List of works - Stephen M. Husbands

14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity

scientific article published on March 2009

14-Amino-4,5-epoxymorphinan derivatives and their pharmacological actions

scientific article published on January 2011

14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles

scientific article

14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists

scientific article published on November 2009

3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy

scientific article published in August 1998

3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group

scientific article published in August 2000

4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity

scientific article

A non-rewarding, non-aversive buprenorphine/naltrexone combination attenuates drug-primed reinstatement to cocaine and morphine in rats in a conditioned place preference paradigm

scientific article

A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates

scientific article published on 29 August 2016

Activities of mixed NOP and mu-opioid receptor ligands.

scientific article

Additive Effects of 3,4-Methylenedioxymethamphetamine (MDMA) and Compassionate Imagery on Self-Compassion in Recreational Users of Ecstasy

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

scientific article published on 21 September 2015

Antidepressant-like effects of BU10119, a novel buprenorphine analogue with mixed κ/μ receptor antagonist properties, in mice.

scientific article

BU08073 a buprenorphine analogue with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice

scientific article

BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates

scientific article published on 01 March 2019

BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism.

scientific article published on February 2005

Behavioral effects of rimcazole analogues alone and in combination with cocaine

scientific article published in May 2003

Behavioural tasks sensitive to acute abstinence and predictive of smoking cessation success: a systematic review and meta-analysis

scientific article

C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.

scientific article published on 6 May 2015

Characterization of BU09059: a novel potent selective κ-receptor antagonist

scientific article

Characterization of [(3)H]harmane binding to rat whole brain membranes.

scientific article published in December 2003

Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist.

scientific article published on September 2004

Combined administration of buprenorphine and naltrexone produces antidepressant-like effects in mice

scientific article published on 4 June 2015

Design and synthesis of [(2,3-dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as novel ligands selective for the dopamine D3 receptor subtype

scientific article

Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents

scientific article

Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates

scientific article

Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain

scientific article published on 07 May 2013

Effects of stimulation of mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors on alcohol drinking in rhesus monkeys

scientific article published on 10 April 2019

Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan

scientific article published in December 2004

Effects of the long-lasting kappa opioid 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl) ethyl] acetamide in a drug discrimination and warm water tail-withdrawal procedure

scientific article published in December 2005

Evaluation and initial in vitro and ex vivo characterization of the potential positron emission tomography ligand, BU99008 (2-(4,5-dihydro-1H-imidazol-2-yl)-1- methyl-1H-indole), for the imidazoline₂ binding site

scientific article published on 22 February 2012

Evaluation of 11C-BU99008, a PET ligand for the imidazoline2 binding sites in rhesus brain

scientific article published on 7 April 2014

Evaluation of 11C-BU99008, a positron emission tomography ligand for the Imidazoline2 binding site in human brain.

scientific article published on 9 March 2018

Extension of the Nenitzescu reaction to simple ketones provides an efficient route to 1'-alkyl-5'-hydroxynaltrindole analogues, potent and selective delta-opioid receptor antagonists

scientific article published in January 2005

First asymmetric synthesis of trans-3,4-dimethyl-4-arylpiperidines

scientific article published on 21 August 2007

Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects

scientific article published on 31 October 2012

Functional studies of specific imidazoline-2 receptor ligands.

scientific article

Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.

scientific article published in December 2003

Harmane and harmalan are bioactive components of classical clonidine-displacing substance.

scientific article published in December 2004

Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore

scientific article published in October 2004

Identification of an imidazoline binding protein: creatine kinase and an imidazoline-2 binding site

scientific article published on 03 May 2009

Identification of ligands selective for central I2-imidazoline binding sites

scientific article published on 01 January 1997

Imaging imidazoline-I2 binding sites in porcine brain using 11C-BU99008.

scientific article

In vitro and ex vivo distribution of [3H]harmane, an endogenous beta-carboline, in rat brain

scientific article published on 19 October 2005

In vivo and in vitro characterization of naltrindole-derived ligands at the κ-opioid receptor

scientific article

Isolation and chemical modification of clerodane diterpenoids from Salvia species as potential agonists at the kappa-opioid receptor.

scientific article

Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter

scientific article

Long-lasting effects of methocinnamox on heroin self-administration in rhesus monkeys

article

Loop diuretics are open-channel blockers of the cystic fibrosis transmembrane conductance regulator with distinct kinetics

scientific article published on January 2014

Methocinnamox Produces Long-Lasting Antagonism of the Behavioral Effects of µ-Opioid Receptor Agonists but Not Prolonged Precipitated Withdrawal in Rats

scientific article published on 22 August 2019

Methyl-orvinol-Dual activity opioid receptor ligand inhibits gastrointestinal transit and alleviates abdominal pain in the mouse models mimicking diarrhea-predominant irritable bowel syndrome

scientific article

Microfluidic reactions using [11C]carbon monoxide solutions for the synthesis of a positron emission tomography radiotracer.

