P. Malherbe

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Activation of protein kinase C results in down‐modulation of different recombinant GABAA‐channels

E. Sigel, R. Baur, P. Malherbe, 1991, FEBS letters.

Human catechol-O-methyltransferase: cloning and expression of the membrane-associated form.

Z Dembic, P. Malherbe, B. Bertocci, 1991, Proceedings of the National Academy of Sciences of the United States of America.

Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine.

P. Malherbe, C. Kratzeisen, Pari Malherbe, 2003, Molecular pharmacology.

Protein kinase C transiently activated heteromeric N-methyl-D-aspartate receptor channels independent of the phosphorylatable C-terminal splice domain and of consensus phosphorylation sites.

E. Sigel, R. Baur, P. Malherbe, 1994, The Journal of biological chemistry.

Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site

J. Kemp, J. Kew, P. Malherbe, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Mutational Analysis and Molecular Modeling of the Allosteric Binding Site of a Novel, Selective, Noncompetitive Antagonist of the Metabotropic Glutamate 1 Receptor*

J. Kew, G. Adam, P. Malherbe, 2003, The Journal of Biological Chemistry.

Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP

Martin Stahl, Andreas Mühlemann, P. Gerber, 2006, Journal of neurochemistry.

G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a survey.

Rainer E. Martin, W. Guba, J. Slack, 2011, Current topics in medicinal chemistry.

Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity

Jens-Uwe Peters, Richard H. P. Porter, W. Spooren, 2005, Journal of Pharmacology and Experimental Therapeutics.

Characterization of [3H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using Semliki Forest virus vectors

T. Woltering, G. Adam, P. Malherbe, 2000, Neuropharmacology.

GABAA receptor: subunit expression in Xenopus oocytes and localization of receptor mRNAs in rat brain

A. Draguhn, P. Malherbe, H. Möhler, 1989 .

The effect of subunit composition of rat brain GABAA receptors on channel function

Gerhard Trube, Erwin Sigel, E. Sigel, 1990, Neuron.

Pharmacological and Electrophysiological Properties of Recombinant GABAA Receptors Comprising the α3, β1 and γ2 Subunits

K. H. Backus, P. Malherbe, P. Pflimlin, 1992 .

The γ3‐subunit of the GABAA‐receptor confers sensitivity to benzodiazepine receptor ligands

E. Sigel, P. Malherbe, F. Knoflach, 1991 .

The rat β1 ‐subunit of the GABAA receptor forms a picrotoxin‐sensitive anion channel open in the absence of GABA

E. Sigel, R. Baur, P. Malherbe, 1989, FEBS letters.

Lazabemide for the treatment of Alzheimer's disease: rationale and therapeutic perspectives.

P. Malherbe, A. Cesura, E. Borroni, 1999, Advances in neurology.

Identification of a mitochondrial form of kynurenine aminotransferase/glutamine transaminase K from rat brain

P. Malherbe, A. Cesura, C. Köhler, 1995, FEBS letters.

Point mutations affecting antagonist affinity and agonist dependent gating of GABAA receptor channels.

E. Sigel, R. Baur, P. Malherbe, 1992, The EMBO journal.

Inhibition of alcohol self-administration by positive allosteric modulators of the GABAB receptor in rats: lack of tolerance and potentiation of baclofen

G. Gessa, P. Malherbe, F. Corelli, 2014, Psychopharmacology.

Dual Hypocretin Receptor Antagonism Is More Effective for Sleep Promotion than Antagonism of Either Receptor Alone

Stephen R. Morairty, P. Malherbe, J. Moreau, 2012, PloS one.

Expression and characterization of human beta-secretase candidates metalloendopeptidase MP78 and cathepsin D in beta APP-overexpressing cells.

