B. Frølund

发表

Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs.

A. Schousboe, P. Krogsgaard‐Larsen, P. Wellendorph, 2017, Advances in neurobiology.

Bioisosterically modified dipeptide excitatory amino acid receptor antagonists containing 3-oxygenated isothiazole ring systems.

P. Krogsgaard‐Larsen, J. Jaroszewski, B. Frølund, 1997, Bioorganic & medicinal chemistry.

GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2006, Advances in pharmacology.

Specific GABA(A) agonists and partial agonists.

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2002, Chemical record.

Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements.

G. Ecker, B. Frølund, R. Clausen, 2017, Advances in neurobiology.

GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects.

P. Krogsgaard‐Larsen, B. Frølund, K. Frydenvang, 2000, Current pharmaceutical design.

GABAA receptor partial agonists and antagonists: structure, binding mode, and pharmacology.

U. Kristiansen, P. Krogsgaard‐Larsen, B. Frølund, 2015, Advances in pharmacology.

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

J. Kehler, A. A. Jensen, B. Frølund, 2011, ChemMedChem.

Design, synthesis, and in vitro pharmacology of new radiolabeled gamma-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity gamma-hydroxybutyric acid binding sites.

P. Wellendorph, B. Frølund, R. Clausen, 2010, Journal of medicinal chemistry.

Functional and Pharmacological Aspects of GABA Transporters

A. Schousboe, B. Frølund, R. Clausen, 2006 .

Molecular determinants underlying DS2 activity at δ-containing GABAA receptors

D. Gloriam, P. Wellendorph, B. Frølund, 2021, bioRxiv.

Molecular Determinants Underlying Delta Selective Compound 2 Activity at δ-Containing GABAA Receptors

D. Gloriam, P. Wellendorph, B. Frølund, 2021, Molecular Pharmacology.

Probing the Orthosteric Binding Site of GABAA Receptors with Heterocyclic GABA Carboxylic Acid Bioisosteres

P. Krogsgaard‐Larsen, B. Frølund, R. Bergmann, 2013, Neurochemical Research.

7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.

K. Davidson, D. Sugden, M. Teh, 2007, Bioorganic & medicinal chemistry.

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

J. Kehler, C. Bundgaard, T. Bek, 2016, ChemMedChem.

Developing new 4-PIOL and 4-PHP analogues for photo-inactivation of γ-aminobutyric acid type A receptors.

A. A. Jensen, T. Smart, B. Frølund, 2019, ACS chemical neuroscience.

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.

D. Gloriam, P. Krogsgaard‐Larsen, A. A. Jensen, 2013, Journal of medicinal chemistry.

Discovery and Evaluation of Anti-Fibrinolytic Plasmin Inhibitors Derived from 5-(4-Piperidyl)isoxazol-3-ol (4-PIOL)

Thomas C. Schmidt, Thomas C Schmidt, D. Cosgrove, 2017, J. Chem. Inf. Model..

Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain.

C. Bundgaard, P. Wellendorph, B. Frølund, 2022, Journal of medicinal chemistry.

5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.

T. Liljefors, U. Kristiansen, P. Krogsgaard‐Larsen, 2007, Journal of Medicinal Chemistry.

GABAB antagonists: Enantiopharmacology of 5‐amino‐4‐hydroxy‐2‐methylvaleric acid and X‐ray structure of the eutomer

U. Kristiansen, P. Krogsgaard‐Larsen, B. Frølund, 1995 .

Synthesis and Pharmacological Evaluation of [C-11]4-Methoxy-N-[2-(thiophen-2-yl) imidazo[1,2-a] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the delta-Subunit-Containing gamma-Aminobutyric Acid Type A Receptors

G. Knudsen, T. Ohlsson, T. Schirmeister, 2019 .

Synthesis and Pharmacological Evaluation of [11C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors

G. Knudsen, T. Ohlsson, T. Schirmeister, 2019, ACS omega.

α4βδ GABAA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)

J. Olsen, G. Knudsen, N. Absalom, 2012, Proceedings of the National Academy of Sciences.

Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α1β2δ GABAA receptors.

P. Wellendorph, B. Frølund, M. Damgaard, 2017, European journal of medicinal chemistry.

Positive allosteric modulation of the GHB high-affinity binding site by the GABAA receptor modulator monastrol and the flavonoid catechin.

