Lista de obras - Helmut Schmidhammer - Dominio Público Uruguay

(-)-N,N'-but-2-ene-1,4-diylbimorphinans.

artículo científico publicado en 1991

14-Methoxymetopon, a highly potent mu opioid agonist, biphasically affects ethanol intake in Sardinian alcohol-preferring rats

artículo científico publicado en 2007

14-Methoxymetopon, a very potent mu-opioid receptor-selective analgesic with an unusual pharmacological profile

artículo científico publicado en 2003

14-methoxymetopon, a potent opioid, induces no respiratory depression, less sedation, and less bradycardia than sufentanil in the dog.

artículo científico publicado en 2000

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

artículo científico publicado en 2008

An opioid agonist with preference for kappa-opioid receptors: (-)-N-cyclopropylmethylmorphinan-6-one.

artículo científico publicado en 1990

Antinociceptive activity of a novel buprenorphine analogue.

artículo científico publicado en 2002

Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist

artículo científico publicado en 2003

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

artículo científico publicado en 2001

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

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

artículo científico publicado en 2008

Cyprodime analogues: synthesis and pharmacological evaluation

scientific article published on 01 January 1990

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

artículo científico publicado en 2007

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

artículo científico publicado en 2012

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

artículo científico publicado en 2011

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

artículo científico publicado en 2012

Effect of novel non-peptidic delta opioid receptor antagonists on human T and B cell activation

artículo científico publicado en 2004

Effects of 14-methoxymetopon, a potent opioid agonist, on the responses to the tail electric stimulation test and plus-maze activity in male rats: neuroendocrine correlates

artículo científico publicado en 2002

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

artículo científico publicado en 2011

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

artículo científico publicado en 2014

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

artículo científico

HS-599: a novel long acting opioid analgesic does not induce place-preference in rats

artículo científico publicado en 2001

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

artículo científico publicado en 2017

Highly potent novel opioid receptor agonist in the 14-alkoxymetopon series.

artículo científico publicado en 1993

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

artículo científico publicado en 2010

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

artículo científico publicado en 2004

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

artículo científico publicado en 2012

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

Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.

artículo científico publicado en 2004

Inverse agonism by Dmt-Tic analogues and HS 378, a naltrindole analogue.

artículo científico publicado en 2000

Involvement of mu- and kappa-, but not delta-, opioid receptors in the peristaltic motor depression caused by endogenous and exogenous opioids in the guinea-pig intestine.

artículo científico publicado en 2002

Lack of regulatory changes of µ-opioid receptors by 14-methoxymetopon treatment in rat brain. Further evidence for functional selectivity

artículo científico publicado en 2013

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

artículo científico publicado en 2006

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

artículo científico publicado en 2022

Mechanistic diversity of the van Leusen reaction applied to 6-ketomorphinans and synthetic potential of the resulting acrylonitrile substructures.

artículo científico publicado en 2005

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

artículo científico publicado en 2008

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

artículo científico publicado en 2017

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

artículo científico publicado en 2010

Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.

artículo científico publicado en 1999

Non-deleterious inhibition of endogenous peroxidase activity (EPA) by cyclopropanone hydrate: a definitive approach

artículo científico publicado en 1989

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

artículo científico publicado en 2008

Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation

artículo científico publicado en 2014

Novel Positive Allosteric Modulators of µ Opioid Receptor-Insight from In Silico and In Vivo Studies

artículo científico publicado en 2020

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

artículo científico publicado en 2010

Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.

artículo científico publicado en 1999

Opioid peptide receptor studies. 9. Identification of a novel non-mu- non-delta-like opioid peptide binding site in rat brain.

artículo científico publicado en 1998

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

artículo científico publicado en 2020

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

artículo científico publicado en 2004

Peripheral μ-opioid receptor mediated inhibition of calcium signaling and action potential-evoked calcium fluorescent transients in primary afferent CGRP nociceptive terminals.

artículo científico publicado en 2015

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

artículo científico publicado en 2005

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

artículo científico publicado en 2014

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

artículo científico publicado en 2012

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

artículo científico publicado en 2017

Separation of binding affinity and intrinsic activity of the potent mu-opioid 14-methoxymetopon.

artículo científico publicado en 2006

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

artículo científico publicado en 2016

Structure-activity relationships of oxygenated morphinans. III. An exploration of the effect of the aromatic oxygen and 6-keto group on antinociceptive activity, receptor affinity, and narcotic antagonism.

artículo científico publicado en 1982

Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 11. 3-Hydroxycyprodime and Analogs: Opioid Antagonist Profile in Comparison to Cyprodime ⬇️

artículo científico publicado el 4 de agosto de 1995

Synthesis and biological evaluation of 14-alkoxymorphinans, V: 6-Deoxyocyprodime, an opioid antagonist with decreased mu receptor selectivity in comparison to cyprodime.

