selected publications
-
academic article
-
5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Cell.
172.
2018
Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors..
Journal of Medicinal Chemistry.
61.
2018
Conformational transitions of the serotonin 5-HT3 receptor.
Nature.
563.
2018
Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors..
Biochemical Pharmacology.
150.
2018
Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts..
Journal of Medicinal Chemistry.
61.
2018
Functional characterization of α7 nicotinic acetylcholine and NMDA receptor signaling in SH-SY5Y neuroblastoma cells in an ERK phosphorylation assay.
European Journal of Pharmacology.
826.
2018
Functional properties and mechanism of action of PPTQ, an allosteric agonist and low nanomolar positive allosteric modulator at GABAA receptors.
Biochemical Pharmacology.
147.
2018
Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors.
Biochemical Pharmacology.
158.
2018
Profiling of GABAA and GABAB receptor expression in the myometrium of the human uterus.
Life Sciences.
214.
2018
Temporally dissociable effects of ketamine on neuronal discharge and gamma oscillations in rat thalamo-cortical networks.
Neuropharmacology.
137.
2018
18 F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT 2A receptor PET ligands.
Organic & Biomolecular Chemistry.
15.
2017
A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE.
Beilstein Journal of Organic Chemistry.
13.
2017
Detailed characterization of the in vitro pharmacological and pharmacokinetic properties of N-(2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine (25CN-NBOH), a highly selective and brain-penetrant 5-HT2A receptor agonist.
Journal of Pharmacology and Experimental Therapeutics.
361.
2017
Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings.
PLoS ONE.
12.
2017
Probing the putative α7 nAChR/NMDAR complex in human and murine cortex and hippocampus: Different degrees of complex formation in healthy and Alzheimer brain tissue.
PLoS ONE.
12.
2017
5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism..
ACS Chemical Neuroscience.
7.
2016
A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain.
International Journal of Biological Macromolecules.
92.
2016
Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH‐102.
ChemMedChem.
11.
2016
Convergent 18F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands.
Bioorganic & Medicinal Chemistry.
24.
2016
Copper and protons directly activate the zinc-activated channel.
Biochemical Pharmacology.
103.
2016
Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT3 receptors.
Biochemical Pharmacology.
110.
2016
Discovery of α‐Substituted Imidazole‐4‐acetic Acid Analogues as a Novel Class of ρ1 γ‐Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone.
ChemMedChem.
11.
2016
Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study..
Journal of Medicinal Chemistry.
59.
2016
Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism.
PLoS ONE.
11.
2016
New Insight into the Structure–Activity Relationships of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors UCPH‐101 and UCPH‐102.
ChemMedChem.
11.
2016
Oxime Ethers of (E)-11-Isonitrosostrychnine as Highly Potent Glycine Receptor Antagonists..
Journal of Natural Products.
79.
2016
Synthesis and evaluation of 18F-labeled 5-HT2A receptor agonists as PET ligands.
Nuclear Medicine and Biology.
43.
2016
Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues..
Journal of Medicinal Chemistry.
59.
2016
β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences..
Journal of Medicinal Chemistry.
59.
2016
γ-Glutamyl-dipeptides: Easy tools to rapidly probe the stereoelectronic properties of the ionotropic glutamate receptor binding pocket.
Tetrahedron.
72.
2016
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).
Molecular Pharmacology.
88.
2015
Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.
European Journal of Medicinal Chemistry.
102.
2015
Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities.
Current Opinion in Pharmacology.
20.
2015
Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
European Journal of Medicinal Chemistry.
102.
2015
Functional Characterization of the 1,5-Benzodiazepine Clobazam and Its Major Active Metabolite N-Desmethylclobazam at Human GABAA Receptors Expressed in Xenopus laevis Oocytes.
PLoS ONE.
10.
2015
Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3..
ACS Chemical Neuroscience.
6.
2015
Targeting α4β2 Nicotinic Acetylcholine Receptors in Central Nervous System Disorders: Perspectives on Positive Allosteric Modulation as a Therapeutic Approach.
Basic & Clinical Pharmacology & Toxicology.
116.
2015
The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells.
BMC Cancer.
15.
2015
The metabolic impact of β‐hydroxybutyrate on neurotransmission: Reduced glycolysis mediates changes in calcium responses and KATP channel receptor sensitivity.
Journal of Neurochemistry.
132.
2015
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors..
ACS Medicinal Chemistry Letters.
6.
2015
5‐(Piperidin‐4‐yl)‐3‐Hydroxypyrazole: A Novel Scaffold for Probing the Orthosteric γ‐Aminobutyric Acid Type A Receptor Binding Site.
ChemMedChem.
9.
2014
GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization.
Biochemical Pharmacology.
91.
2014
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands..
Journal of Medicinal Chemistry.
57.
2014
Pharmacological characterisation of α6β4⁎ nicotinic acetylcholine receptors assembled from three chimeric α6/α3 subunits in tsA201 cells.
European Journal of Pharmacology.
740.
2014
Probing for Improved Potency and In Vivo Bioavailability of Excitatory Amino Acid Transporter Subtype 1 Inhibitors UCPH-101 and UCPH-102: Design, Synthesis and Pharmacological Evaluation of Substituted 7-Biphenyl Analogs.
