List of works - Marcello Leopoldo

1-Substituted-4-[3-(1,2,3,4-tetrahydro-5- or 7-methoxynaphthalen-1-yl)propyl]piperazines: influence of the N-1 piperazine substituent on 5-HT1A receptor affinity and selectivity versus D2 and alpha1 receptors. Part 6

scientific article published on 01 May 2000

1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5

scientific article published on 01 February 1999

3-(1H-indol-3-yl)-2-[3-(4-nitrophenyl)ureido]propanamide enantiomers with human formyl-peptide receptor agonist activity: molecular modeling of chiral recognition by FPR2

scientific article published on 3 December 2012

4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization

scientific article published on 12 September 2007

5-HT(7) receptor modulators: a medicinal chemistry survey of recent patent literature (2004 - 2009).

scientific article published on June 2010

5-HT1A receptor, an old target for new therapeutic agents

scientific article published on January 2008

5-HT7 receptor activation: procognitive and antiamnesic effects

scientific article published on 31 July 2014

A benzopyrane derivative as a P-glycoprotein stimulator: a potential agent to decrease β-amyloid accumulation in Alzheimer's disease

scientific article

A multireceptorial binding reinvestigation on an extended class of sigma ligands: N-[omega-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards sigma1 and EBP sites

scientific article

A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand

scientific article published in January 2000

ABC transporters in CSCs membranes as a novel target for treating tumor relapse

scientific article

Activatable fluorescent probes: a new concept in optical molecular imaging

scientific article published on January 2012

Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics

scientific article published on 11 March 2015

Activation of 5-HT7 serotonin receptors reverses metabotropic glutamate receptor-mediated synaptic plasticity in wild-type and Fmr1 knockout mice, a model of Fragile X syndrome

scientific article published on 18 July 2012

Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments

scientific article published on 16 May 2013

Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.

scientific article published in June 2015

Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists

scientific article published on 07 October 2019

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.

scientific article published on 6 May 2007

Comparative evaluation of two dye probes in the rat everted gut sac model for unambiguous classification of P-gp substrate and inhibitor

scientific article published on 9 December 2012

Design and Synthesis of New Selective P-gp Substrates and Inhibitors

scientific article

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors

scientific article published on January 2006

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.

scientific article

Design, synthesis, lipophilic properties, and binding affinities of potential ligands in positron emission tomography (PET) for visualization of brain dopamine D4 receptors

scientific article published in February 2014

Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor

scientific article

Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors

scientific article

Determination of 1-aryl-4-propylpiperazine pKa values: the substituent on aryl modulates basicity

scientific article

Determination of dopamine D(4) receptor density in rat striatum using PB12 as a probe

scientific article

Developments in fluorescent probes for receptor research.

scientific article published on 08 April 2009

Differential responses to acute administration of a new 5-HT7-R agonist as a function of adolescent pre-treatment: phMRI and immuno-histochemical study

scientific article published on 16 December 2014

EGFR tyrosine kinase inhibitors and multidrug resistance: perspectives

scientific article published on January 2011

Editorial [Hot Topic “Fluorescent Probes: From Bench to Bedside” (Guest Editors: Enza Lacivita & Marcello Leopoldo)]

scientific article published on 01 January 2012

Emotional and risk seeking behavior after prepuberal subchronic or adult acute stimulation of 5-HT7-Rs in Naples High Excitability rats.

scientific article published on 2 December 2013

First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure

scientific article

GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved?

scientific article published in April 2015

Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors.

scientific article

In vitro and in vivo evaluation of N-{2-[4-(3-Cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[(11) C]methoxybenz-amide, a positron emission tomography (PET) radioligand for dopamine D4 receptors, in rodents

scientific article published in September 2014

Increase of capsaicin-induced trigeminal Fos-like immunoreactivity by 5-HT(7) receptors

scientific article published on November 2011

Interplay between serotonin 5-HT1A and 5-HT7 receptors in depressive disorders

scientific article

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo

scholarly article by Enza Lacivita et al published 26 July 2012 in Journal of Medicinal Chemistry

LP-211 is a brain penetrant selective agonist for the serotonin 5-HT(7) receptor

scientific article

Long-lasting beneficial effects of central serotonin receptor 7 stimulation in female mice modeling Rett syndrome

scientific article

ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth.

scientific article

Microinjection of the 5-HT7 receptor antagonist SB-269970 into the rat brainstem and basal forebrain: site-dependent effects on REM sleep

scientific article

Modulatory effects following subchronic stimulation of brain 5-HT7-R system in mice and rats.