scientific article published on 25 March 2011

Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines.

scientific article published on March 2009

N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands

scientific article published in May 2002

Novel approaches for the treatment of psychostimulant and opioid abuse - focus on opioid receptor-based therapies

scientific article

Novel ligands for the investigation of imidazoline receptors and their binding proteins.

scientific article published in December 2003

Novel mixed NOP/MOP agonist BU08070 alleviates pain and inhibits gastrointestinal motility in mouse models mimicking diarrhea-predominant irritable bowel syndrome symptoms

scientific article published on 6 May 2014

Novel selective compounds for the investigation of imidazoline receptors

scientific article

OREX-1019: A Novel Treatment of Opioid Use Disorder and Relapse Prevention

scientific article published on 20 November 2019

Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge

scientific article

Orvinols with mixed kappa/mu opioid receptor agonist activity

scientific article published on 3 April 2013

Palladium-mediated oxidative carbonylation reactions for the synthesis of (11) C-radiolabelled ureas

scientific article published on 11 December 2013

Pharmacological characterisation of novel alpha 2-adrenoceptor antagonists as potential brain imaging agents.

scientific article published in May 2004

Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand

scientific article published on 01 March 2000

Proerectile effects of dopamine D2-like agonists are mediated by the D3 receptor in rats and mice.

scientific article published on 09 January 2009

Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.

scientific article

Reversal and Prevention of the Respiratory-Depressant Effects of Heroin by the Novel μ-Opioid Receptor Antagonist Methocinnamox in Rhesus Monkeys

scientific article published on 21 November 2018

Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins

scientific article

Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters

scientific article (publication date: December 2001)

Ring constrained analogues of the orvinols: the furanomorphides

scientific article published in March 1999

Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization

scientific article published on 26 May 2015

Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.

scientific article published in April 2001

Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series

scientific article

Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity

scientific article

Selectivity and anti-Parkinson's potential of thiadiazolidinone RGS4 inhibitors

scientific article

Simultaneous Transdermal Delivery of Buprenorphine Hydrochloride and Naltrexone Hydrochloride by Iontophoresis

scientific article published on 22 May 2019

Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins

scientific article published on February 2012

Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine

scientific article published in January 2000

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones

scientific article published on August 2006

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring

scientific article published on October 2006

Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol

scientific article published in May 2000

Structural insights into µ-opioid receptor activation

scientific article

Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues

scientific article

Synthesis and in vivo brain distribution of carbon-11-labeled δ-opioid receptor agonists.

scientific article

Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile

scientific article published on 19 September 2018

Synthetic Cannabinoid Receptor Agonists Detection Using Fluorescence Spectral Fingerprinting

scientific article published on 03 October 2019

Targeting opioid receptor signaling in depression: do we need selective κ opioid receptor antagonists?

scientific article published on 14 May 2018

The effect of 1-(4,5-dihydro-1H-imidazol-2-yl) isoquinoline on monoamine release and turnover in the rat frontal cortex

scientific article

The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mous

scientific article

The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception.

scientific article published on 26 March 2018

The orvinols and related opioids--high affinity ligands with diverse efficacy profiles

scientific article

The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole

scientific article

Yawning and hypothermia in rats: effects of dopamine D3 and D2 agonists and antagonists.

scientific article

[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter

scientific article published in December 2001

beta-carboline binding to imidazoline receptors

scientific article

¹H, ¹³C, ¹⁵N HMBC, and ¹⁹F NMR spectroscopic characterisation of seized flephedrone, cut with benzocaine

scientific article published on 30 December 2014

List of works by Stephen M. Husbands

14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity

14-Amino-4,5-epoxymorphinan derivatives and their pharmacological actions

14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles

14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists

3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy

3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group

4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity

A non-rewarding, non-aversive buprenorphine/naltrexone combination attenuates drug-primed reinstatement to cocaine and morphine in rats in a conditioned place preference paradigm

A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates

Activities of mixed NOP and mu-opioid receptor ligands.

Additive Effects of 3,4-Methylenedioxymethamphetamine (MDMA) and Compassionate Imagery on Self-Compassion in Recreational Users of Ecstasy

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

Antidepressant-like effects of BU10119, a novel buprenorphine analogue with mixed κ/μ receptor antagonist properties, in mice.