P. Wellendorph, B. Frølund, K. T. Kongstad, 2014, European journal of pharmacology.

In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1

J. Kehler, C. Bundgaard, P. Wellendorph, 2015, The Journal of Pharmacology and Experimental Therapeutics.

Structure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors.

A. Schousboe, P. Krogsgaard‐Larsen, B. Frølund, 2006, Advances in pharmacology.

GABA(A) receptor ligands and their therapeutic potentials.

T. Liljefors, U. Kristiansen, P. Krogsgaard‐Larsen, 2002, Current topics in medicinal chemistry.

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.

J. Kehler, D. Gloriam, P. Wellendorph, 2019, Journal of medicinal chemistry.

Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs.

David E. Gloriam, J. Kehler, D. Gloriam, 2017, Journal of medicinal chemistry.

Novel Cyclic γ-Hydroxybutyrate (GHB) Analogs with High Affinity and Stereoselectivity of Binding to GHB Sites in Rat Brain

J. Greenwood, P. Wellendorph, B. Frølund, 2005, Journal of Pharmacology and Experimental Therapeutics.

Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter.

C. Bundgaard, P. Wellendorph, B. Frølund, 2017, ACS chemical neuroscience.

GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.

A. Schousboe, P. Krogsgaard‐Larsen, F. Jørgensen, 1994, Journal of medicinal chemistry.

The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction.

A. Clarkson, P. Wellendorph, B. Frølund, 2022, Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.

Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).

T. Liljefors, B. Frølund, T. Balle, 2009, Bioorganic & medicinal chemistry letters.

Synthesis of 3‐Hydroxy‐ and 3‐Carboxy‐Δ2‐isoxazoline Amino Acids and Evaluation of Their Interaction with GABA Receptors and Transporters

A. Pinto, L. Tamborini, P. Conti, 2006 .

Lack of evidence for synaptic high‐affinity γ‐hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+‐dependent SLC neurotransmitter transporters

P. Wellendorph, B. Frølund, Louise Thiesen, 2019, Journal of neurochemistry.

Effects of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazol (exo-THPO) and its N-substituted analogs on GABA transport in cultured neurons and astrocytes and by the four cloned mouse GABA transporters

A. Schousboe, P. Krogsgaard‐Larsen, B. Frølund, 2003, Neurochemistry International.

Inhibitors of gamma-aminobutyric acid transport as experimental tools and therapeutic agents.

P. Krogsgaard‐Larsen, E. Falch, B. Frølund, 1998, Methods in enzymology.

Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites.

C. Bundgaard, G. Knudsen, S. Lehel, 2017, ACS chemical neuroscience.

Structural Determinants for the Mode of Action of the Imidazopyridine DS2 at d-containing g-Aminobutyric Acid Type A (GABAA) Receptors

D. Gloriam, T. Schirmeister, P. Wellendorph, 2020 .

The GABAA Antagonist DPP-4-PIOL Selectively Antagonises Tonic over Phasic GABAergic Currents in Dentate Gyrus Granule Cells

U. Kristiansen, B. Frølund, Kim Boddum, 2014, Neurochemical Research.

Novel Radioiodinated γ-Hydroxybutyric Acid Analogues for Radiolabeling and Photolinking of High-Affinity γ-Hydroxybutyric Acid Binding Sites

G. Knudsen, P. Wellendorph, B. Frølund, 2010, Journal of Pharmacology and Experimental Therapeutics.

GABA and Glutamate Receptor Ligands and their Therapeutic Potential in CNS Disorders

T. Liljefors, J. Greenwood, P. Krogsgaard‐Larsen, 2010 .

Ligands for the GABAA receptor complex

U. Kristiansen, P. Krogsgaard‐Larsen, B. Frølund, 2001 .

GABAA Receptor Agonists, Partial Agonists, and Antagonists

P. Krogsgaard‐Larsen, B. Frølund, B. Ebert, 1997 .

Characterization of GABAA receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors?

B. Frølund, M. Mortensen, Signe í Stórustovu, 2002, British journal of pharmacology.

Structural and molecular aspects of betaine-GABA transporter 1 (BGT1) and its relation to brain function

G. Ecker, A. Schousboe, P. Wellendorph, 2019, Neuropharmacology.

Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues.

Arne Schousboe, A. Schousboe, P. Krogsgaard‐Larsen, 2005, Bioorganic & medicinal chemistry.

Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.

T. Liljefors, U. Kristiansen, P. Krogsgaard‐Larsen, 2002, Journal of medicinal chemistry.

4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.

J. Kehler, T. Liljefors, P. Krogsgaard‐Larsen, 2007, Journal of medicinal chemistry.

Analogues of the low-efficacy partial GABAA agonist 4-PIOL. Syntheses and in vitro pharmacological studies

P. Krogsgaard‐Larsen, B. Frølund, M. Amici, 1991 .

Substituted 4-hydroxy-1,2,3-triazoles: synthesis, characterization and first drug design applications through bioisosteric modulation and scaffold hopping approaches

K. Janda, K. Martina, F. Dosio, 2015 .

Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.

J. Kehler, U. Kristiansen, B. Frølund, 2013, Journal of medicinal chemistry.

Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at -Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.

D. Gloriam, B. Rolando, D. Boschi, 2019, Journal of medicinal chemistry.

Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2005, Journal of medicinal chemistry.

GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain

J. Olsen, J. Kuriyan, D. Kerr, 2021, Proceedings of the National Academy of Sciences.

Development of a Robust Mammalian Cell‐based Assay for Studying Recombinant α4β1/3δ GABAA Receptor Subtypes

K. Madsen, P. Wellendorph, B. Frølund, 2017, Basic & clinical pharmacology & toxicology.

4-Hydroxy-1,2,3-triazole moiety as bioisostere of the carboxylic acid function: a novel scaffold to probe the orthosteric γ-aminobutyric acid receptor binding site.

B. Rolando, D. Boschi, B. Frølund, 2018, European journal of medicinal chemistry.

Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1

S. Shuto, G. Ecker, P. Wellendorph, 2021, Frontiers in Chemistry.

Activation of single heteromeric GABAA receptor ion channels by full and partial agonists

U. Kristiansen, P. Krogsgaard‐Larsen, T. Smart, 2004, The Journal of physiology.

Carbamoylcholine homologs: synthesis and pharmacology at nicotinic acetylcholine receptors.

P. Krogsgaard‐Larsen, E. Falch, I. Mikkelsen, 2004, European journal of pharmacology.

GABAergic control of arteriolar diameter in the rat retina.

J. Mcgeown, T. Curtis, B. Frølund, 2013, Investigative ophthalmology & visual science.

Neuroactive polyamine wasp toxins: nuclear magnetic resonance spectroscopic analysis of the protolytic properties of philanthotoxin-343.

P. Krogsgaard‐Larsen, J. Jaroszewski, B. Frølund, 1996, Journal of medicinal chemistry.

Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2006, Journal of medicinal chemistry.

Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology.

J. Greenwood, P. Krogsgaard‐Larsen, B. Frølund, 2005, Bioorganic & medicinal chemistry.

Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.

U. Kristiansen, P. Krogsgaard‐Larsen, E. Falch, 1995, Journal of medicinal chemistry.

Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT3 receptors.

U. Kristiansen, B. Frølund, P. Ahring, 2016, Biochemical pharmacology.

Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain.

P. Wellendorph, B. Frølund, M. Shehata, 2022, Journal of medicinal chemistry.

New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.

J. Kehler, C. Bundgaard, P. Wellendorph, 2013, Journal of medicinal chemistry.

Novel high-affinity and selective biaromatic 4-substituted gamma-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies.

Hans Bräuner-Osborne, P. Wellendorph, B. Frølund, 2008, Journal of medicinal chemistry.

Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3.

G. Ecker, P. Wellendorph, B. Frølund, 2015, ACS chemical neuroscience.

First Demonstration of a Functional Role for Central Nervous System Betaine/γ-Aminobutyric Acid Transporter (mGAT2) Based on Synergistic Anticonvulsant Action among Inhibitors of mGAT1 and mGAT2

Scott Slough, Arne Schousboe, A. Schousboe, 2005, Journal of Pharmacology and Experimental Therapeutics.

Correlation between Anticonvulsant Activity and Inhibitory Action on Glial γ-Aminobutyric Acid Uptake of the Highly Selective Mouse γ-Aminobutyric Acid Transporter 1 Inhibitor 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and ItsN-Alkylated Analogs

Arne Schousboe, A. Schousboe, P. Krogsgaard‐Larsen, 2002, Journal of Pharmacology and Experimental Therapeutics.

Differential interactions of 5-(4-piperidyl)-3-isoxazolol analogues with insect γ-aminobutyric acid receptors leading to functional selectivity.

Genyan Liu, B. Frølund, F. Ozoe, 2015, Insect biochemistry and molecular biology.

