List of works - Dirk Schepmann

2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.

scientific article published on 7 December 2017

A ¹⁸F-labeled fluorobutyl-substituted spirocyclic piperidine derivative as a selective radioligand for PET Imaging of sigma₁ receptors

scientific article published on 25 May 2011

Antinociceptive effects of a new sigma-1 receptor antagonist (N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy)acetamide) in two types of nociception

scientific article published on 10 December 2015

Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of σ1 Receptors in the Brain

scientific article published on 22 January 2014

Asymmetric synthesis of 3-substituted tetrahydro-2-benzazepines.

scientific article published on 9 June 2015

Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists

scientific article published on 28 March 2016

Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position

scientific article

Bicyclic sigma receptor ligands by stereoselective Dieckmann analogous cyclization of piperazinebutyrate.

scientific article published on 16 June 2010

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

scientific article published on 19 July 2017

Characterization of ligand binding to the σ(1) receptor in a human tumor cell line (RPMI 8226) and establishment of a competitive receptor binding assay.

scientific article

Chemical, pharmacological, and in vitro metabolic stability studies on enantiomerically pure RC-33 compounds: promising neuroprotective agents acting as σ₁ receptor agonists

scientific article published on 5 July 2013

Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ1 receptor ligands.

scientific article published on 17 July 2017

Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.

scientific article

Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.

scientific article

Comparative Pharmacological Study of Common NMDA Receptor Open Channel Blockers Regarding Their Affinity and Functional Activity toward GluN2A and GluN2B NMDA Receptors

scientific article published on 27 January 2018

Comparison of in Silico, Electrochemical, in Vitro and in Vivo Metabolism of a Homologous Series of (Radio)fluorinated σ1 Receptor Ligands Designed for Positron Emission Tomography

scientific article published on 28 September 2016

Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.

scientific article published on 3 June 2016

Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols ⬇️

scientific article published on September 24, 2010

Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.

scientific article published on 16 September 2015

Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.

scientific article

Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors

scientific article published in July 2017

Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo

scientific article

Design, Synthesis, Pharmacological Evaluation and Docking Studies of GluN2B-Selective NMDA Receptor Antagonists with a Benzo[7]annulen-7-amine Scaffold

scientific article published on 27 July 2017

Design, Synthesis, and Biological Evaluation of 3-Benzazepin-1-ols as NR2B-Selective NMDA Receptor Antagonists.

scientific article published on May 2010

Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).

scientific article published on 21 December 2009

Design, synthesis and pharmacological evaluation of spirocyclic σ(1) receptor ligands with exocyclic amino moiety (increased distance 1)

scientific article published on 06 April 2011

Design, synthesis and receptor affinity of novel conformationally restricted σ ligands based on the [4.3.3]propellane scaffold.

scientific article published on 27 September 2013

Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation

scientific article published on 09 January 2019

Development of a selective competitive receptor binding assay for the determination of the affinity to NR2B containing NMDA receptors.

scientific article published on 18 April 2010

Development of fluorinated CB(2) receptor agonists for PET studies.

scientific article published on 24 September 2013

Discovery of 2-(3,4-dichlorophenoxy)-N-(2-morpholin-4-ylethyl)acetamide: A selective σ1 receptor ligand with antinociceptive effect

scientific article published on 14 March 2016

Diverse modifications of the 4-methylphenyl moiety of TAK-779 by late-stage Suzuki-Miyaura cross-coupling

scientific article published on 12 November 2013

Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?

scientific article published on 17 March 2017

Enantiomerically Pure 2-Methyltetrahydro-3-benzazepin-1-ols Selectively Blocking GluN2B Subunit Containing N-Methyl-D-aspartate Receptors.

scientific article

Enantioselective synthesis of encecaline-derived potent antimalarial agents.

scientific article published on November 2013

Enantioselective σ1 receptor binding and biotransformation of the spirocyclic PET tracer 1'-benzyl-3-(3-fluoropropyl)-3H-spiro[[2]benzofuran-1,4'-piperidine].

scientific article published on 15 September 2010

Exploitation of an additional hydrophobic pocket of σ1 receptors: late-stage diverse modifications of spirocyclic thiophenes by C-H bond functionalization

scientific article published on 11 October 2011

Expression of σ receptors of human urinary bladder tumor cells (RT-4 cells) and development of a competitive receptor binding assay for the determination of ligand affinity to human σ(2) receptors

scientific article published on 08 April 2011

Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies

scientific article published on 17 April 2018

Frontiers in Medicinal Chemistry 2010: the highlights

scientific article published on 01 June 2010

Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines.