BU08073 a buprenorphine analogue with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice

BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates

BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism.

Behavioral effects of rimcazole analogues alone and in combination with cocaine

Behavioural tasks sensitive to acute abstinence and predictive of smoking cessation success: a systematic review and meta-analysis

C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.

Characterization of BU09059: a novel potent selective κ-receptor antagonist

Characterization of [(3)H]harmane binding to rat whole brain membranes.

Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist.

Combined administration of buprenorphine and naltrexone produces antidepressant-like effects in mice

Design and synthesis of [(2,3-dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as novel ligands selective for the dopamine D3 receptor subtype

Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents

Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates

Effects of spinally administered bifunctional nociceptin/orphanin FQ peptide receptor/μ-opioid receptor ligands in mouse models of neuropathic and inflammatory pain

Effects of stimulation of mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors on alcohol drinking in rhesus monkeys

Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan

Effects of the long-lasting kappa opioid 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl) ethyl] acetamide in a drug discrimination and warm water tail-withdrawal procedure

Evaluation and initial in vitro and ex vivo characterization of the potential positron emission tomography ligand, BU99008 (2-(4,5-dihydro-1H-imidazol-2-yl)-1- methyl-1H-indole), for the imidazoline₂ binding site

Evaluation of 11C-BU99008, a PET ligand for the imidazoline2 binding sites in rhesus brain

Evaluation of 11C-BU99008, a positron emission tomography ligand for the Imidazoline2 binding site in human brain.

Extension of the Nenitzescu reaction to simple ketones provides an efficient route to 1'-alkyl-5'-hydroxynaltrindole analogues, potent and selective delta-opioid receptor antagonists

First asymmetric synthesis of trans-3,4-dimethyl-4-arylpiperidines

Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects

Functional studies of specific imidazoline-2 receptor ligands.

Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.

Harmane and harmalan are bioactive components of classical clonidine-displacing substance.

Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore

Identification of an imidazoline binding protein: creatine kinase and an imidazoline-2 binding site

Identification of ligands selective for central I2-imidazoline binding sites

Imaging imidazoline-I2 binding sites in porcine brain using 11C-BU99008.

In vitro and ex vivo distribution of [3H]harmane, an endogenous beta-carboline, in rat brain

In vivo and in vitro characterization of naltrindole-derived ligands at the κ-opioid receptor

Isolation and chemical modification of clerodane diterpenoids from Salvia species as potential agonists at the kappa-opioid receptor.

Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter

Long-lasting effects of methocinnamox on heroin self-administration in rhesus monkeys

Loop diuretics are open-channel blockers of the cystic fibrosis transmembrane conductance regulator with distinct kinetics

Methocinnamox Produces Long-Lasting Antagonism of the Behavioral Effects of µ-Opioid Receptor Agonists but Not Prolonged Precipitated Withdrawal in Rats

Methyl-orvinol-Dual activity opioid receptor ligand inhibits gastrointestinal transit and alleviates abdominal pain in the mouse models mimicking diarrhea-predominant irritable bowel syndrome

Microfluidic reactions using [11C]carbon monoxide solutions for the synthesis of a positron emission tomography radiotracer.

Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines.

N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands

Novel approaches for the treatment of psychostimulant and opioid abuse - focus on opioid receptor-based therapies

Novel ligands for the investigation of imidazoline receptors and their binding proteins.

Novel mixed NOP/MOP agonist BU08070 alleviates pain and inhibits gastrointestinal motility in mouse models mimicking diarrhea-predominant irritable bowel syndrome symptoms

Novel selective compounds for the investigation of imidazoline receptors

OREX-1019: A Novel Treatment of Opioid Use Disorder and Relapse Prevention

Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge

Orvinols with mixed kappa/mu opioid receptor agonist activity

Palladium-mediated oxidative carbonylation reactions for the synthesis of (11) C-radiolabelled ureas

Pharmacological characterisation of novel alpha 2-adrenoceptor antagonists as potential brain imaging agents.

Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand

Proerectile effects of dopamine D2-like agonists are mediated by the D3 receptor in rats and mice.

Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.

Reversal and Prevention of the Respiratory-Depressant Effects of Heroin by the Novel μ-Opioid Receptor Antagonist Methocinnamox in Rhesus Monkeys

Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins

Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters

Ring constrained analogues of the orvinols: the furanomorphides

Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization

Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.

Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series

Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity

Selectivity and anti-Parkinson's potential of thiadiazolidinone RGS4 inhibitors

Simultaneous Transdermal Delivery of Buprenorphine Hydrochloride and Naltrexone Hydrochloride by Iontophoresis

Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins

Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones