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2022 (6)

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Book
A Themed Issue in Honor of Professor Raphael Mechoulam: The Father of Cannabinoid and Endocannabinoid Research
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Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

During the last 60 years the relevance of cannabis (Cannabis sativa or Cannabis indica) ingredients, like the psychoactive Δ9-tetrahydrocannabinol (THC), cannabidiol, 120+ additional cannabinoids and 440+ non-cannabinoid compounds, for human health and disease has become apparent. Approximately 30 years after the elucidation of THC structure the molecular reasons for the biological activity of these plant extracts were made clearer by the discovery of endocannabinoids, that are endogenous lipids able to bind to the same receptors activated by THC. Besides endocannabinoids, that include several N-acylethanolamines and acylesters, a complex array of receptors, metabolic enzymes, transporters (transmembrane, intracellular and extracellular carriers) were also discovered, and altogether they form a so-called “endocannabinoid system” that has been shown to finely tune the manifold biological activities of these lipid signals. Both plant-derived cannabinoids and endocannabinoids were first discovered by the group led by Prof. Dr. Raphael Mechoulam, who has just celebrated his 90th birthday and clearly stood out as a giant of modern science. The many implications of his seminal work for chemistry, biochemistry, biology, pharmacology and medicine are described in this special issue by the scientists who reached during the last 20 years the highest recognition in the field of (endo)cannabinoid research, receiving the Mechoulam Award for their major contributions. I thank them for having accepted my invitation to be part of this honorary issue of Molecules, and Raphi for continuing to illuminate our field with his always inspiring investigations and new ideas.

Keywords

Research & information: general --- Biology, life sciences --- Biochemistry --- cannabinoid --- MRI-1867 --- hybrid ligand --- CB1 receptor antagonist --- iNOS inhibitor --- rimonabant --- intracerebroventricular administration --- alcohol craving --- two-bottle paradigm --- drinking in the dark --- N-acyltransferase --- anandamide --- endocannabinoid --- phospholipase A2 --- cannabichromene --- cannabidiolic acid --- cannabidivarin --- cannabidivarinic acid --- phytocannabinoids --- tetrahydrocannabivarin --- 4′-fluoro-cannabidiol --- cannabinoid tetrad --- elevated plus maze --- catalepsy --- marble bury --- HUF-101 --- equilibrative nucleoside transporter --- CB1 --- biased signaling --- functional selectivity --- G-protein --- β-arrestin --- cannabigerol --- anti-inflammatory --- obesity --- cannabinoid receptor 2 (CB2R) --- microglia --- inflammaging --- memory --- lipofuscin --- aminoalkylindole --- allodynia --- antinociception --- cannabinoid receptor --- CP55940 --- JWH-018 --- K2 --- pravadoline --- spice --- WIN55212-2 --- type 1 cannabinoid receptor CB1 --- cholesterol --- hippocampus --- frontal cortex --- synaptosomes --- rescue model --- anti-CB1 antibody --- cannabinoids --- GPR55 receptors --- VCE-006.1 --- chromenopyrazole --- Parkinson’s disease --- 6-hydroxydopamine --- lipopolysaccharide --- amyotrophic lateral sclerosis --- mSOD1 mice --- TDP-43 transgenic mice --- PPARs --- gut microbiome --- intestine --- ghrelin --- LEAP2 --- n/a --- 4'-fluoro-cannabidiol --- Parkinson's disease


Book
Opioids and Their Receptors : Present and Emerging Concepts in Opioid Drug Discovery II
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Few neurotransmitter systems have fascinated as much as the opioid system (i.e., opioid ligands and their receptors). Over the years, scientific studies of the endogenous opioid system have uncovered a complex and subtle system that exhibits impressive diversity, based on its critical role in modulating a large number of sensory, motivational, emotional and cognitive functions. Additionally, its important therapeutic value for the treatment of many human disorders, including pain, affective and addictive disorders, and gastrointestinal motility disorders, has been of persistent interest. This book specifically covers a broad area of the opioid research, offering up-to-date and new perspectives about opioid drug discovery. The diversity among the discussed topics ranging from medicinal chemistry to opioid pharmacology, from basic science to translational research, is a testimony to the complexity of the opioid system that results from the expression, regulation and functional role of opioid ligands and their receptors. This book will serve as a useful reference to scientists while also stimulating continuous research in the chemistry and pharmacology of the opioid system, with the prospective for finding improved therapies of human diseases where the opioid system plays a central role.