Neurochemical Research.
39.
2014
Probing α4βδ GABAA Receptor Heterogeneity: Differential Regional Effects of a Functionally Selective α4β1δ/α4β3δ Receptor Agonist on Tonic and Phasic Inhibition in Rat Brain.
Journal of Neuroscience.
34.
2014
Semisynthetic analogues of toxiferine I and their pharmacological properties at α7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors..
Journal of Natural Products.
77.
2014
Structure–Activity Relationships of Strychnine Analogs at Glycine Receptors.
Chemistry & Biodiversity.
11.
2014
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists..
ACS Medicinal Chemistry Letters.
5.
2014
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABAA receptor agonists.
European Journal of Medicinal Chemistry.
84.
2014
Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors.
European Journal of Medicinal Chemistry.
75.
2014
-
dataset
-
Discovery of 2‑(Imidazo[1,2‑b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective
for the γ‑Hydroxybutyric Acid (GHB) High-Affinity Binding
Sites.
american-chemical-society.
2019
Five-Membered N‑Heterocyclic Scaffolds as Novel Amino Bioisosteres
at γ‑Aminobutyric Acid (GABA) Type A Receptors and GABA
Transporters.
american-chemical-society.
2019
Five-Membered N‑Heterocyclic Scaffolds as Novel Amino Bioisosteres
at γ‑Aminobutyric Acid (GABA) Type A Receptors and GABA
Transporters.
american-chemical-society.
2019
Five-Membered N‑Heterocyclic Scaffolds as Novel Amino Bioisosteres
at γ‑Aminobutyric Acid (GABA) Type A Receptors and GABA
Transporters.
american-chemical-society.
2019
Use of the 4‑Hydroxytriazole
Moiety as a Bioisosteric
Tool in the Development of Ionotropic Glutamate Receptor Ligands.
american-chemical-society.
2019
Chemoenzymatic
Synthesis and Pharmacological Characterization
of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid
Transporter Inhibitors.
american-chemical-society.
2018
Dual Nicotinic
Acetylcholine Receptor α4β2
Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological
Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium
Salts.
american-chemical-society.
2018
Clinicopathologic data of patients and human brain materials..
public-library-of-science.
2017
Pharmacological properties of the drugs used in the present study..
public-library-of-science.
2017
Probing the putative α7 nAChR/NMDAR complex in human and murine cortex and hippocampus: Different degrees of complex formation in healthy and Alzheimer brain tissue.
public-library-of-science.
2017
Sequences of primers used in the RT-qPCR..
public-library-of-science.
2017
GABA concentration-response curve parameters at various receptor subtypes derived from curve-fitting procedures..
public-library-of-science.
2016
Identification
of a New Class of Selective Excitatory
Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a
Structure–Activity Relationship Study.
american-chemical-society.
2016
Tweaking Subtype
Selectivity and Agonist Efficacy at (S)‑2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic
acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
american-chemical-society.
2016
β‑Sulfonamido
Functionalized Aspartate
Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct
Subtype Selectivity Profiles Arising from Subtle Structural Differences.
american-chemical-society.
2016
β‑Sulfonamido
Functionalized Aspartate
Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct
Subtype Selectivity Profiles Arising from Subtle Structural Differences.
american-chemical-society.
2016
Functional properties of GABA at the human α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, α6β2δ and α6β2GABAARs expressed in Xenopus oocytes..
public-library-of-science.
2015
Functional properties of clobazam, N-desmethylclobazam, and clonazepam at the human α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, α6β2δ and α6β2GABAARs expressed in Xenopus oocytes..
public-library-of-science.
2015
Statistical analysis of the functional properties of clobazam, N-desmethylclobazam, and clonazepam at the human α1β2γ2S, α2β2γ2S, α3β2γ2S and α5β2γ2S GABAARs..
public-library-of-science.
2015
-
hide from search
-
Allosteric Modulation of an Excitatory Amino Acid Transporter: The Subtype-Selective Inhibitor UCPH-101 Exerts Sustained Inhibition of EAAT1 through an Intramonomeric Site in the Trimerization Domain.
Journal of Neuroscience.
2013
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters..
Journal of Medicinal Chemistry.
2013
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties..
Journal of Medicinal Chemistry.
2013
Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.
Biochemical Pharmacology.
2013
Elucidation of Molecular Impediments in the α6 Subunit for in Vitro Expression of Functional α6β4* Nicotinic Acetylcholine Receptors.
Journal of Biological Chemistry.
2013
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation..
Journal of Medicinal Chemistry.
2013
Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the Excitatory Amino Acid Transporters (EAATs): improving the potency of a micromolar screening Hit is not truism.
SpringerPlus.
2013
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists..
Journal of Medicinal Chemistry.
2013
Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists..
Journal of Medicinal Chemistry.
2013
The orthosteric GABAA receptor ligand Thio‐4‐PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors.
British Journal of Pharmacology.
2013
Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors.
British Journal of Pharmacology.
2013
Stereoselective Chemoenzymatic Synthesis of the Four Stereoisomers of
l-2-(2-Carboxycyclobutyl)glycine and Pharmacological Characterization at Human Excitatory
Amino Acid Transporter Subtypes 1, 2, and 3.
american-chemical-society.
2006