List of works - Agostino Marrazzo

(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties

scientific article published on 8 December 2017

(+)-Pentazocine attenuates SH-SY5Y cell death, oxidative stress and microglial migration induced by conditioned medium from activated microglia

scientific article published on 2 February 2017

(+)-Pentazocine reduces oxidative stress and apoptosis in microglia following hypoxia/reoxygenation injury.

scientific article published on 18 May 2016

(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ1 antagonist properties and antinociceptive effects

scientific article

4-Nitro-2,1,3-benzoxadiazole derivatives as potential fluorescent sigma receptor probes

scholarly article in RSC Advances, vol. 5 no. 58, 2015

A Pseudouridine Isoxazolidinyl Nucleoside Analogue Structural Analysis: A Morphological Approach

A Structure- and Ligand-Based Virtual Screening of a Database of "Small" Marine Natural Products for the Identification of "Blue" Sigma-2 Receptor Ligands

scientific article published on 14 October 2018

A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect

scientific article

A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through sigma1 receptors

scientific article published on 06 March 2006

Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. A comprehensive systematic review.

scientific article

Anti-amnesic and neuroprotective actions of the sigma-1 receptor agonist (-)-MR22 in rats with selective cholinergic lesion and amyloid infusion.

scientific article published on January 2011

Anti-amnesic properties of (+/-)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats.

scientific article published on 20 February 2009

Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells

scientific article published on 25 October 2016

Antinociceptive profile of LP1, a non-peptide multitarget opioid ligand

scientific article

Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.

scientific article published on 15 October 2010

Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review

scientific article published on 17 February 2018

CCB, a novel specific kappa opioid agonist, which discriminates between opioid and sigma 1 recognition sites.

scientific article published in January 1995

Comprehensive data on a 2D-QSAR model for Heme Oxygenase isoform 1 inhibitors

scientific article published on 21 September 2017

Crystal morphologies and polymorphs in tolbutamide microcrystalline powder

scientific article published on 5 October 2012

Development of a Sigma-2 Receptor affinity filter through a Monte Carlo based QSAR analysis.

scientific article published on 29 May 2017

Effect of MRJF4 on C6 Glioma Cells Proliferation and Migration

scientific article published on 23 August 2016

Effects of a selective sigma 1 antagonist compound on inflammatory pain

scientific article published on 01 February 2014

Evaluation of N-substitution in 6,7-benzomorphan compounds.

scientific article published on 9 June 2010

Exploiting the Power of Stereochemistry in Drug Action: 3-[(2S,6S,11S)-8-Hydroxy-6,11-dimethyl-1,4,5,6-tetrahydro-2,6-methano-3-benzazocin-3(2H)-yl]-N-phenylpropanamide as Potent Sigma-1 Receptor Antagonist

scientific article published on 23 March 2020

Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.

scientific article published on 6 November 2014

Heme Oxygenase Database (HemeOxDB) and QSAR Analysis of Isoform 1 Inhibitors.

scientific article published on 14 July 2017

How molecular interactions affect crystal morphology: The case of haloperidol

scientific article published on 07 June 2011

Hyphenated 3D-QSAR statistical model-scaffold hopping analysis for the identification of potentially potent and selective sigma-2 receptor ligands

scientific article published on 25 August 2017

Identification of potentially potent Heme Oxygenase-1 inhibitors through 3D-QSAR coupled to scaffold hopping analysis.

scientific article

In vivo evaluation of (+)-MR200 as a new selective sigma ligand modulating MOP, DOP and KOP supraspinal analgesia.

scientific article published in December 2005

Intrastriatal administration of sigma ligands inhibits basal dopamine release in vivo.

scientific article published in December 2003

Molecular modeling studies of pseudouridine isoxazolidinyl nucleoside analogues as potential inhibitors of the pseudouridine 5'-monophosphate glycosidase

scientific article

Morphing of Ibogaine: A Successful Attempt into the Search for Sigma-2 Receptor Ligands

scientific article published on 23 January 2019

Nanoencapsulation strategies for the delivery of novel bifunctional antioxidant/σ1 selective ligands.

scientific article published on 12 April 2017

Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity.

scientific article published in August 2005

New Arylethanolimidazole Derivatives as HO-1 Inhibitors with Cytotoxicity against MCF-7 Breast Cancer Cells

scientific article published on 11 March 2020

New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation

scientific article

Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.

scientific article published on 27 November 2017

Novel Sigma-1 receptor antagonists: from opioids to small molecules: what is new?