P. Malherbe, A. Thompson, G. Huber, 1997, Brain research. Molecular brain research.

Characterization of (R,S)‐5,7‐di‐tert‐butyl‐3‐hydroxy‐3‐trifluoromethyl‐3H‐benzofuran‐2‐one as a positive allosteric modulator of GABAB receptors

W. Spooren, E. Prinssen, A. Sleight, 2008, British journal of pharmacology.

Molecular neuroanatomy of human monoamine oxidases A and B revealed by quantitative enzyme radioautography and in situ hybridization histochemistry

P. Malherbe, J. Shih, J. Saura, 1996, Neuroscience.

cDNA cloning of a novel secreted isoform of the human receptor for advanced glycation end products and characterization of cells co-expressing cell-surface scavenger receptors and Swedish mutant amyloid precursor protein.

P. Malherbe, C. Diener, J. Richards, 1999, Brain research. Molecular brain research.

Functional monoclonal antibody acts as a biased agonist by inducing internalization of metabotropic glutamate receptor 7

P. Malherbe, B. Bohrmann, H. Matile, 2012, British journal of pharmacology.

GABAA-receptor subunits: functional expression and gene localisation.

A. Draguhn, E. Sigel, P. Malherbe, 1990, Advances in biochemical psychopharmacology.

Biochemical and behavioural characterization of EMPA, a novel high‐affinity, selective antagonist for the OX2 receptor

E. Pinard, P. Malherbe, J. Moreau, 2009, British journal of pharmacology.

Biochemical and Electrophysiological Characterization of Almorexant, a Dual Orexin 1 Receptor (OX1)/Orexin 2 Receptor (OX2) Antagonist: Comparison with Selective OX1 and OX2 Antagonists

E. Pinard, P. Malherbe, F. Knoflach, 2009, Molecular Pharmacology.

Mapping the Binding Pocket of Dual Antagonist Almorexant to Human Orexin 1 and Orexin 2 Receptors: Comparison with the Selective OX 1 Antagonist SB-674042 and the Selective OX 2 Antagonist N -Ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-

C. Bissantz, P. Malherbe, C. Kratzeisen, 2010 .

Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo.

P. Malherbe, Gavin Kilpatrick, C. Kratzeisen, 2001, The Journal of pharmacology and experimental therapeutics.

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.

C. Bissantz, P. Malherbe, C. Kratzeisen, 2009, Journal of medicinal chemistry.

Cloning and functional expression of human kynurenine 3‐monooxygenase

P. Malherbe, C. Broger, A. Cesura, 1997, FEBS letters.

Effect of the umami peptides on the ligand binding and function of rat mGlu4a receptor might implicate this receptor in the monosodium glutamate taste transduction

P. Malherbe, K. Lundstrom, V. Mutel, 1999, British journal of pharmacology.

Differential regulation of indoleamine 2,3-dioxygenase expression by nitric oxide and inflammatory mediators in IFN-gamma-activated murine macrophages and microglial cells.

P. Ricciardi-Castagnoli, P. Malherbe, A. Cesura, 1997, Journal of immunology.

Stoichiometry of a recombinant GABAA receptor deduced from mutation-induced rectification.

K. H. Backus, J. Benson, P. Malherbe, 1993, Neuroreport.

The positive allosteric GABAB receptor modulator rac-BHFF enhances baclofen-mediated analgesia in neuropathic mice

William T. Ralvenius, P. Malherbe, Khaled Zemoura, 2016, Neuropharmacology.

Localization of GABAA receptor subunit mRNAs in the rat locus coeruleus.

P. Malherbe, J. Richards, J. M. Luque, 1994, Brain research. Molecular brain research.

Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro.

J. Kemp, J. Kew, P. Malherbe, 1997, The Journal of pharmacology and experimental therapeutics.

In situ hybridization histochemistry reveals a diversity of GABAA receptor subunit mRNAs in neurons of the rat spinal cord and dorsal root ganglia

P. Malherbe, E. Persohn, J. Richards, 1991, Neuroscience.

Functional expression and sites of gene transcription of a novel α subunit of the GABAA receptor in rat brain

E. Sigel, R. Baur, P. Malherbe, 1990 .

Functional expression and sites of gene transcription of a novel alpha subunit of the GABAA receptor in rat brain.

E. Sigel, R. Baur, P. Malherbe, 1990, FEBS letters.

Identification and characterization of a novel splice variant of the metabotropic glutamate receptor 5 gene in human hippocampus and cerebellum.