scientific article published on January 2014

Modulatory effects of two novel agonists for serotonin receptor 7 on emotion, motivation and circadian rhythm profiles in mice

scientific article

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand

scientific article published on November 1998

N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands

scientific article published on 13 February 2008

Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters

scientific article

Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2

scientific article published on 13 December 2014

Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity

scientific article

Novel 64Cu Labeled RGD2-BBN Heterotrimers for PET Imaging of Prostate Cancer.

scientific article published on 27 March 2018

Novel agonists for serotonin 5-HT7 receptors reverse metabotropic glutamate receptor-mediated long-term depression in the hippocampus of wild-type and Fmr1 KO mice, a model of Fragile X Syndrome.

scientific article published on 12 March 2015

Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.

scientific article published on 17 September 2013

Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine

scientific article published on August 7, 1992

PET radiotracers for imaging P-glycoprotein: the challenge for early diagnosis in AD.

scientific article published on 31 October 2013

Persistent modification of forebrain networks and metabolism in rats following adolescent exposure to a 5-HT7 receptor agonist

scientific article

Pharmacological stimulation of the brain serotonin receptor 7 as a novel therapeutic approach for Rett syndrome

scientific article published on 9 May 2014

Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp

scientific article published on 5 January 2013

Prepuberal stimulation of 5-HT7-R by LP-211 in a rat model of hyper-activity and attention-deficit: permanent effects on attention, brain amino acids and synaptic markers in the fronto-striatal interface.

scientific article

Selective 5-HT7 receptor agonists LP 44 and LP 211 elicit an analgesic effect on formalin-induced orofacial pain in mice

scientific article published on May 2016

Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview.

scientific article published on January 2014

Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders

scientific article

Serotonin(7) receptors (5-HT(7)Rs) and their ligands.

scientific article

Small and Innovative Molecules as New Strategy to Revert MDR

scientific article

Stimulation of 5-HT7 receptor during adolescence determines its persistent upregulation in adult rat forebrain areas

scientific article

Stimulation of the brain serotonin receptor 7 rescues mitochondrial dysfunction in female mice from two models of Rett syndrome

scientific article

Structural insights into serotonin receptor ligands polypharmacology

scientific article published on 6 April 2018

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.

scientific article

Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.

scientific article published on 6 May 2016

Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4

scientific article published on 01 December 1996

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.

scientific article

Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents

scientific article

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.

scientific article published on December 2002

Structure–Activity Relationships and Therapeutic Potentials of 5-HT7 Receptor Ligands: An Update

scientific article published on 05 June 2018

Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors

scientific article published on February 2004

Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure

scientific article published in December 2009

Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.

scientific article published on February 2003

Synthesis, radiolabeling and in vivo evaluation of [(11)C](R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT(7) receptor

scientific article published on 29 March 2014

Systemic administration and local microinjection into the central nervous system of the 5-HT(7) receptor agonist LP-211 modify the sleep-wake cycle in the rat.

scientific article published on 25 November 2013

Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions

scientific article published on 17 October 2017

The 5-HT7 receptor triggers cerebellar long-term synaptic depression via PKC-MAPK.

scientific article

The Contribution of Formyl Peptide Receptor Dysfunction to the Course of Neuroinflammation: A Potential Role in the Brain Pathology

scientific article published on 01 January 2020

The serotonin receptor 7 promotes neurite outgrowth via ERK and Cdk5 signaling pathways

scientific article published on 16 November 2012

The therapeutic potential of 5-HT1A receptors: a patent review

scientific article published on 13 July 2012

Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

scientific article published on 10 April 2013

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines

scientific article published in December 2001

List of works by Marcello Leopoldo

1-Substituted-4-[3-(1,2,3,4-tetrahydro-5- or 7-methoxynaphthalen-1-yl)propyl]piperazines: influence of the N-1 piperazine substituent on 5-HT1A receptor affinity and selectivity versus D2 and alpha1 receptors. Part 6

1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5

3-(1H-indol-3-yl)-2-[3-(4-nitrophenyl)ureido]propanamide enantiomers with human formyl-peptide receptor agonist activity: molecular modeling of chiral recognition by FPR2

4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization

5-HT(7) receptor modulators: a medicinal chemistry survey of recent patent literature (2004 - 2009).