scientific article published on 29 November 2017

Novel Structural Insight into Inhibitors of Heme Oxygenase-1 (HO-1) by New Imidazole-Based Compounds: Biochemical and In Vitro Anticancer Activity Evaluation

scientific article published on 18 May 2018

Novel imidazole derivatives as heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2) inhibitors and their cytotoxic activity in human-derived cancer cell lines.

scientific article published on 7 April 2015

Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties

scientific article published on 21 April 2011

Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors

scientific article published on 9 February 2018

Preparation and characterization of polymeric micelles loaded with a potential anticancer prodrug

Recent advances in drug discovery of phototherapeutic non-porphyrinic anticancer agents.

scientific article

Repurposing of Human Kinase Inhibitors in Neglected Protozoan Diseases.

scientific article

Role of the Nrf2/HO-1 axis in bronchopulmonary dysplasia and hyperoxic lung injuries.

scientific article published on 30 June 2017

S2RSLDB: a comprehensive manually curated, internet-accessible database of the sigma-2 receptor selective ligands

scientific article (publication date: 2017)

Sigma-1 and Sigma-2 receptor ligands induce apoptosis and autophagy but have opposite effect on cell proliferation in uveal melanoma

scientific article published on 25 July 2017

Sigma-2 receptor ligands QSAR model dataset

scientific article published on 16 June 2017

Specific kappa opioid receptor agonists.

scientific article

Structure–activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents

scientific article published in June 2014

Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectivity for sigma sites

scientific article published on 01 June 2000

Synthesis and Effects on the COX‐1 and COX‐2 Activity in Human Whole Blood ex vivo of Derivatives Containing the [1]Benzothienol‐[3, 2‐d]pyrimidin‐4‐one Heterocyclic System ⬇️

scientific article published on September 1, 2003

Synthesis and Molecular Modelling Studies of New 1,3-Diaryl-5-Oxo-Proline Derivatives as Endothelin Receptor Ligands

scientific article published on 17 April 2020

Synthesis and Structure-Activity Relationships of LP1 Derivatives: N-Methyl-N-phenylethylamino Analogues as Novel MOR Agonists.

scientific article published on 16 March 2018

Synthesis and binding affinity of cis-(-)- and cis-(+)-N-ethyleneamino-N-nordeoxymetazocine and cis-(-)-N-normetazocine analogues at sigma1, sigma2 and kappa opioid receptors.

scientific article

Synthesis and biological evaluation of new benzo-thieno[3,2-d]pyrimidin-4-one sulphonamide thio-derivatives as potential selective cyclooxygenase-2 inhibitors.

scientific article published on 26 April 2013

Synthesis and evaluation of haloperidol metabolite II prodrugs as anticancer agents.

scientific article published on 4 September 2017

Synthesis, physical properties, toxicological studies and bioavailability of L-pyroglutamic and L-glutamic acid esters of paracetamol as potentially useful prodrugs.

scientific article

The antagonistic effect of the sigma 1 receptor ligand (+)-MR200 on persistent pain induced by inflammation.

scientific article

The benzomorphan-based LP1 ligand is a suitable MOR/DOR agonist for chronic pain treatment

scientific article published on 9 November 2011

Tuning Properties for Blood-Brain Barrier Permeation: A Statistics-Based Analysis

scientific article published on 18 December 2019

List of works by Agostino Marrazzo

(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties

(+)-Pentazocine attenuates SH-SY5Y cell death, oxidative stress and microglial migration induced by conditioned medium from activated microglia

(+)-Pentazocine reduces oxidative stress and apoptosis in microglia following hypoxia/reoxygenation injury.

(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ1 antagonist properties and antinociceptive effects

4-Nitro-2,1,3-benzoxadiazole derivatives as potential fluorescent sigma receptor probes

A Pseudouridine Isoxazolidinyl Nucleoside Analogue Structural Analysis: A Morphological Approach

A Structure- and Ligand-Based Virtual Screening of a Database of "Small" Marine Natural Products for the Identification of "Blue" Sigma-2 Receptor Ligands

A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect

A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through sigma1 receptors

Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. A comprehensive systematic review.

Anti-amnesic and neuroprotective actions of the sigma-1 receptor agonist (-)-MR22 in rats with selective cholinergic lesion and amyloid infusion.

Anti-amnesic properties of (+/-)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats.

Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells

Antinociceptive profile of LP1, a non-peptide multitarget opioid ligand

Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.

Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review

CCB, a novel specific kappa opioid agonist, which discriminates between opioid and sigma 1 recognition sites.

