists

(2020) Ferenc Baska et al.   ACS Chemical Neuroscience

New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines

(2020) Éva Bozó et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A PHASE 2 RANDOMIZED CONTROLLED TRIAL OF BALOVAPTAN IN PEDIATRIC PARTICIPANTS WITH AUTISM SPECTRUM DISORDER

(2020) Eric Hollander et al.   JOURNAL OF THE AMERICAN ACADEMY OF CHILD AND ADOLESCENT PSYCHIATRY

6.14 PHASE 3 RANDOMIZED CONTROLLED TRIAL OF BALOVAPTAN IN ADULTS WITH AUTISM SPECTRUM DISORDER

(2020) Suma Jacob et al.   JOURNAL OF THE AMERICAN ACADEMY OF CHILD AND ADOLESCENT PSYCHIATRY

A phase 2 clinical trial of a vasopressin V1a receptor antagonist shows improved adaptive behaviors in men with autism spectrum disorder

(2019) Federico Bolognani et al.   Science Translational Medicine

Atropisomerism in medicinal chemistry: challenges and opportunities

(2018) Sean T Toenjes et al.   Future Medicinal Chemistry

Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form

(2017) Hidetsugu Tabata et al.   JOURNAL OF MEDICINAL CHEMISTRY

Determining Inversion Barriers in Atrop- isomers – A Tutorial for Organic Chemists

(2016) Michel Rickhaus et al.   CHIMIA

Prevalence and Characteristics of Autism Spectrum Disorder Among 4-Year-Old Children in the Autism and Developmental Disabilities Monitoring Network

(2016) Deborah L. Christensen et al.   JOURNAL OF DEVELOPMENTAL AND BEHAVIORAL PEDIATRICS

Stereochemistry of N-Benzoyl-5-substituted-1-benzazepines Revisited: Synthesis of the Conformationally Biased Derivatives and Revision of the Reported Structure

(2016) Hidetsugu Tabata et al.   JOURNAL OF ORGANIC CHEMISTRY

A Single Dose, Randomized, Controlled Proof-Of-Mechanism Study of a Novel Vasopressin 1a Receptor Antagonist (RG7713) in High-Functioning Adults with Autism Spectrum Disorder

(2016) Daniel Umbricht et al.   NEUROPSYCHOPHARMACOLOGY

The MM/PBSA and MM/GBSA methods to estimate ligand-binding affinities

(2015) Samuel Genheden et al.   Expert Opinion on Drug Discovery

Vasopressin V1a and V1b receptor modulators: a patent review (2012 – 2014)

(2015) Magdalena J Ślusarz   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery of Highly Selective Brain-Penetrant Vasopressin 1a Antagonists for the Potential Treatment of Autism via a Chemogenomic and Scaffold Hopping Approach

(2015) Hasane Ratni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Jaguar: A high-performance quantum chemistry software program with strengths in life and materials sciences

(2013) Art D. Bochevarov et al.   INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY

Pharmacokinetics and Metabolism of SRX246: A Potent and Selective Vasopressin 1a Antagonist

(2013) Karine M. Fabio et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Atropisomerism in the Vaptan Class of Vasopressin Receptor Ligands: The Active Conformation Recognized by the Receptor

(2011) Hidetsugu Tabata et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist

(2011) William Arbuckle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability

(2011) Patrick S. Johnson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Assessing Atropisomer Axial Chirality in Drug Discovery and Development

(2011) Steven R. LaPlante et al.   JOURNAL OF MEDICINAL CHEMISTRY

Atropisomeric Properties of 7-, 8-, and 9-Membered-Ring Dibenzolactams: Conformation, Thermal Stability, and Chemical Reactivity

(2010) Hidetsugu Tabata et al.   JOURNAL OF ORGANIC CHEMISTRY

Characterization of the V1a antagonist, JNJ-17308616, in rodent models of anxiety-like behavior

(2008) C. J. Bleickardt et al.   PSYCHOPHARMACOLOGY

Vasopressin: Behavioral roles of an “original” neuropeptide

(2007) Heather K. Caldwell et al.   PROGRESS IN NEUROBIOLOGY