Progress in the development of neurokinin 3 modulators for the treatment of schizophrenia: molecule development and clinical progress

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

Pharmacokinetics and central nervous system effects of the novel dual NK1/NK3receptor antagonist GSK1144814 in alcohol-intoxicated volunteers

(2012) Erik T. te Beek et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Identification of a Crucial Amino Acid in the Helix Position 6.51 of Human Tachykinin Neurokinin 1 and 3 Receptors Contributing to the Insurmountable Mode of Antagonism by Dual NK1/NK3 Antagonists

(2012) Caterina Bissantz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the δ-opioid receptor bound to naltrindole

(2012) Sébastien Granier et al.   NATURE

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia

(2011) Maria Pia Catalani et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor

(2011) Hamid R. Hoveyda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a new series of non-peptidic NK3 receptor antagonists

(2011) Karsten Juhl et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tachykinin neurokinin 3 receptor antagonists: a patent review (2005 – 2010)

(2011) Pari Malherbe et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Molecular Modeling of Neurokinin B and Tachykinin NK3Receptor Complex

(2011) Anjali D. Ganjiwale et al.   Journal of Chemical Information and Modeling

Involvement of Neurokinin Receptors in the Control of Pulsatile Luteinizing Hormone Secretion in Rats

(2011) Ken-ichi NORITAKE et al.   JOURNAL OF REPRODUCTION AND DEVELOPMENT

Is there still a future for neurokinin 3 receptor antagonists as potential drugs for the treatment of psychiatric diseases?

(2011) Guy Griebel et al.   PHARMACOLOGY & THERAPEUTICS

Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands

(2010) Jens-Uwe Peters et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists

(2010) Hassen Ratni et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists

(2010) Hui Xiong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Neurokinin B and the hypothalamic regulation of reproduction

(2010) Naomi E. Rance et al.   BRAIN RESEARCH

Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK1 and NK3 receptors

(2010) P Malherbe et al.   BRITISH JOURNAL OF PHARMACOLOGY

Virtual Screening to Identify Novel Antagonists for the G Protein-Coupled NK3Receptor

(2010) Werner J. Geldenhuys et al.   JOURNAL OF MEDICINAL CHEMISTRY

CHARACTERIZATION OF RO4583298 AS A HIGHLY POTENT, DUAL ANTAGONIST WITH IN VIVO ACTIVITY AT TACHYKININ NK1 AND NK3 RECEPTORS

(2010) Pari Malherbe et al.   SCHIZOPHRENIA RESEARCH

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

(2010) B. Wu et al.   SCIENCE

In vitroassessment of metabolic drug–drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P450enzyme identification, inhibition, and induction studies

(2010) Yan Li et al.   XENOBIOTICA

Characterization of behavioral response to amphetamine, tyrosine hydroxylase levels, and dopamine receptor levels in neurokinin 3 receptor knockout mice

(2009) Rebecca E. Nordquist et al.   BEHAVIOURAL PHARMACOLOGY

Tachykinin Receptors as Therapeutic Targets in Stress-Related Disorders

(2009) Karl Ebner et al.   CURRENT PHARMACEUTICAL DESIGN

In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics

(2009) Lee A. Dawson et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Identification of a Critical Residue in the Transmembrane Domain 2 of Tachykinin Neurokinin 3 Receptor Affecting the Dissociation Kinetics and Antagonism Mode of Osanetant (SR 142801) and Piperidine-Based Structures

(2009) Pari Malherbe et al.   JOURNAL OF MEDICINAL CHEMISTRY

New quinoline NK3 receptor antagonists with CNS activity

(2008) Paul W. Smith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel triple neurokinin receptor antagonist CS-003 strongly inhibits neurokinin related responses

(2008) Hiroshi Tsuchida et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Psychomotor and cognitive effects of a single oral dose of talnetant (SB223412) in healthy volunteers compared with placebo or haloperidol

(2008) M. Liem-Moolenaar et al.   JOURNAL OF PSYCHOPHARMACOLOGY

Me-Talnetant and Osanetant Interact within Overlapping but Not Identical Binding Pockets in the Human Tachykinin Neurokinin 3 Receptor Transmembrane Domains

(2008) P. Malherbe et al.   MOLECULAR PHARMACOLOGY

TAC3 and TACR3 mutations in familial hypogonadotropic hypogonadism reveal a key role for Neurokinin B in the central control of reproduction

(2008) A Kemal Topaloglu et al.   NATURE GENETICS

Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412)

(2008) Raúl de la Flor et al.   NEUROPHARMACOLOGY

Localization and function of NK3 subtype tachykinin receptors of layer V pyramidal neurons of the guinea-pig medial prefrontal cortex

(2008) M.A. Simmons et al.   NEUROSCIENCE

Cognitive performance in neurokinin 3 receptor knockout mice

(2008) R. E. Nordquist et al.   PSYCHOPHARMACOLOGY

MAPPING THE BINDING SITE FOR TACHYKININ NK3 RECEPTOR ANTAGONISTS

(2008) Pari Malherbe et al.   SCHIZOPHRENIA RESEARCH