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List of works by Michael Kassiou

A patent review of oxytocin receptor antagonists 2013-2017.

scientific article published on 14 September 2017

A systematic exploration of the effects of flexibility and basicity on sigma (σ) receptor binding in a series of substituted diamines.

scientific article published in October 2016

Acute Prosocial Effects of Oxytocin and Vasopressin When Given Alone or in Combination with 3,4-Methylenedioxymethamphetamine in Rats: Involvement of the V1A Receptor ⬇️

scientific article published on May 16, 2013

Acute and residual effects in adolescent rats resulting from exposure to the novel synthetic cannabinoids AB-PINACA and AB-FUBINACA.

scientific article published in January 2017

Altered proteostasis in aging and heat shock response in C. elegans revealed by analysis of the global and de novo synthesized proteome

scientific article

Amyloid load and translocator protein 18 kDa in APPswePS1-dE9 mice: a longitudinal study.

scientific article published on 16 January 2015

Bio-orthogonal labeling as a tool to visualize and identify newly synthesized proteins in Caenorhabditis elegans

scientific article

Body temperature and cardiac changes induced by peripherally administered oxytocin, vasopressin and the non-peptide oxytocin receptor agonist WAY 267,464: a biotelemetry study in rats.

scientific article

Boron in Drug Discovery: Carboranes as Unique Pharmacophores in Biologically Active Compounds ⬇️

scientific article published on June 30, 2011

Brain inflammation is induced by co-morbidities and risk factors for stroke

scientific article

Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors

Comparative Evaluation of Three TSPO PET Radiotracers in a LPS-Induced Model of Mild Neuroinflammation in Rats

scientific article published on August 2016

Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.

scientific article published on 23 October 2017

Correction to Synthesis of Usnic Acid Derivatives and Evaluation of Their Antiproliferative Activity against Cancer Cells

scientific article published on 17 February 2020

Could (18) F-DPA-714 PET imaging be interesting to use in the early post-stroke period?

scientific article

Cubanes in Medicinal Chemistry

scientific article published on 06 September 2018

DYRK1A in neurodegeneration and cancer: Molecular basis and clinical implications

scientific article published on 17 March 2015

Derivatives of the pyrazolo[1,5-a]pyrimidine acetamide DPA-713 as translocator protein (TSPO) ligands and pro-apoptotic agents in human glioblastoma

scientific article

Detection of Neuroinflammation in a Rat Model of Subarachnoid Hemorrhage Using [18F]DPA-714 PET Imaging

scientific article published on 26 April 2016

Detection of the recently emerged synthetic cannabinoid 5F-MDMB-PICA in 'legal high' products and human urine samples

scientific article

Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination

scientific article published on 15 November 2016

Differential mitochondrial protein interaction profile between human translocator protein and its A147T polymorphism variant

scientific article published on 06 May 2022

Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X7 receptor antagonists.

scientific article

Disinhibition-like behavior in a P301S mutant tau transgenic mouse model of frontotemporal dementia

scientific article published on 10 August 2016

Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135.

scientific article

Erratum: Corrigendum: Bio-orthogonal labeling as a tool to visualize and identify newly synthesized proteins in Caenorhabditis elegans

scholarly article published in Nature Protocols

Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).

scientific article

First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).

scientific article published on 13 October 2015

First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold

scientific article published on 28 August 2019

Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors

scientific article published on 13 December 2015

Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases

scientific article published on 04 January 2019

Identification of the allosteric P2X7 receptor antagonist [11C]SMW139 as a PET tracer of microglial activation.

scientific article

Imaging glial activation in patients with post-treatment Lyme disease symptoms: a pilot study using [C]DPA-713 PET

article

Imaging of Glial Cell Activation and White Matter Integrity in Brains of Active and Recently Retired National Football League Players.

scientific article

In vitro determination of the efficacy of illicit synthetic cannabinoids at CB1 receptors

scientific article published on 10 December 2019

In vivo assessment of neuroinflammation in progressive multiple sclerosis: a proof of concept study with [F]DPA714 PET

scientific article published on 13 November 2018

In vivo markers of inflammatory response in recent-onset schizophrenia: a combined study using [(11)C]DPA-713 PET and analysis of CSF and plasma

scientific article published on 12 April 2016

Increased Expression of Translocator Protein (TSPO) Marks Pro-inflammatory Microglia but Does Not Predict Neurodegeneration

scientific article published on 10 July 2017

Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists

scientific article

Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.

scientific article published on 9 July 2014

Kinase targets in CNS drug discovery.

scientific article published on 8 February 2017

Lack of neuroinflammation in the HIV-1 transgenic rat: an [(18)F]-DPA714 PET imaging study

scientific article

Longitudinal investigation of neuroinflammation and metabolite profiles in the APPswe ×PS1Δe9 transgenic mouse model of Alzheimer's disease

scientific article published on 10 November 2017

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

scientific article published on 31 March 2020

MDMA ('Ecstasy'), oxytocin and vasopressin modulate social preference in rats: A role for handling and oxytocin receptors

scientific article published on 7 October 2016

Mouse models of frontotemporal dementia: A comparison of phenotypes with clinical symptomatology

scientific article published on 11 January 2017

N-substituted 8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes as σ receptor ligands with potential neuroprotective effects.

