List of works - Mariana Spetea

5-Benzyl substituted 14-methoxymetopon, a high affinity μ opioid receptor agonist with potent antinociceptive activity in mice.

scientific article

A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects

scientific article published on 01 September 2018

A ligand-based 3D pharmacophore model for the μ opioid receptor: application to the morphinan class of opioids

scientific article published on 16 November 2010

Affinity profiles of novel delta-receptor selective benzofuran derivatives of non-peptide opioids

scientific article published in September 1998

Alteration in endogenous opioid systems due to chronic inflammatory pain conditions

scientific article published in January 2002

Anti-inflammatory effect of dual nociceptin and opioid receptor agonist, BU08070, in experimental colitis in mice

scientific article published on 21 September 2015

Anti-inflammatory effects of contralateral administration of the kappa-opioid agonist U-50,488H in rats with unilaterally induced adjuvant arthritis

scientific article published on 25 October 2005

Bifunctional peptide-based opioid agonist/nociceptin antagonist ligand for dual treatment of nociceptive and neuropathic pain

scientific article published on 09 December 2016

Binding, pharmacological and immunological profiles of the delta-selective opioid receptor antagonist HS 378.

scientific article published in August 2001

Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides

scholarly article by Charlotte Martin et al published 16 October 2018 in Journal of Medicinal Chemistry

Biological, pharmacological and immunological activities of novel 6-amino-acid-substituted 14-alkoxy-N-methylmorphinans

scholarly article by Elena Guerrieri et al published 2011 in BMC Pharmacology

Bone Reinnervation After Fracture: A Study in the Rat

scientific article published on 01 August 2001

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6

scientific article published on 28 December 2019

Comparison of physicochemical properties and biological activities of opioid morphinans interacting with mu opioid receptors.

scientific article published on 5 November 2008

Contralateral but not systemic administration of the kappa-opioid agonist U-50,488H induces anti-nociception in acute hindpaw inflammation in rats

scientific article

Contralateral, ipsilateral and bilateral treatments with the kappa-opioid receptor agonist U-50,488H in mononeuropathic rats

scientific article

Current κ opioid receptor ligands and discovery of a new molecular scaffold as a κ opioid receptor antagonist using pharmacophore-based virtual screening

scientific article published on January 2013

DAMGO and 6β-glycine substituted 14-O-methyloxymorphone but not morphine show peripheral, preemptive antinociception after systemic administration in a mouse visceral pain model and high intrinsic efficacy in the isolated rat vas deferens

scientific article published on 30 July 2007

Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile

scientific article

Development of Diphenethylamines as Selective Kappa Opioid Receptor Ligands and Their Pharmacological Activities

scientific article published on 02 November 2020

Development of novel N-methyl and N-allyl-substituted oxazolomorphinans and their interaction with opioid receptors.

scientific article

Discovery and Pharmacological Evaluation of a Diphenethylamine Derivative (HS665), a Highly Potent and Selective κ Opioid Receptor Agonist ⬇️

scientific article published on November 7, 2012

Discovery and biological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.

scientific article published on 17 September 2012

Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency

scientific article published in July 2005

Efficacy of systemic HS-198, an analogue of oxymorphone, on cancer pain-related behaviour in mice.

scientific article published on 5 September 2011

Exploring pharmacological activities and signaling of morphinans substituted in position 6 as potent agonists interacting with the μ opioid receptor

scientific article

Functionalization of the carbonyl group in position 6 of morphinan-6-ones. Development of novel 6-amino and 6-guanidino substituted 14-alkoxymorphinans.

scientific article published on January 2013

Highly Potent and Selective New Diphenethylamines Interacting with the κ-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.

scientific article published on 21 August 2017

Identification of novel ligands interacting with kappa opioid receptors

scientific article published on 5 September 2011

In vitro and in vivo pharmacological profile of the 5-benzyl analogue of 14-methoxymetopon, a novel mu opioid analgesic with reduced propensity to alter motor function

scientific article

In vitro binding and signaling profile of the novel mu opioid receptor agonist endomorphin 2 in rat brain membranes

scientific article published in September 1998

In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone

scientific article

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist-neurokinin 1 receptor antagonist chimera

scientific article published on 30 January 2012

In vivo brain GPCR signaling elucidated by phosphoproteomics.

scientific article published in June 2018

Influence of the 14-alkoxy group and the substitution in position 5 in N-methyl-14-alkoxymorphinan-6-ones on in vitro and in vivo pharmacological activities

scientific article

Injectable peptide hydrogels for controlled-release of opioids

Injectable peptide-based hydrogel formulations for the extended in vivo release of opioids

Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line

scientific article published on January 1998

Introduction of a 6-cyano group in 14-oxygenated N-methylmorphinans influences in vitro and in vivo pharmacological activities

scholarly article by Valeria Follia et al published 2011 in BMC Pharmacology

Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat.

scientific article published on 25 November 2006

Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors

scientific article published on 28 January 2022

Mechanistic Understanding of Peptide Analogues, DALDA, [Dmt1]DALDA, and KGOP01, Binding to the mu Opioid Receptor

scientific article published on 29 April 2020

Modulation of basal and stress-induced amygdaloid substance P release by the potent and selective NK1 receptor antagonist L-822429.

scientific article published on 30 July 2008

Molecular Docking, Molecular Dynamics, and Structure-Activity Relationship Explorations of 14-Oxygenated N-Methylmorphinan-6-ones as Potent μ-Opioid Receptor Agonists

scientific article

Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.

scientific article

Non-peptidic delta-opioid receptor antagonists suppress mitogen-induced tryptophan degradation in peripheral blood mononuclear cells in vitro

scientific article

Novel approach to demonstrate high efficacy of mu opioids in the rat vas deferens: a simple model of predictive value.

scientific article published in January 2010

On the Role of Peripheral Sensory and Gut Mu Opioid Receptors: Peripheral Analgesia and Tolerance

scientific article published on 26 May 2020

Opioid peptides and receptors in joint tissues: study in the rat.

scientific article published in June 2006

Opioid receptors and their ligands in the musculoskeletal system and relevance for pain control.

scientific article published on January 2013

Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery

scientific article published on 01 December 2020

Peripheral versus central antinociceptive actions of 6-amino acid-substituted derivatives of 14-O-methyloxymorphone in acute and inflammatory pain in the rat.

scientific article published on 21 September 2004

Peripherally mediated antinociception of the mu-opioid receptor agonist 2-[(4,5alpha-epoxy-3-hydroxy-14beta-methoxy-17-methylmorphinan-6beta-yl)amino]acetic acid (HS-731) after subcutaneous and oral administration in rats with carrageenan-induced hi

scientific article published on 8 December 2005

Pharmacological investigations of N-substituent variation in morphine and oxymorphone: opioid receptor binding, signaling and antinociceptive activity

scientific article

Recent advances in the development of 14-alkoxy substituted morphinans as potent and safer opioid analgesics.

scientific article published on January 2012

Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice.

scientific article

Specific activation of the mu opioid receptor (MOR) by endomorphin 1 and endomorphin 2.

scientific article published in February 2000

Structural determinants of diphenethylamines for interaction with the κ opioid receptor: Synthesis, pharmacology and molecular modeling studies

scientific article

Synthesis and binding characteristics of the highly selective radiolabelled deltorphin analogues containing 2-aminotetralin-2-carboxylic acid in position 3.

scientific article

Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.

scientific article published in November 2002

Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime

scientific article

Synthesis and characterization of thiazolo- and thiazinomorphinans and their intermediate products as novel opioid-active derivatives

scientific article

Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.

scientific article

Synthesis and pharmacological evaluation of [(3)H]HS665, a novel, highly selective radioligand for the kappa opioid receptor.

scientific article published on 24 December 2014

Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions ⬇️

scientific article published on January 1, 2011

Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14-O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives

scholarly article by Mariana Spetea et al published 3 January 2019 in Journal of Medicinal Chemistry

Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists

scientific article published on 20 October 2017

Synthesis, opioid receptor binding profile and SAR studies of 14-alkoxy-substituted indolo- and benzofuromorphinans

The µ opioid receptor and ligands acting at the µ opioid receptor, as therapeutics and potential therapeutics

scientific article published on January 2013

Unveiling 7-Hydroxymitragynine as the Key Active Metabolite of Mitragynine and the Promise for Creating Novel Pain Relievers

scientific article published on 29 May 2019

Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution

scientific article published on 12 November 2012

and Pharmacological Activities of 14--Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice

scientific article published on 31 August 2018

μ Opioid receptor: novel antagonists and structural modeling

scientific article published on 18 February 2016

List of works by Mariana Spetea

5-Benzyl substituted 14-methoxymetopon, a high affinity μ opioid receptor agonist with potent antinociceptive activity in mice.

A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects

A ligand-based 3D pharmacophore model for the μ opioid receptor: application to the morphinan class of opioids

Affinity profiles of novel delta-receptor selective benzofuran derivatives of non-peptide opioids

Alteration in endogenous opioid systems due to chronic inflammatory pain conditions

Anti-inflammatory effect of dual nociceptin and opioid receptor agonist, BU08070, in experimental colitis in mice

Anti-inflammatory effects of contralateral administration of the kappa-opioid agonist U-50,488H in rats with unilaterally induced adjuvant arthritis

Bifunctional peptide-based opioid agonist/nociceptin antagonist ligand for dual treatment of nociceptive and neuropathic pain

Binding, pharmacological and immunological profiles of the delta-selective opioid receptor antagonist HS 378.

Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides

Biological, pharmacological and immunological activities of novel 6-amino-acid-substituted 14-alkoxy-N-methylmorphinans

Bone Reinnervation After Fracture: A Study in the Rat

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-6

Comparison of physicochemical properties and biological activities of opioid morphinans interacting with mu opioid receptors.