J. Kemp, R. Faull, J. Kew, 2002, Brain research. Molecular brain research.

Cloning and Functional Expression of a Soluble Form of Kynurenine/α -Aminoadipate Aminotransferase from Rat Kidney *

P. Malherbe, C. Broger, A. Cesura, 1995, The Journal of Biological Chemistry.

Cloning and Characterization of a Soluble Kynurenine Aminotransferase from Rat Brain: Identity with Kidney Cysteine Conjugate β‐Lyase

P. Malherbe, A. Cesura, C. Köhler, 1995 .

Localization of NMDA receptor subunit mRNAs in the rat locus coeruleus.

P. Malherbe, J. Richards, J. M. Luque, 1994, Brain research. Molecular brain research.

The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration.

G. Gessa, P. Malherbe, P. Maccioni, 2010, Drug and alcohol dependence.

An Automated System for the Analysis of G Protein-Coupled Receptor Transmembrane Binding Pockets: Alignment, Receptor-Based Pharmacophores, and Their Application

Martin Ebeling, Martin Stahl, Paul R. Gerber, 2005, J. Chem. Inf. Model..

Monoamine oxidases: from brain maps to physiology and transgenics to pathophysiology.

P. Malherbe, E. Borroni, A. Cesura, 1998, Journal of neural transmission. Supplementum.

Lack of β-Amyloidosis in transgenic mice expressing low levels of familial Alzheimer's disease missense mutations

P. Malherbe, H. Bluethmann, J. Richards, 1996, Neurobiology of Aging.

PS2APP Transgenic Mice, Coexpressing hPS2mut and hAPPswe, Show Age-Related Cognitive Deficits Associated with Discrete Brain Amyloid Deposition and Inflammation

J. Kemp, J. Kew, G. Higgins, 2003, The Journal of Neuroscience.

Identification of Critical Residues in the Amino Terminal Domain of the Human NR2B Subunit Involved in the RO 25-6981 Binding Pocket

J. Kemp, J. Kew, P. Malherbe, 2003, Journal of Pharmacology and Experimental Therapeutics.

Pharmacological Characterization of Ro 63-1908 (1-[2-(4-Hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a Novel Subtype-SelectiveN-Methyl-d-Aspartate Antagonist

J. Kemp, J. Kew, E. Pinard, 2002, Journal of Pharmacology and Experimental Therapeutics.

Comparative molecular neuroanatomy of cloned GABAA receptor subunits in the rat CNS

P. Malherbe, E. Persohn, J. Richards, 1992, The Journal of comparative neurology.

Subunit Stoichiometry of Oligomeric Membrane Proteins: GABAA Receptors Isolated by Selective Immunoprecipitation from the Cell Surface

E. Sigel, R. Baur, P. Malherbe, 1996, Neuropharmacology.

Opposite effects of Zn on the in vitro binding of [3H]LY354740 to recombinant and native metabotropic glutamate 2 and 3 receptors

S. Nakanishi, P. Malherbe, C. Broger, 2005, Journal of neurochemistry.

Expression of Functional Membrane‐Bound and Soluble Catechol‐O‐Methyltransferase in Escherichia coli and a Mammalian Cell Line

P. Caspers, P. Malherbe, B. Bertocci, 1992, Journal of neurochemistry.

GABAA-receptor expressed from rat brain α- and β-subunit cDNAs displays potentiation by benzodiazepine receptor ligands

A. Draguhn, G. Multhaup, K. Beyreuther, 1990 .

Positive Allosteric Modulation of GABAB Receptors Ameliorates Sensorimotor Gating in Rodent Models

P. Malherbe, R. Frau, M. Bortolato, 2014, CNS neuroscience & therapeutics.

Highly flexible and efficient synthesis of the GABAB enhancer 4-(2-hexylsulfanyl-6-methyl-pyrimidin-4-ylmethyl)-morpholine

P. Malherbe, E. Prinssen, A. Thomas, 2007 .

Efficient One-Pot Synthesis of the GABAB Positive Allosteric Modulator (R,S)-5,7-Di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one

P. Malherbe, A. Thomas, François Grillet, 2008 .

Efficient One‐Pot Synthesis of GABAB Positive Allosteric Modulator (R,S)‐5,7‐Di‐tert‐butyl‐3‐hydroxy‐3‐trifluoromethyl‐3H‐benzofuran‐2‐one.

