Affiliation: F. Hoffmann-La Roche Ltd
- Trace amine-associated receptors form structurally and functionally distinct subfamilies of novel G protein-coupled receptorsLothar Lindemann
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, CH 4070 Basel, Switzerland
Genomics 85:372-85. 2005..We propose a uniform nomenclature describing this novel GPCR family in all mammalian species as trace-amine-associated receptors (TAARs), which resolves the ambiguities and contradictions of the previous naming...
- Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depressionLothar Lindemann
Roche Pharmaceutical Research and Early Development, Discovery Neuroscience, Neuroscience, Ophthalmology, and Rare Diseases L L, S H S, B K, A B, M V K, M H, E B, E P, W S, J G W, Discovery Chemistry E V, S K, J W, G J, Operations for Neuroscience, Ophthalmology, and Rare Diseases R H P, J L M, Pharmaceutical Sciences A C H, A P, C F, A G, M S, N J P, L P, U N, and Small Molecules Process Research and Synthesis T H, Roche Innovation Center Basel, Basel
J Pharmacol Exp Ther 353:213-33. 2015....
- 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...
- CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitorLothar Lindemann
F Hoffmann La Roche Ltd Pharmaceuticals Division, Discovery Neuroscience, Grenzacherstrasse 124, 4070 Basel, Switzerland
J Pharmacol Exp Ther 339:474-86. 2011..By enabling long-term treatment through a wide age range, CTEP allows the exploration of the full therapeutic potential of mGlu5 inhibitors for indications requiring chronic receptor inhibition...
- A renaissance in trace amines inspired by a novel GPCR familyLothar Lindemann
F Hoffmann La Roche, Pharmaceuticals Division, Discovery Neuroscience, CH 4070 Basel, Switzerland
Trends Pharmacol Sci 26:274-81. 2005..Current research focuses on dissecting their molecular pharmacology and on the identification of endogenous ligands for the apparently TA-insensitive members of this receptor family...
- Chronic metabotropic glutamate receptor 5 inhibition corrects local alterations of brain activity and improves cognitive performance in fragile X miceAubin Michalon
Discovery Neuroscience, F Hoffmann La Roche AG, Pharma Research and Early Development, Basel
Biol Psychiatry 75:189-97. 2014..To better understand the pathophysiology of FXS and the effect of treatment, brain activity was analyzed using functional magnetic resonance imaging in relation to learning and memory performance...
- Chronic pharmacological mGlu5 inhibition corrects fragile X in adult miceAubin Michalon
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche, CH 4070 Basel, Switzerland
Neuron 74:49-56. 2012..It is of great interest how these findings may translate into ongoing clinical research testing mGlu5 inhibitors in FXS patients...
- G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a surveyNicole A Kratochwil
Pharma Research and Early Development, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland and Nutley, New Jersey 07110 1199, USA
Curr Top Med Chem 11:1902-24. 2011..Illustrative examples are taken from the GPCR family class C, metabotropic glutamate receptors 1 and 5 and sweet taste receptors, and from the GPCR class A, e.g. nicotinic acid and 5-hydroxytryptamine 5A receptor...
- Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseasesGeorg Jaeschke
Discovery Chemistry, Therapeutic Modalities, Discovery Neuroscience, Neuroscience, Ophthalmology and Rare Diseases NORD, Communications, Pharmaceutical Sciences, Molecular Design and Chemical Biology, Therapeutic Modalities, Small Molecules Process Research and Synthesis, Therapeutic Modalities, Infections Diseases, and Operations for Neuroscience, Ophthalmology, and Rare Diseases NORD, Innovation Center Basel, Roche Pharmaceutical Research and Early Development, Grenzacherstrasse 124, CH 4070 Basel, Switzerland
J Med Chem 58:1358-71. 2015..Analogue 3 is the first reported mGlu5 NAM with a long half-life in rodents and is therefore an ideal tool compound for chronic studies in mice and rats. ..
- An automated system for the analysis of G protein-coupled receptor transmembrane binding pockets: alignment, receptor-based pharmacophores, and their applicationNicole A Kratochwil
Pharmaceuticals Division, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
J Chem Inf Model 45:1324-36. 2005..The value of the 3D receptor model is demonstrated for a class C GPCR family, the metabotropic glutamate receptors...
- Metabotropic glutamate receptor 5 as drug target for Fragile X syndromeSebastian H Scharf
Roche Pharmaceutical Research and Early Development, Neuroscience, Ophthalmology and Rare Diseases, Roche Innovation Center Basel, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, 4070 Basel, Switzerland
Curr Opin Pharmacol 20:124-34. 2015..Recent clinical trials, however, with two different mGlu5 inhibitors (basimglurant and mavoglurant) showed no therapeutic benefit in FXS patients for reasons as yet unclear. ..
- Drug discovery for autism spectrum disorder: challenges and opportunitiesAnirvan Ghosh
F Hoffmann La Roche, pRED, Pharma Research and Early Development, DTA Neuroscience, Grenzacherstrasse 124, 4070 Basel, Switzerland
Nat Rev Drug Discov 12:777-90. 2013..Here, we propose a conceptual framework for drug discovery in ASD encompassing target identification, drug profiling and considerations for clinical trials in this novel area. ..
- In vitro pharmacological selectivity profile of oseltamivir prodrug (Tamiflu) and active metaboliteLothar Lindemann
Discovery Neuroscience, Pharmaceuticals Division, F Hoffmann La Roche Ltd, Basel, Switzerland
Eur J Pharmacol 628:6-10. 2010..Neuropsychiatric adverse events observed in influenza patients are likely a phenomenon caused by the infection rather than by oseltamivir...
- 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...
- Trace amine-associated receptor 1 modulates dopaminergic activityLothar Lindemann
Pharmaceuticals Division, Central Nervous System Research, Department PRDNP5 CH, Bldg 70 331, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
J Pharmacol Exp Ther 324:948-56. 2008..Taken together, the data reveal TAAR1 as regulator of dopaminergic neurotransmission...