Contralateral but not systemic administration of the kappa-opioid agonist U-50,488H induces anti-nociception in acute hindpaw inflammation in rats

Contralateral, ipsilateral and bilateral treatments with the kappa-opioid receptor agonist U-50,488H in mononeuropathic rats

Current κ opioid receptor ligands and discovery of a new molecular scaffold as a κ opioid receptor antagonist using pharmacophore-based virtual screening

DAMGO and 6β-glycine substituted 14-O-methyloxymorphone but not morphine show peripheral, preemptive antinociception after systemic administration in a mouse visceral pain model and high intrinsic efficacy in the isolated rat vas deferens

Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile

Development of Diphenethylamines as Selective Kappa Opioid Receptor Ligands and Their Pharmacological Activities

Development of novel N-methyl and N-allyl-substituted oxazolomorphinans and their interaction with opioid receptors.

Discovery and Pharmacological Evaluation of a Diphenethylamine Derivative (HS665), a Highly Potent and Selective κ Opioid Receptor Agonist ⬇️

Discovery and biological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.

Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency

Efficacy of systemic HS-198, an analogue of oxymorphone, on cancer pain-related behaviour in mice.

Exploring pharmacological activities and signaling of morphinans substituted in position 6 as potent agonists interacting with the μ opioid receptor

Functionalization of the carbonyl group in position 6 of morphinan-6-ones. Development of novel 6-amino and 6-guanidino substituted 14-alkoxymorphinans.

Highly Potent and Selective New Diphenethylamines Interacting with the κ-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.

Identification of novel ligands interacting with kappa opioid receptors

In vitro and in vivo pharmacological profile of the 5-benzyl analogue of 14-methoxymetopon, a novel mu opioid analgesic with reduced propensity to alter motor function

In vitro binding and signaling profile of the novel mu opioid receptor agonist endomorphin 2 in rat brain membranes

In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist-neurokinin 1 receptor antagonist chimera

In vivo brain GPCR signaling elucidated by phosphoproteomics.

Influence of the 14-alkoxy group and the substitution in position 5 in N-methyl-14-alkoxymorphinan-6-ones on in vitro and in vivo pharmacological activities

Injectable peptide hydrogels for controlled-release of opioids

Injectable peptide-based hydrogel formulations for the extended in vivo release of opioids

Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line

Introduction of a 6-cyano group in 14-oxygenated N-methylmorphinans influences in vitro and in vivo pharmacological activities

Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat.

Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors

Mechanistic Understanding of Peptide Analogues, DALDA, [Dmt1]DALDA, and KGOP01, Binding to the mu Opioid Receptor

Modulation of basal and stress-induced amygdaloid substance P release by the potent and selective NK1 receptor antagonist L-822429.

Molecular Docking, Molecular Dynamics, and Structure-Activity Relationship Explorations of 14-Oxygenated N-Methylmorphinan-6-ones as Potent μ-Opioid Receptor Agonists

Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.

Non-peptidic delta-opioid receptor antagonists suppress mitogen-induced tryptophan degradation in peripheral blood mononuclear cells in vitro

Novel approach to demonstrate high efficacy of mu opioids in the rat vas deferens: a simple model of predictive value.

On the Role of Peripheral Sensory and Gut Mu Opioid Receptors: Peripheral Analgesia and Tolerance

Opioid peptides and receptors in joint tissues: study in the rat.

Opioid receptors and their ligands in the musculoskeletal system and relevance for pain control.

Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery

Peripheral versus central antinociceptive actions of 6-amino acid-substituted derivatives of 14-O-methyloxymorphone in acute and inflammatory pain in the rat.

Peripherally mediated antinociception of the mu-opioid receptor agonist 2-[(4,5alpha-epoxy-3-hydroxy-14beta-methoxy-17-methylmorphinan-6beta-yl)amino]acetic acid (HS-731) after subcutaneous and oral administration in rats with carrageenan-induced hi

Pharmacological investigations of N-substituent variation in morphine and oxymorphone: opioid receptor binding, signaling and antinociceptive activity

Recent advances in the development of 14-alkoxy substituted morphinans as potent and safer opioid analgesics.

Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice.

Specific activation of the mu opioid receptor (MOR) by endomorphin 1 and endomorphin 2.

Structural determinants of diphenethylamines for interaction with the κ opioid receptor: Synthesis, pharmacology and molecular modeling studies

Synthesis and binding characteristics of the highly selective radiolabelled deltorphin analogues containing 2-aminotetralin-2-carboxylic acid in position 3.

Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.

Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime

Synthesis and characterization of thiazolo- and thiazinomorphinans and their intermediate products as novel opioid-active derivatives

Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.

Synthesis and pharmacological evaluation of [(3)H]HS665, a novel, highly selective radioligand for the kappa opioid receptor.

Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions ⬇️

Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14-O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives

Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists

Synthesis, opioid receptor binding profile and SAR studies of 14-alkoxy-substituted indolo- and benzofuromorphinans

The µ opioid receptor and ligands acting at the µ opioid receptor, as therapeutics and potential therapeutics

Unveiling 7-Hydroxymitragynine as the Key Active Metabolite of Mitragynine and the Promise for Creating Novel Pain Relievers

Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution

and Pharmacological Activities of 14--Phenylpropyloxymorphone, a Potent Mixed Mu/Delta/Kappa-Opioid Receptor Agonist With Reduced Constipation in Mice

μ Opioid receptor: novel antagonists and structural modeling