Affiliation: F. Hoffmann-La Roche Ltd
- Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608)Will P J M Spooren
Novartis Pharma AG, Nervous System Research, WSJ 386 2 45, CH 4002, Basel, Switzerland
Eur J Pharmacol 435:161-70. 2002..In conclusion, all the data presented here indicate that the modified version of the stress-induced hyperthermia-paradigm is a valid and interesting alternative to the classical stress-induced hyperthermia test...
- Metabotropic glutamate receptors: their therapeutic potential in anxietyWill Spooren
CNS Disease Biology Area, pRED, Building 74 3W308, Basel CH 4070, Switzerland
Curr Top Behav Neurosci 2:391-413. 2010....
- Differential effects of diazepam and MPEP on habituation and neuro-behavioural processes in inbred miceAmber R Salomons
Department of Animals in Science and Society, Division of Animal Welfare and Laboratory Animal Science, Faculty of Veterinary Medicine, Utrecht University, Yalelaan 2, 3584 Utrecht, CM, The Netherlands
Behav Brain Funct 8:30. 2012..The present study investigated whether this non-adaptive phenotype of 129P3 mice is primarily based on anxiety-related characteristics...
- Synapse dysfunction in autism: a molecular medicine approach to drug discovery in neurodevelopmental disordersWill Spooren
CNS Research and Early Clinical Development, F Hoffmann La Roche Ltd, Basel, Switzerland
Trends Pharmacol Sci 33:669-84. 2012..Here, we review the opportunities and challenges in drug development for autism and provide insight into the neurobiology of ASDs...
- Insight into the function of Group I and Group II metabotropic glutamate (mGlu) receptors: behavioural characterization and implications for the treatment of CNS disordersW Spooren
F Hoffmann La Roche, Pharma Research Basel Dsicovery Neuroscience, Basel, Switzerland
Behav Pharmacol 14:257-77. 2003....
- Pharmacological and genetic evidence indicates that combined inhibition of NR2A and NR2B subunit containing NMDA receptors is required to disrupt prepulse inhibitionWill Spooren
F Hoffmann La Roche Ltd, Pharma Research Basel Discovery, Building 72 148, 4070 Basel, Switzerland
Psychopharmacology (Berl) 175:99-105. 2004....
- mGlu5 receptor antagonists: a novel class of anxiolytics?Will Spooren
F Hoffmann La Roche, Pharma Research Basel Discovery, Neuroscience, Basel, Switzerland
Drug News Perspect 17:251-7. 2004..Upcoming clinical studies will soon indicate if the preclinical anxiolytic-like efficacy translates into anxiolytic activity in humans...
- Opinion: NK3 receptor antagonists: the next generation of antipsychotics?Will Spooren
Will Spooren and Claus Riemer are at F Hoffmann La Roche, Pharmaceuticals Division, Psychiatry Disease Area, Building 72 148, 4070 Basel, Switzerland
Nat Rev Drug Discov 4:967-75. 2005..Here we discuss the preclinical and clinical evidence that indicates that NK(3) receptor antagonists might represent a new approach to the treatment of schizophrenia and possibly other neuropsychiatric disorders...
- Metabotropic glutamate receptor subtype 5 (mGlu5) and nociceptive function. I. Selective blockade of mGlu5 receptors in models of acute, persistent and chronic painK Walker
Nervous System Research, Novartis Pharma AG, CH 4002, Basle, Switzerland
Neuropharmacology 40:1-9. 2001..In contrast to its effects in models of inflammatory pain, MPEP did not produce significant reversal of mechanical hyperalgesia in a rat model of neuropathic pain...
- Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptorsP Malherbe
Discovery Research CNS, F Hoffmann La Roche Ltd, Basel, Switzerland
Br J Pharmacol 162:929-46. 2011..The objective of this study was to characterize the in vitro and in vivo properties of a novel dual NK₁/NK₃ antagonist, RO4583298 (2-phenyl-N-(pyridin-3-yl)-N-methylisobutyramide derivative)...