GHB confers neuroprotection by stabilizing the CaMKIIα hub domain

J. Olsen, J. Kuriyan, D. Kerr, 2020, bioRxiv.

Structure-activity relationships of selective GABA uptake inhibitors.

Arne Schousboe, A. Schousboe, J. Greenwood, 2006, Current topics in medicinal chemistry.

Transport of amino acids and GABA analogues via the human proton-coupled amino acid transporter, hPAT1: characterization of conditions for affinity and transport experiments in Caco-2 cells.

B. Larsen, C. Nielsen, M. Larsen, 2008, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists.

E. Nielsen, J. Kastrup, M. Gajhede, 2013, Journal of medicinal chemistry.

Context-Dependent Modulation of GABAAR-Mediated Tonic Currents

D. Bright, T. Smart, B. Frølund, 2016, The Journal of Neuroscience.

Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors

G. Ecker, P. Wellendorph, B. Frølund, 2020, Scientific Reports.

Activity of novel 4-PIOL analogues at human α1β2γ2S GABAA receptors—correlation with hydrophobicity

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2002 .

Designing Poly-agonists for Treatment of Metabolic Diseases: Challenges and Opportunities

K. Strømgaard, B. Frølund, C. Clemmensen, 2019, Drugs.

Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC)

A. Schousboe, P. Krogsgaard‐Larsen, K. Wilcox, 2008, Epilepsy Research.

A novel selective γ-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS

Arne Schousboe, H. Steve White, A. Schousboe, 2006, Neurochemistry International.

Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings

B. Frølund, Anne Steder, O. Schroeder, 2017, PloS one.

GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2004, Biochemical pharmacology.

Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.

P. Krogsgaard‐Larsen, E. Falch, I. Mikkelsen, 2003, Molecular pharmacology.

Phosphinic, phosphonic and seleninic acid bioisosteres of isonipecotic acid as novel and selective GABAC receptor antagonists

J. Kehler, P. Krogsgaard‐Larsen, B. Frølund, 2003, Neurochemistry International.

Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors.

Judith Weber, M. Piel, F. Rösch, 2018, Journal of medicinal chemistry.

The orthosteric GABAA receptor ligand Thio‐4‐PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors

U. Kristiansen, N. O. Dalby, J. Cryan, 2013, British journal of pharmacology.

Design, synthesis and pharmacology of model compounds for indirect elucidation of the topography of AMPA receptor sites

P. Krogsgaard‐Larsen, B. Frølund, U. Madsen, 1993 .

Differences in kinetics of structurally related competitive GABAA receptor antagonists

U. Kristiansen, B. Frølund, H. Vestergaard, 2007, Neuropharmacology.

Potentiating action of propofol at GABAA receptors of retinal bipolar cells.

H. Qian, K. Bruzik, B. Frølund, 2011, Investigative ophthalmology & visual science.

A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.

T. Liljefors, U. Kristiansen, P. Krogsgaard‐Larsen, 2000, Journal of medicinal chemistry.

Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.

C. Bundgaard, U. Kristiansen, P. Wellendorph, 2021, Journal of medicinal chemistry.

Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.

B. Frølund, R. Bergmann, B. Nielsen, 2014, European journal of medicinal chemistry.

Probing the Orthosteric Binding Site of GABAA Receptors with Heterocyclic GABA Carboxylic Acid Bioisosteres

P. Krogsgaard‐Larsen, B. Frølund, R. Bergmann, 2014, Neurochemical Research.

New insights into the GABAA receptor structure and orthosteric ligand binding: Receptor modeling guided by experimental data

J. Mccammon, I. Ivanov, B. Frølund, 2011, Proteins.

Design and synthesis of a new series of 4-alkylated 3-isoxazolol GABAA antagonists

T. Liljefors, U. Kristiansen, P. Krogsgaard‐Larsen, 2003 .

Characterization of the GABAA Receptor Recognition Site Through Ligand Design and Pharmacophore Modeling

T. Liljefors, P. Krogsgaard‐Larsen, B. Frølund, 2004 .

Sex-specific alterations in GABA receptor-mediated responses in laterodorsal tegmentum (LDT) are associated with prenatal exposure to nicotine.

B. Frølund, Jacob Krall, K. Kohlmeier, 2020, Developmental neurobiology.

P. Krogsgaard‐Larsen, B. Frølund, B. Ebert, 2003, Bioorganic & medicinal chemistry.

Stereospecific GABAB Receptor Antagonism

U. Kristiansen, P. Krogsgaard‐Larsen, B. Frølund, 1996 .

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.