scientific article published on 11 October 2016

GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists derived from 3-benzazepines: synthesis and pharmacological evaluation of benzo[7]annulen-7-amines

scientific article published on 23 February 2014

High-affinity, selective σ ligands of the 1,2,3,4-tetrahydro-1,4'-silaspiro[naphthalene-1,4'-piperidine] type: syntheses, structures, and pharmacological properties

scientific article published on 11 November 2011

Hydroxyalkylation with cyclic sulfates: synthesis of carbazole derived CB(2) ligands with increased polarity.

scientific article published on 18 November 2013

Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation

scientific article published on 18 December 2017

Identification of a potent and selective σ₁ receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells

scientific article published on 14 September 2011

Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents

scientific article published on 08 September 2018

Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands

scientific article published on 26 June 2014

Improving selectivity preserving affinity: New piperidine-4-carboxamide derivatives as effective sigma-1-ligands

scientific article published on 12 December 2014

Isolation and identification of 8-hydroxypraziquantel as a metabolite of the antischistosomal drug praziquantel

scientific article

Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pure σ ligands with 2-benzopyran structure

scientific article published on 30 April 2017

Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance

scientific article published on 21 April 2012

Molecular imaging of σ receptors: synthesis and evaluation of the potent σ1 selective radioligand [18F]fluspidine.

scientific article published on 12 November 2010

Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives.

scientific article published on 9 September 2013

New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes

scientific article published on 17 September 2013

Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring

scientific article published on 14 October 2015

Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand

scientific article published on 16 October 2017

Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies.

scientific article published on 30 January 2018

Oxa-Pictet-Spengler reaction as key step in the synthesis of novel σ receptor ligands with 2-benzopyran structure

scientific article

Oxetanyl Amino Acids for Peptidomimetics.

scientific article published in May 2017

Pd-Catalyzed Direct C–H Bond Functionalization of Spirocyclic σ1 Ligands: Generation of a Pharmacophore Model and Analysis of the Reverse Binding Mode by Docking into a 3D Homology Model of the σ1 Receptor

article

Pharmacological characterization of high-affinity σ1 receptor ligands with spirocyclic thienopyran and thienofuran scaffold

scientific article published on 19 November 2019

Pyridine analogues of spirocyclic σ₁ receptor ligands.

scientific article published on 22 May 2014

Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold

scientific article published on 04 August 2018

Quality and functionality of saffron: quality control, species assortment and affinity of extract and isolated saffron compounds to NMDA and sigma1 (sigma-1) receptors.

scientific article published on 21 May 2008

Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.

scientific article

Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.

scientific article

Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity

scientific article published on 29 July 2017

Replacement of benzylpiperidine moiety by fluorinated phenylalkyl side chains for the development of novel GluN2B receptor ligands

article

Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?

scientific article published on 9 May 2016

Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold

scientific article published on 21 December 2015

Separation and identification of zaleplon metabolites in human urine using capillary electrophoresis with laser-induced fluorescence detection and liquid chromatography-mass spectrometry.

scientific article

Solid-phase organic synthesis of chiral, non-racemic 1,2,4-trisubstituted 1,4-diazepanes with high σ1 receptor affinity.

scientific article

Stereoselective synthesis and pharmacological evaluation of [4.3.3]propellan-8-amines as analogs of adamantanamines.

scientific article

Stereoselective synthesis and structure-affinity relationships of bicyclic kappa receptor agonists.

scientific article published on 12 November 2009

Stereoselective synthesis of conformationally restricted KOR agonists based on the 2,5-diazabicyclo[2.2.2]octane scaffold.

scientific article published in August 2017

Structure-affinity-relationship study of bicyclic sigma receptor ligands.

scientific article published in September 2009

Studies on the enantiomers of RC-33 as neuroprotective agents: isolation, configurational assignment, and preliminary biological profile.