- In vitro and in vivo characterization of MPEP, an allosteric modulator of the metabotropic glutamate receptor subtype 5: review articleR Kuhn
Nervous System Research, Novartis, Pharma AG, Basel, Switzerland
Amino Acids 23:207-11. 2002..Recent studies in animal models implicate mGlu(5) receptors as a potentially important therapeutic target particularly for the treatment of pain and anxiety...
- Metabotropic glutamate receptor modulation, translational methods, and biomarkers: relationships with anxietyR E Nordquist
CNS Discovery Research, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, Building 72 148, CH 4070, Basel, Switzerland
Psychopharmacology (Berl) 199:389-402. 2008..This review examines the implications of translational medicine for psychiatric disorders, focusing on metabotropic glutamate (mGlu) receptor biology in anxiety disorders and on anxiety-related biomarkers...
- Cognitive performance in neurokinin 3 receptor knockout miceR E Nordquist
Psychiatry Disease Area, PRBD N, F Hoffmann La Roche, Building 72 148, 4070 Basel, Switzerland
Psychopharmacology (Berl) 198:211-20. 2008..However, research on effects of NK(3) antagonism with animal models has been hindered because of species differences in the receptor between humans, rats, and mice...
- PEGylation enhances the therapeutic potential for insulin-like growth factor I in central nervous system disordersS Saenger
F Hoffmann La Roche Ltd, CNS Pharma Research and Early Development, Basel, Switzerland
Growth Horm IGF Res 21:292-303. 2011..However, insufficient brain delivery to yield beneficial central without peripheral side effects have prevented clinical development in most instances...
- Effects of aripiprazole/OPC-14597 on motor activity, pharmacological models of psychosis, and brain activity in ratsR E Nordquist
CNS Research, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
Neuropharmacology 54:405-16. 2008..Thus, D2 partial agonists may constitute a new group of antipsychotics...
- Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptorsP Malherbe
Discovery Research CNS, F Hoffmann La Roche Ltd, Basel, Switzerland
Br J Pharmacol 154:797-811. 2008..The aim of this study was to characterize derivatives of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one (rac-BHFF) as enhancers of GABAB receptors...
- Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepinesJohn F Cryan
Psychiatry Program, Neuroscience Research, The Novartis Institutes for BioMedical Research WSJ 386 344, Novartis Pharma AG, Basel CH 4002, Switzerland
J Pharmacol Exp Ther 310:952-63. 2004..Overall, the data obtained here suggest that positive modulation of GABAB receptors may serve as a novel therapeutic strategy for the development of anxiolytics, with a superior side effect profile to both baclofen and benzodiazepines...
- Epilepsy, hyperalgesia, impaired memory, and loss of pre- and postsynaptic GABA(B) responses in mice lacking GABA(B(1))V Schuler
Novartis Pharma AG, TA Nervous System, CH 4002, Basel, Switzerland
Neuron 31:47-58. 2001..This demonstrates that GABA(B(1)) is an essential component of pre- and postsynaptic GABA(B) receptors and casts doubt on the existence of proposed receptor subtypes...
- Allosteric modulators for mGlu receptorsF Gasparini
Novartis Institutes for BioMedical Research Basel, Neuroscience Research, WSJ 386 743, Postfach, CH 4002 Basel, Switzerland
Curr Neuropharmacol 5:187-94. 2007..The present review presents the most recent developments in the identification and the characterization of allosteric modulators for the mGlu receptors...
- Effects of metabotropic glutamate receptor 5 on latent inhibition in conditioned taste aversionCarla Bills
Department of Psychological Sciences, University of Missouri, Columbia, MO 65211, USA
Behav Brain Res 157:71-8. 2005..The results found that MPEP attenuates latent inhibition suggesting that the mGlu5 receptor exerts an influence on the processes that underlie the effects of taste pre-exposure on conditioning...