Comprehensive data on a 2D-QSAR model for Heme Oxygenase isoform 1 inhibitors

Crystal morphologies and polymorphs in tolbutamide microcrystalline powder

Development of a Sigma-2 Receptor affinity filter through a Monte Carlo based QSAR analysis.

Effect of MRJF4 on C6 Glioma Cells Proliferation and Migration

Effects of a selective sigma 1 antagonist compound on inflammatory pain

Evaluation of N-substitution in 6,7-benzomorphan compounds.

Exploiting the Power of Stereochemistry in Drug Action: 3-[(2S,6S,11S)-8-Hydroxy-6,11-dimethyl-1,4,5,6-tetrahydro-2,6-methano-3-benzazocin-3(2H)-yl]-N-phenylpropanamide as Potent Sigma-1 Receptor Antagonist

Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.

Heme Oxygenase Database (HemeOxDB) and QSAR Analysis of Isoform 1 Inhibitors.

How molecular interactions affect crystal morphology: The case of haloperidol

Hyphenated 3D-QSAR statistical model-scaffold hopping analysis for the identification of potentially potent and selective sigma-2 receptor ligands

Identification of potentially potent Heme Oxygenase-1 inhibitors through 3D-QSAR coupled to scaffold hopping analysis.

In vivo evaluation of (+)-MR200 as a new selective sigma ligand modulating MOP, DOP and KOP supraspinal analgesia.

Intrastriatal administration of sigma ligands inhibits basal dopamine release in vivo.

Molecular modeling studies of pseudouridine isoxazolidinyl nucleoside analogues as potential inhibitors of the pseudouridine 5'-monophosphate glycosidase

Morphing of Ibogaine: A Successful Attempt into the Search for Sigma-2 Receptor Ligands

Nanoencapsulation strategies for the delivery of novel bifunctional antioxidant/σ1 selective ligands.

Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity.

New Arylethanolimidazole Derivatives as HO-1 Inhibitors with Cytotoxicity against MCF-7 Breast Cancer Cells

New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation

Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.

Novel Sigma-1 receptor antagonists: from opioids to small molecules: what is new?

Novel Structural Insight into Inhibitors of Heme Oxygenase-1 (HO-1) by New Imidazole-Based Compounds: Biochemical and In Vitro Anticancer Activity Evaluation

Novel imidazole derivatives as heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2) inhibitors and their cytotoxic activity in human-derived cancer cell lines.

Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties

Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors

Preparation and characterization of polymeric micelles loaded with a potential anticancer prodrug

Recent advances in drug discovery of phototherapeutic non-porphyrinic anticancer agents.

Repurposing of Human Kinase Inhibitors in Neglected Protozoan Diseases.

Role of the Nrf2/HO-1 axis in bronchopulmonary dysplasia and hyperoxic lung injuries.

S2RSLDB: a comprehensive manually curated, internet-accessible database of the sigma-2 receptor selective ligands

Sigma-1 and Sigma-2 receptor ligands induce apoptosis and autophagy but have opposite effect on cell proliferation in uveal melanoma

Sigma-2 receptor ligands QSAR model dataset

Specific kappa opioid receptor agonists.

Structure–activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents

Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectivity for sigma sites

Synthesis and Effects on the COX‐1 and COX‐2 Activity in Human Whole Blood ex vivo of Derivatives Containing the [1]Benzothienol‐[3, 2‐d]pyrimidin‐4‐one Heterocyclic System ⬇️

Synthesis and Molecular Modelling Studies of New 1,3-Diaryl-5-Oxo-Proline Derivatives as Endothelin Receptor Ligands

Synthesis and Structure-Activity Relationships of LP1 Derivatives: N-Methyl-N-phenylethylamino Analogues as Novel MOR Agonists.

Synthesis and binding affinity of cis-(-)- and cis-(+)-N-ethyleneamino-N-nordeoxymetazocine and cis-(-)-N-normetazocine analogues at sigma1, sigma2 and kappa opioid receptors.

Synthesis and biological evaluation of new benzo-thieno[3,2-d]pyrimidin-4-one sulphonamide thio-derivatives as potential selective cyclooxygenase-2 inhibitors.

Synthesis and evaluation of haloperidol metabolite II prodrugs as anticancer agents.

Synthesis, physical properties, toxicological studies and bioavailability of L-pyroglutamic and L-glutamic acid esters of paracetamol as potentially useful prodrugs.

The antagonistic effect of the sigma 1 receptor ligand (+)-MR200 on persistent pain induced by inflammation.

The benzomorphan-based LP1 ligand is a suitable MOR/DOR agonist for chronic pain treatment

Tuning Properties for Blood-Brain Barrier Permeation: A Statistics-Based Analysis