scientific article published on 7 September 2013

Synthesis and NMDA-receptor affinity of 4-oxo-dexoxadrol derivatives

scientific article published on 05 June 2006

Synthesis and Pharmacological Evaluation of Enantiomerically Pure GluN2B Selective NMDA Receptor Antagonists

scientific article published on 04 July 2018

Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety

scientific article published on 12 April 2019

Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold

scientific article published on 22 April 2017

Synthesis and biological evaluation of conformationally restricted σ(1) receptor ligands with 7,9-diazabicyclo[4.2.2]decane scaffold.

scientific article published on 15 October 2010

Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents

scientific article published on 31 August 2016

Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2).

scientific article

Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands.

scientific article

Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.

scientific article published on 5 August 2014

Synthesis and pharmacological evaluation of SNC80 analogues with a bridged piperazine ring

scientific article published on December 2009

Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.

scientific article

Synthesis and pharmacological evaluation of like- and unlike-configured tetrahydro-2-benzazepines with the α-substituted benzyl moiety in the 5-position

scientific article published in August 2014

Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold

scientific article published on 10 January 2019

Synthesis and σ receptor affinity of regioisomeric spirocyclic furopyridines

scientific article published on 30 June 2014

Synthesis of 3-aza[4.4.3]propellanes with high σ1 receptor affinity.

scientific article published on 15 February 2018

Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore

scientific article published on 03 February 2011

Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.

scientific article published on 30 October 2007

Synthesis of conformationally restricted 1,3-dioxanes to analyze the bioactive conformation of 1,3-dioxane-based σ1 and PCP receptor antagonists.

scientific article published on 7 March 2017

Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability

scientific article (publication date: 15 May 2009)

Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines

scientific article published on 12 October 2014

Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety

article

Synthesis, characterization, and metabolism studies of fluspidine enantiomers

scientific article

Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ(1) receptor ligands with a (2-fluoroethyl) residue in 3-position

scientific article published on 11 November 2010

Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.

scientific article published on 27 March 2014

Synthesis, σ receptor affinity, and pharmacological evaluation of 5-phenylsulfanyl- and 5-benzyl-substituted tetrahydro-2-benzazepines

scientific article published on 4 June 2014

Systematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201.

scientific article published on 14 February 2017

Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201

scientific article published on 06 September 2018

The sigma enigma: in vitro/in silico site-directed mutagenesis studies unveil σ1 receptor ligand binding

scientific article published on 28 April 2014

Thiazole-Based σ1 Receptor Ligands: Diversity by Late-Stage C-H Arylation of Thiazoles, Structure-Affinity and Selectivity Relationships, and Molecular Interactions

scientific article published on 24 May 2017

List of works by Dirk Schepmann

2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.

A ¹⁸F-labeled fluorobutyl-substituted spirocyclic piperidine derivative as a selective radioligand for PET Imaging of sigma₁ receptors

Antinociceptive effects of a new sigma-1 receptor antagonist (N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy)acetamide) in two types of nociception

Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of σ1 Receptors in the Brain

Asymmetric synthesis of 3-substituted tetrahydro-2-benzazepines.

Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists

Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position

Bicyclic sigma receptor ligands by stereoselective Dieckmann analogous cyclization of piperazinebutyrate.

Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

Characterization of ligand binding to the σ(1) receptor in a human tumor cell line (RPMI 8226) and establishment of a competitive receptor binding assay.

Chemical, pharmacological, and in vitro metabolic stability studies on enantiomerically pure RC-33 compounds: promising neuroprotective agents acting as σ₁ receptor agonists

Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel σ1 receptor ligands.

Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.

Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.

Comparative Pharmacological Study of Common NMDA Receptor Open Channel Blockers Regarding Their Affinity and Functional Activity toward GluN2A and GluN2B NMDA Receptors

Comparison of in Silico, Electrochemical, in Vitro and in Vivo Metabolism of a Homologous Series of (Radio)fluorinated σ1 Receptor Ligands Designed for Positron Emission Tomography

Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.

Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols ⬇️

Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.

Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.

Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors

Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo

Design, Synthesis, Pharmacological Evaluation and Docking Studies of GluN2B-Selective NMDA Receptor Antagonists with a Benzo[7]annulen-7-amine Scaffold

Design, Synthesis, and Biological Evaluation of 3-Benzazepin-1-ols as NR2B-Selective NMDA Receptor Antagonists.

Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).

Design, synthesis and pharmacological evaluation of spirocyclic σ(1) receptor ligands with exocyclic amino moiety (increased distance 1)

Design, synthesis and receptor affinity of novel conformationally restricted σ ligands based on the [4.3.3]propellane scaffold.

Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation

Development of a selective competitive receptor binding assay for the determination of the affinity to NR2B containing NMDA receptors.

Development of fluorinated CB(2) receptor agonists for PET studies.

Discovery of 2-(3,4-dichlorophenoxy)-N-(2-morpholin-4-ylethyl)acetamide: A selective σ1 receptor ligand with antinociceptive effect

Diverse modifications of the 4-methylphenyl moiety of TAK-779 by late-stage Suzuki-Miyaura cross-coupling

Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?

Enantiomerically Pure 2-Methyltetrahydro-3-benzazepin-1-ols Selectively Blocking GluN2B Subunit Containing N-Methyl-D-aspartate Receptors.

Enantioselective synthesis of encecaline-derived potent antimalarial agents.

Enantioselective σ1 receptor binding and biotransformation of the spirocyclic PET tracer 1'-benzyl-3-(3-fluoropropyl)-3H-spiro[[2]benzofuran-1,4'-piperidine].

Exploitation of an additional hydrophobic pocket of σ1 receptors: late-stage diverse modifications of spirocyclic thiophenes by C-H bond functionalization

Expression of σ receptors of human urinary bladder tumor cells (RT-4 cells) and development of a competitive receptor binding assay for the determination of ligand affinity to human σ(2) receptors

Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies

Frontiers in Medicinal Chemistry 2010: the highlights

Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines.

GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists derived from 3-benzazepines: synthesis and pharmacological evaluation of benzo[7]annulen-7-amines

High-affinity, selective σ ligands of the 1,2,3,4-tetrahydro-1,4'-silaspiro[naphthalene-1,4'-piperidine] type: syntheses, structures, and pharmacological properties

Hydroxyalkylation with cyclic sulfates: synthesis of carbazole derived CB(2) ligands with increased polarity.

Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation

Identification of a potent and selective σ₁ receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells

Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents

Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands

Improving selectivity preserving affinity: New piperidine-4-carboxamide derivatives as effective sigma-1-ligands

Isolation and identification of 8-hydroxypraziquantel as a metabolite of the antischistosomal drug praziquantel

Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pure σ ligands with 2-benzopyran structure

Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance

Molecular imaging of σ receptors: synthesis and evaluation of the potent σ1 selective radioligand [18F]fluspidine.

Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives.

New combination of pharmacophoric elements of potent σ₁ ligands: design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes

Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring

Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand

Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies.

Oxa-Pictet-Spengler reaction as key step in the synthesis of novel σ receptor ligands with 2-benzopyran structure

Oxetanyl Amino Acids for Peptidomimetics.

Pd-Catalyzed Direct C–H Bond Functionalization of Spirocyclic σ1 Ligands: Generation of a Pharmacophore Model and Analysis of the Reverse Binding Mode by Docking into a 3D Homology Model of the σ1 Receptor

Pharmacological characterization of high-affinity σ1 receptor ligands with spirocyclic thienopyran and thienofuran scaffold

Pyridine analogues of spirocyclic σ₁ receptor ligands.

Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold

Quality and functionality of saffron: quality control, species assortment and affinity of extract and isolated saffron compounds to NMDA and sigma1 (sigma-1) receptors.

Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.

Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.

Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity

Replacement of benzylpiperidine moiety by fluorinated phenylalkyl side chains for the development of novel GluN2B receptor ligands

Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?

Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold

Separation and identification of zaleplon metabolites in human urine using capillary electrophoresis with laser-induced fluorescence detection and liquid chromatography-mass spectrometry.

Solid-phase organic synthesis of chiral, non-racemic 1,2,4-trisubstituted 1,4-diazepanes with high σ1 receptor affinity.

Stereoselective synthesis and pharmacological evaluation of [4.3.3]propellan-8-amines as analogs of adamantanamines.

Stereoselective synthesis and structure-affinity relationships of bicyclic kappa receptor agonists.

Stereoselective synthesis of conformationally restricted KOR agonists based on the 2,5-diazabicyclo[2.2.2]octane scaffold.

Structure-affinity-relationship study of bicyclic sigma receptor ligands.

Studies on the enantiomers of RC-33 as neuroprotective agents: isolation, configurational assignment, and preliminary biological profile.

Synthesis and NMDA-receptor affinity of 4-oxo-dexoxadrol derivatives