P. Malherbe, A. Thomas, François Grillet, 2009 .

Characterization of [3H]Quisqualate Binding to Recombinant Rat Metabotropic Glutamate 1a and 5a Receptors and to Rat and Human Brain Sections

R. Faull, G. Adam, P. Malherbe, 2000, Journal of neurochemistry.

Isolation and expression of a cDNA clone encoding human kynureninase.

P. Malherbe, C. Broger, A. Cesura, 1996, European journal of biochemistry.

Characterization of transgenic mice expressing Apolipoprotein E4(C112R) and Apolipoprotein E4(L28P; C112R)

N. Sueoka, W. März, P. Malherbe, 2000, Neuroscience.

Reduction of alcohol intake by the positive allosteric modulator of the GABA(B) receptor, rac-BHFF, in alcohol-preferring rats.

G. Gessa, P. Malherbe, P. Maccioni, 2013, Alcohol.

Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.

R. Faull, P. Malherbe, K. Lundstrom, 1999, Brain research. Molecular brain research.

Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK3 receptor antagonist: Biochemical and electrophysiological characterization

W. Spooren, C. Bissantz, P. Malherbe, 2014, Neuropharmacology.

Evidence that nicotinic alpha(7) receptors are not involved in the hyperlocomotor and rewarding effects of nicotine.

G. Higgins, A. Grottick, P. Malherbe, 2000, The Journal of pharmacology and experimental therapeutics.

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.

C. Bissantz, T. Hoffmann, P. Malherbe, 2012, Journal of medicinal chemistry.

Molecular cloning and functional characterization of human vesicular glutamate transporter 3

P. Malherbe, C. Broger, S. Takamori, 2002, EMBO reports.

Functional characteristics and sites of gene expression of the alpha 1, beta 1, gamma 2-isoform of the rat GABAA receptor

E. Sigel, R. Baur, P. Malherbe, 1990, The Journal of neuroscience : the official journal of the Society for Neuroscience.

Mapping of brain areas containing RNA homologous to cDNAs encoding the alpha and beta subunits of the rat GABAA gamma-aminobutyrate receptor.

P. Malherbe, G. W. Price, J. Richards, 1988, Proceedings of the National Academy of Sciences of the United States of America.

Recombinant GABAA receptor function and ethanol

E. Sigel, R. Baur, P. Malherbe, 1993, FEBS letters.

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

P. Malherbe, T. Ballard, Pari Malherbe, 2011, Expert opinion on therapeutic patents.

Structure-function relationships of mitochondrial monoamine oxidase A and B: chimaeric enzymes and site-directed mutagenesis studies.

P. Malherbe, A. Cesura, M. da Prada, 1998, Journal of neural transmission. Supplementum.

cDNA Cloning and Molecular Characterization of Human Brain Metalloprotease MP100

H. Hauri, P. Malherbe, R. Hochstrasser, 1999 .

Inhibition of alcohol self-administration by positive allosteric modulators of the GABAB receptor in rats: lack of tolerance and potentiation of baclofen

G. Gessa, P. Malherbe, F. Corelli, 2015, Psychopharmacology.

Structure/function relationships of mitochondrial monoamine oxidase A and B chimeric forms.

P. Malherbe, A. Cesura, M. da Prada, 1995, European journal of biochemistry.

Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors.

Andreas Mühlemann, P. Malherbe, N. Ward, 2006, European journal of pharmacology.

Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor.

J. Kemp, G. Adam, P. Malherbe, 2001, Molecular pharmacology.

GABAA-receptors: Structural requirements and sites of gene expression in mammalian brain

A. Draguhn, P. Malherbe, H. Mohler, 1990, Neurochemical Research.

Alternatively spliced isoforms of the N-methyl-d-aspartate receptor subunit 1 are differentially distributed within the rat spinal cord

P. Malherbe, J. Richards, J. M. Luque, 1994, Neuroscience.

Molecular cloning and functional expression of human 3-hydroxyanthranilic-acid dioxygenase.