5-HT1A receptor, an old target for new therapeutic agents

5-HT7 receptor activation: procognitive and antiamnesic effects

A benzopyrane derivative as a P-glycoprotein stimulator: a potential agent to decrease β-amyloid accumulation in Alzheimer's disease

A multireceptorial binding reinvestigation on an extended class of sigma ligands: N-[omega-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards sigma1 and EBP sites

A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand

ABC transporters in CSCs membranes as a novel target for treating tumor relapse

Activatable fluorescent probes: a new concept in optical molecular imaging

Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics

Activation of 5-HT7 serotonin receptors reverses metabotropic glutamate receptor-mediated synaptic plasticity in wild-type and Fmr1 knockout mice, a model of Fragile X syndrome

Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments

Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.

Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.

Comparative evaluation of two dye probes in the rat everted gut sac model for unambiguous classification of P-gp substrate and inhibitor

Design and Synthesis of New Selective P-gp Substrates and Inhibitors

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.

Design, synthesis, lipophilic properties, and binding affinities of potential ligands in positron emission tomography (PET) for visualization of brain dopamine D4 receptors

Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor

Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors

Determination of 1-aryl-4-propylpiperazine pKa values: the substituent on aryl modulates basicity

Determination of dopamine D(4) receptor density in rat striatum using PB12 as a probe

Developments in fluorescent probes for receptor research.

Differential responses to acute administration of a new 5-HT7-R agonist as a function of adolescent pre-treatment: phMRI and immuno-histochemical study

EGFR tyrosine kinase inhibitors and multidrug resistance: perspectives

Editorial [Hot Topic “Fluorescent Probes: From Bench to Bedside” (Guest Editors: Enza Lacivita & Marcello Leopoldo)]

Emotional and risk seeking behavior after prepuberal subchronic or adult acute stimulation of 5-HT7-Rs in Naples High Excitability rats.

First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure

GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved?

Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors.

In vitro and in vivo evaluation of N-{2-[4-(3-Cyanopyridin-2-yl)piperazin-1-yl]ethyl}-3-[(11) C]methoxybenz-amide, a positron emission tomography (PET) radioligand for dopamine D4 receptors, in rodents

Increase of capsaicin-induced trigeminal Fos-like immunoreactivity by 5-HT(7) receptors

Interplay between serotonin 5-HT1A and 5-HT7 receptors in depressive disorders

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo

LP-211 is a brain penetrant selective agonist for the serotonin 5-HT(7) receptor

Long-lasting beneficial effects of central serotonin receptor 7 stimulation in female mice modeling Rett syndrome

ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth.

Microinjection of the 5-HT7 receptor antagonist SB-269970 into the rat brainstem and basal forebrain: site-dependent effects on REM sleep

Modulatory effects following subchronic stimulation of brain 5-HT7-R system in mice and rats.

Modulatory effects of two novel agonists for serotonin receptor 7 on emotion, motivation and circadian rhythm profiles in mice

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand

N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands

Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters

Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2

Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity

Novel 64Cu Labeled RGD2-BBN Heterotrimers for PET Imaging of Prostate Cancer.

Novel agonists for serotonin 5-HT7 receptors reverse metabotropic glutamate receptor-mediated long-term depression in the hippocampus of wild-type and Fmr1 KO mice, a model of Fragile X Syndrome.

Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.

Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine

PET radiotracers for imaging P-glycoprotein: the challenge for early diagnosis in AD.

Persistent modification of forebrain networks and metabolism in rats following adolescent exposure to a 5-HT7 receptor agonist

Pharmacological stimulation of the brain serotonin receptor 7 as a novel therapeutic approach for Rett syndrome

Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp

Prepuberal stimulation of 5-HT7-R by LP-211 in a rat model of hyper-activity and attention-deficit: permanent effects on attention, brain amino acids and synaptic markers in the fronto-striatal interface.

Selective 5-HT7 receptor agonists LP 44 and LP 211 elicit an analgesic effect on formalin-induced orofacial pain in mice

Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview.

Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders

Serotonin(7) receptors (5-HT(7)Rs) and their ligands.

Small and Innovative Molecules as New Strategy to Revert MDR

Stimulation of 5-HT7 receptor during adolescence determines its persistent upregulation in adult rat forebrain areas

Stimulation of the brain serotonin receptor 7 rescues mitochondrial dysfunction in female mice from two models of Rett syndrome

Structural insights into serotonin receptor ligands polypharmacology

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.

Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.

Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.

Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.

Structure–Activity Relationships and Therapeutic Potentials of 5-HT7 Receptor Ligands: An Update

Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors

Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure

Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.

Synthesis, radiolabeling and in vivo evaluation of [(11)C](R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT(7) receptor

Systemic administration and local microinjection into the central nervous system of the 5-HT(7) receptor agonist LP-211 modify the sleep-wake cycle in the rat.