Jun O. Liu, B. Frølund, J. V. van Muijlwijk-Koezen, 2015, European journal of medicinal chemistry.

Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology

P. Wellendorph, B. Frølund, A. Marek, 2020 .

Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using 3H-HOCPCA

G. Knudsen, P. Wellendorph, B. Frølund, 2016, Neurochemistry International.

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.

B. Frølund, B. Nielsen, T. Balle, 2013, Journal of medicinal chemistry.

The labeling of unsaturated γ-hydroxybutyric acid by heavy isotopes of hydrogen: iridium complex-mediated H/D exchange by C─H bond activation vs reduction by boro-deuterides/tritides.

B. Frølund, R. Clausen, S. B. Vogensen, 2016, Journal of labelled compounds & radiopharmaceuticals.

Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABAA receptors

C. Bundgaard, U. Kristiansen, D. Gloriam, 2020, Scientific Reports.

Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)

P. Wellendorph, B. Frølund, R. Clausen, 2014, Neurochemical Research.

Novel cyclic gamma-hydroxybutyrate (GHB) analogs with high affinity and stereoselectivity of binding to GHB sites in rat brain.

J. Greenwood, P. Wellendorph, B. Frølund, 2005, The Journal of pharmacology and experimental therapeutics.

Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.

T. Liljefors, B. Frølund, T. Balle, 2008, Journal of medicinal chemistry.

Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.

M. de la Fuente Revenga, B. Frølund, T. Balle, 2015, European journal of medicinal chemistry.

Probing α4βδ GABAA Receptor Heterogeneity: Differential Regional Effects of a Functionally Selective α4β1δ/α4β3δ Receptor Agonist on Tonic and Phasic Inhibition in Rat Brain

N. O. Dalby, P. Krogsgaard‐Larsen, B. Frølund, 2014, The Journal of Neuroscience.

Silencing of spontaneous activity at α4β1/3δ GABAA receptors in hippocampal granule cells reveals different ligand pharmacology

N. O. Dalby, P. Scholze, P. Wellendorph, 2020, British journal of pharmacology.

Kinase activity simultaneously determines the constitutive and the orthosteric gating in α4β1/3δ GABAA receptors in hippocampal granule cells

N. O. Dalby, P. Scholze, P. Wellendorph, 2018, bioRxiv.

Equilibrium binding characteristics of [3H]thiomuscimol

P. Krogsgaard‐Larsen, N. Diemer, B. Frølund, 1999, Neurochemistry International.

David E. Gloriam, D. Gloriam, P. Krogsgaard‐Larsen, 2013, Journal of medicinal chemistry.

Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements.

G. Ecker, B. Frølund, R. Clausen, 2017, Advances in neurobiology.

Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter.

C. Bundgaard, P. Wellendorph, B. Frølund, 2017, ACS chemical neuroscience.

Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)

P. Wellendorph, B. Frølund, R. Clausen, 2014, Neurochemical Research.

Synthesis and receptor binding of 5‐amino[3H]2methyl‐3‐isothiazolol ([3H]thiomuscimol), a specific GABAa agonist photoaffinity label

P. Krogsgaard‐Larsen, B. Frølund, B. Ebert, 1995 .

GABAA agonists: resolution and pharmacology of (+)- and (-)-isoguvacine oxide.

P. Krogsgaard‐Larsen, B. Frølund, L. Jeppesen, 1995, Chirality.

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

J. Kehler, B. Frølund, Charlotte G. Jørgensen, 2011, ChemMedChem.

Pregnenolone sulfate analogues differentially modulate GABAA receptor closed/desensitised states

B. Frølund, M. Mortensen, M. Ernst, 2023, British journal of pharmacology.

AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.

P. Krogsgaard‐Larsen, J. Jaroszewski, B. Frølund, 1997, Journal of medicinal chemistry.

In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1

J. Kehler, C. Bundgaard, P. Wellendorph, 2015, The Journal of Pharmacology and Experimental Therapeutics.

The orthosteric GABAA receptor ligand Thio‐4‐PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors

N. O. Dalby, J. Cryan, B. Frølund, 2013, British journal of pharmacology.

Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine

P. Wellendorph, B. Frølund, F. Bavo, 2023, Medicinal Chemistry Research.

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

J. Kehler, C. Bundgaard, T. Bek, 2016, ChemMedChem.