R. Schwarcz, P. Malherbe, A. Cesura, 1994, The Journal of biological chemistry.

Function of the alpha 1 beta 2 gamma 2S gamma-aminobutyric acid type A receptor is modulated by protein kinase C via multiple phosphorylation sites.

E. Sigel, P. Malherbe, S. Kellenberger, 1992, The Journal of biological chemistry.

Distribution and abundance of metabotropic glutamate receptor subtype 2 in rat brain revealed by [3H]LY354740 binding in vitro and quantitative radioautography: correlation with the sites of synthesis, expression, and agonist stimulation of [35S]GTPgammas binding.

P. Malherbe, V. Mutel, M. Brockhaus, 2005, The Journal of comparative neurology.

Distribution and abundance of metabotropic glutamate receptor subtype 2 in rat brain revealed by [3H]LY354740 binding in vitro and quantitative radioautography: Correlation with the sites of synthesis, expression, and agonist stimulation of [35S]GTPγs binding

P. Malherbe, V. Mutel, M. Brockhaus, 2005 .

Mapping the Binding Pocket of Dual Antagonist Almorexant to Human Orexin 1 and Orexin 2 Receptors: Comparison with the Selective OX1 Antagonist SB-674042 and the Selective OX2 Antagonist N-Ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA)

C. Bissantz, P. Malherbe, C. Kratzeisen, 2010, Molecular Pharmacology.

Pharmacological and Electrophysiological Properties of Recombinant GABAA Receptors Comprising the alpha3, beta1 and gamma2 Subunits.

K. H. Backus, P. Malherbe, P. Pflimlin, 1992, The European journal of neuroscience.

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

W. Spooren, C. Bissantz, P. Malherbe, 2008, Molecular Pharmacology.

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

W. Spooren, T. Hoffmann, P. Malherbe, 2011, British journal of pharmacology.

Mechanisms of release of nucleotides and integration of their action as P2X- and P2Y-receptor activating molecules.

T Kendall Harden, Richard C Boucher, T. K. Harden, 2003, Molecular pharmacology.

Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis.

P. Malherbe, A. Cesura, M. da Prada, 1996, European journal of biochemistry.

Characterisation of wild‐type and mutant forms of human monoamine oxidase A and B expressed in a mammalian cell line

P. Malherbe, A. Cesura, M. da Prada, 1993, FEBS letters.

Full and partial agonism displayed by benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes.

P. Malherbe, F. Knoflach, H. Mohler, 1993, The Journal of pharmacology and experimental therapeutics.

Cloning and characterization of a soluble kynurenine aminotransferase from rat brain: identity with kidney cysteine conjugate beta-lyase.

P. Malherbe, A. Cesura, C. Köhler, 1995, Journal of Neurochemistry.

Regional and cellular distribution of bleomycin hydrolase mRNA in human brain: comparison between Alzheimer's diseased and control brains

R. Faull, P. Malherbe, J. Richards, 2000, Neuroscience Letters.

Molecular Characterisation of Kynurenine Pathway Enzymes

P. Malherbe, C. Broger, M. Heitz, 1996 .

Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site

J. Kemp, J. Kew, P. Malherbe, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Abstract of the 68th Meeting (Spring Meeting) 6–9 March 1990, Heidelberg

A. Konnerth, B. Sakmann, P. Jonas, 1990, Pflügers Archiv.

Point mutations of the alpha 1 beta 2 gamma 2 gamma-aminobutyric acid(A) receptor affecting modulation of the channel by ligands of the benzodiazepine binding site.

E. Sigel, R. Baur, P. Malherbe, 1996, Molecular pharmacology.

The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration.

G. Gessa, P. Malherbe, P. Maccioni, 2010, Drug and alcohol dependence.

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

P. Malherbe, F. Knoflach, T. Ballard, 2011, British journal of pharmacology.