artículo científico publicado en 1991

Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones ⬇️

artículo científico publicado el 1 de diciembre de 1984

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

artículo científico publicado en 2002

Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.

artículo científico publicado en 1989

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

artículo científico publicado en 2004

Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds

artículo científico publicado en 1990

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

artículo científico publicado en 2011

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

artículo científico publicado en 2014

Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions ⬇️

artículo científico publicado el 1 de enero de 2011

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

artículo científico publicado en 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

artículo científico publicado en 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

Use of selective antagonists and antisense oligonucleotides to evaluate the mechanisms of BUBU antinociception

artículo científico publicado en 1999

[Interaction of S-(+)-ketamine with opiate receptors. Effects on EEG, evoked potentials and respiration in awake dogs]

scientific article published on 01 November 1994

[New reactions of phthalidoisoquinoline alkaloids. Alkoxy exchange reactions and isomerisations of alpha- and beta-narcotine (author's transl)]

artículo científico publicado en 1978

[Pharmacodynamic effects of S-(+)-ketamine on EEG, evoked potentials and respiration. A study in the awake dog]

artículo científico publicado en 1992

Lista de obras de Helmut Schmidhammer

(-)-N,N'-but-2-ene-1,4-diylbimorphinans.

14-Methoxymetopon, a highly potent mu opioid agonist, biphasically affects ethanol intake in Sardinian alcohol-preferring rats

14-Methoxymetopon, a very potent mu-opioid receptor-selective analgesic with an unusual pharmacological profile

14-methoxymetopon, a potent opioid, induces no respiratory depression, less sedation, and less bradycardia than sufentanil in the dog.

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

An opioid agonist with preference for kappa-opioid receptors: (-)-N-cyclopropylmethylmorphinan-6-one.

Antinociceptive activity of a novel buprenorphine analogue.

Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist

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

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

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

Cyprodime analogues: synthesis and pharmacological evaluation

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

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

Effect of novel non-peptidic delta opioid receptor antagonists on human T and B cell activation

Effects of 14-methoxymetopon, a potent opioid agonist, on the responses to the tail electric stimulation test and plus-maze activity in male rats: neuroendocrine correlates

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.

HS-599: a novel long acting opioid analgesic does not induce place-preference in rats

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

Highly potent novel opioid receptor agonist in the 14-alkoxymetopon series.

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

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

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

Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.

Inverse agonism by Dmt-Tic analogues and HS 378, a naltrindole analogue.

Involvement of mu- and kappa-, but not delta-, opioid receptors in the peristaltic motor depression caused by endogenous and exogenous opioids in the guinea-pig intestine.

Lack of regulatory changes of µ-opioid receptors by 14-methoxymetopon treatment in rat brain. Further evidence for functional selectivity

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 diversity of the van Leusen reaction applied to 6-ketomorphinans and synthetic potential of the resulting acrylonitrile substructures.

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.

Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.

Non-deleterious inhibition of endogenous peroxidase activity (EPA) by cyclopropanone hydrate: a definitive approach

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

Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation

Novel Positive Allosteric Modulators of µ Opioid Receptor-Insight from In Silico and In Vivo Studies

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

Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.

Opioid peptide receptor studies. 9. Identification of a novel non-mu- non-delta-like opioid peptide binding site in rat brain.

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.

Peripheral μ-opioid receptor mediated inhibition of calcium signaling and action potential-evoked calcium fluorescent transients in primary afferent CGRP nociceptive terminals.

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.

Separation of binding affinity and intrinsic activity of the potent mu-opioid 14-methoxymetopon.

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

Structure-activity relationships of oxygenated morphinans. III. An exploration of the effect of the aromatic oxygen and 6-keto group on antinociceptive activity, receptor affinity, and narcotic antagonism.

Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 11. 3-Hydroxycyprodime and Analogs: Opioid Antagonist Profile in Comparison to Cyprodime ⬇️

Synthesis and biological evaluation of 14-alkoxymorphinans, V: 6-Deoxyocyprodime, an opioid antagonist with decreased mu receptor selectivity in comparison to cyprodime.

Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones ⬇️

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. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.

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

Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds

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, 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

Use of selective antagonists and antisense oligonucleotides to evaluate the mechanisms of BUBU antinociception

[Interaction of S-(+)-ketamine with opiate receptors. Effects on EEG, evoked potentials and respiration in awake dogs]

[New reactions of phthalidoisoquinoline alkaloids. Alkoxy exchange reactions and isomerisations of alpha- and beta-narcotine (author's transl)]

[Pharmacodynamic effects of S-(+)-ketamine on EEG, evoked potentials and respiration. A study in the awake dog]