scientific article

Neuroimaging of translocator protein in patients with systemic lupus erythematosus: a pilot study using [11C]DPA-713 positron emission tomography

scientific article published on 6 July 2016

Neuroinflammation and brain atrophy in former NFL players: An in vivo multimodal imaging pilot study

scientific article

O-GlcNAc Modification Protects against Protein Misfolding and Aggregation in Neurodegenerative Disease

scientific article published on 26 April 2019

Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling

scientific article published on 12 November 2009

Peptides, Peptidomimetics, and Carbohydrate-Peptide Conjugates as Amyloidogenic Aggregation Inhibitors for Alzheimer's Disease

scientific article published on 26 June 2018

Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist.

scientific article

Pharmacological evaluation of [11C]A-84543: An enantioselective ligand for in vivo studies of neuronal nicotinic acetylcholine receptors ⬇️

scientific article published on January 1, 1998

Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X7 receptor antagonists

scientific article published on 04 April 2017

Pharmacology of Cumyl-Carboxamide Synthetic Cannabinoid New Psychoactive Substances (NPS) CUMYL-BICA, CUMYL-PICA, CUMYL-5F-PICA, CUMYL-5F-PINACA, and Their Analogues.

scientific article published on 9 August 2017

Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA.

scientific article

Pharmacology of Valinate and tert-Leucinate Synthetic Cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and Their Analogues

scientific article

Pharmacology of novel small-molecule tubulin inhibitors in glioblastoma cells with enhanced EGFR signalling

scientific article published on 28 October 2015

Promising potential of new generation translocator protein tracers providing enhanced contrast of arthritis imaging by positron emission tomography in a rat model of arthritis

scientific article

Rapid access to N-(indol-2-yl)amides and N-(indol-3-yl)amides as unexplored pharmacophores

scientific article

Regional brain distribution of translocator protein using [(11)C]DPA-713 PET in individuals infected with HIV.

scientific article

Remarkable Enhancement in Boron Uptake Within Glioblastoma Cells With Carboranyl-Indole Carboxamides

Ring-opened aminothienopyridazines as novel tau aggregation inhibitors

scientific article published on 05 May 2017

Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma.

scientific article

Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.

scientific article published on 14 March 2015

Structure-activity relationships of N-substituted 4-(trifluoromethoxy)benzamidines with affinity for GluN2B-containing NMDA receptors

scientific article

Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues

Synthesis and Pharmacological Profiling of the Metabolites of Synthetic Cannabinoid Drugs APICA, STS-135, ADB-PINACA, and 5F-ADB-PINACA.

scientific article published on 2 June 2017

Synthesis and Radiolabelling of Ipratropium and Tiotropium for Use as PET Ligands in the Study of Inhaled Drug Deposition

Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells ⬇️

scientific article published on October 13, 2011

Synthesis and in vitro evaluation of diverse heterocyclic diphenolic compounds as inhibitors of DYRK1A

scientific article published on 28 October 2018

Synthesis and in vitro evaluation of fluorine-18 benzimidazole sulfones as CB2 PET-radioligands

scientific article published on 09 May 2019

Synthesis of Usnic Acid Derivatives and Evaluation of Their Antiproliferative Activity against Cancer Cells

scientific article published on 08 July 2019

TSPO as a target for glioblastoma therapeutics

scientific article published on 03 August 2015

Targeting the Oxytocin System: New Pharmacotherapeutic Approaches

scientific article published on 30 November 2018

The 2-alkyl-2H-indazole regioisomers of synthetic cannabinoids AB-CHMINACA, AB-FUBINACA, AB-PINACA, and 5F-AB-PINACA are possible manufacturing impurities with cannabimimetic activities

scientific article published on 27 April 2016

The Formation of Seven-Membered Heterocycles under Mild Pictet-Spengler Conditions: A Route to Pyrazolo[3,4]benzodiazepines

scientific article published on 13 May 2016

The Polyphenol Altenusin Inhibits in Vitro Fibrillization of Tau and Reduces Induced Tau Pathology in Primary Neurons

scientific article published on 9 January 2017

The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases.

scientific article published on 26 January 2016

The chemistry and pharmacology of synthetic cannabinoid SDB-006 and its regioisomeric fluorinated and methoxylated analogues

scientific article

The development of CNS-active LRRK2 inhibitors using property-directed optimisation.

scientific article published on 9 May 2013

The development of radiotracers for imaging sigma (σ) receptors in the central nervous system (CNS) using positron emission tomography (PET).

scientific article published on March 2013

The first CNS-active carborane: A novel P2X7 receptor antagonist with antidepressant activity.

scientific article published on 03 April 2014

The synthesis and pharmacological evaluation of adamantane-derived indoles: cannabimimetic drugs of abuse

scientific article

The therapeutic potential of α7 nicotinic acetylcholine receptor (α7 nAChR) agonists for the treatment of the cognitive deficits associated with schizophrenia

scientific article published on 05 August 2015

The translocator protein (TSPO): a novel target for cancer chemotherapy.

scientific article published on 18 March 2013

The translocator protein as a drug target in Alzheimer's disease.

scientific article published on April 2014

Translational evaluation of translocator protein as a marker of neuroinflammation in schizophrenia

scientific article published on 17 January 2017

WAY 267,464, a non-peptide oxytocin receptor agonist, impairs social recognition memory in rats through a vasopressin 1A receptor antagonist action.

scientific article published on 13 March 2015

[18F]DPA-714: direct comparison with [11C]PK11195 in a model of cerebral ischemia in rats

scientific article

[18F]DPA-C5yne, a novel fluorine-18-labelled analogue of DPA-714: radiosynthesis and preliminary evaluation as a radiotracer for imaging neuroinflammation with PET.

scientific article published on 24 April 2014

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