Book
A Themed Issue in Honor of Professor Raphael Mechoulam: The Father of Cannabinoid and Endocannabinoid Research
Author:
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
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Choose an application

Bookmark

Abstract

During the last 60 years the relevance of cannabis (Cannabis sativa or Cannabis indica) ingredients, like the psychoactive Δ9-tetrahydrocannabinol (THC), cannabidiol, 120+ additional cannabinoids and 440+ non-cannabinoid compounds, for human health and disease has become apparent. Approximately 30 years after the elucidation of THC structure the molecular reasons for the biological activity of these plant extracts were made clearer by the discovery of endocannabinoids, that are endogenous lipids able to bind to the same receptors activated by THC. Besides endocannabinoids, that include several N-acylethanolamines and acylesters, a complex array of receptors, metabolic enzymes, transporters (transmembrane, intracellular and extracellular carriers) were also discovered, and altogether they form a so-called “endocannabinoid system” that has been shown to finely tune the manifold biological activities of these lipid signals. Both plant-derived cannabinoids and endocannabinoids were first discovered by the group led by Prof. Dr. Raphael Mechoulam, who has just celebrated his 90th birthday and clearly stood out as a giant of modern science. The many implications of his seminal work for chemistry, biochemistry, biology, pharmacology and medicine are described in this special issue by the scientists who reached during the last 20 years the highest recognition in the field of (endo)cannabinoid research, receiving the Mechoulam Award for their major contributions. I thank them for having accepted my invitation to be part of this honorary issue of Molecules, and Raphi for continuing to illuminate our field with his always inspiring investigations and new ideas.


Book
Opioids and Their Receptors : Present and Emerging Concepts in Opioid Drug Discovery II
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

Few neurotransmitter systems have fascinated as much as the opioid system (i.e., opioid ligands and their receptors). Over the years, scientific studies of the endogenous opioid system have uncovered a complex and subtle system that exhibits impressive diversity, based on its critical role in modulating a large number of sensory, motivational, emotional and cognitive functions. Additionally, its important therapeutic value for the treatment of many human disorders, including pain, affective and addictive disorders, and gastrointestinal motility disorders, has been of persistent interest. This book specifically covers a broad area of the opioid research, offering up-to-date and new perspectives about opioid drug discovery. The diversity among the discussed topics ranging from medicinal chemistry to opioid pharmacology, from basic science to translational research, is a testimony to the complexity of the opioid system that results from the expression, regulation and functional role of opioid ligands and their receptors. This book will serve as a useful reference to scientists while also stimulating continuous research in the chemistry and pharmacology of the opioid system, with the prospective for finding improved therapies of human diseases where the opioid system plays a central role.


Book
A Themed Issue in Honor of Professor Raphael Mechoulam: The Father of Cannabinoid and Endocannabinoid Research
Author:
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

During the last 60 years the relevance of cannabis (Cannabis sativa or Cannabis indica) ingredients, like the psychoactive Δ9-tetrahydrocannabinol (THC), cannabidiol, 120+ additional cannabinoids and 440+ non-cannabinoid compounds, for human health and disease has become apparent. Approximately 30 years after the elucidation of THC structure the molecular reasons for the biological activity of these plant extracts were made clearer by the discovery of endocannabinoids, that are endogenous lipids able to bind to the same receptors activated by THC. Besides endocannabinoids, that include several N-acylethanolamines and acylesters, a complex array of receptors, metabolic enzymes, transporters (transmembrane, intracellular and extracellular carriers) were also discovered, and altogether they form a so-called “endocannabinoid system” that has been shown to finely tune the manifold biological activities of these lipid signals. Both plant-derived cannabinoids and endocannabinoids were first discovered by the group led by Prof. Dr. Raphael Mechoulam, who has just celebrated his 90th birthday and clearly stood out as a giant of modern science. The many implications of his seminal work for chemistry, biochemistry, biology, pharmacology and medicine are described in this special issue by the scientists who reached during the last 20 years the highest recognition in the field of (endo)cannabinoid research, receiving the Mechoulam Award for their major contributions. I thank them for having accepted my invitation to be part of this honorary issue of Molecules, and Raphi for continuing to illuminate our field with his always inspiring investigations and new ideas.

Keywords

Research & information: general --- Biology, life sciences --- Biochemistry --- cannabinoid --- MRI-1867 --- hybrid ligand --- CB1 receptor antagonist --- iNOS inhibitor --- rimonabant --- intracerebroventricular administration --- alcohol craving --- two-bottle paradigm --- drinking in the dark --- N-acyltransferase --- anandamide --- endocannabinoid --- phospholipase A2 --- cannabichromene --- cannabidiolic acid --- cannabidivarin --- cannabidivarinic acid --- phytocannabinoids --- tetrahydrocannabivarin --- 4'-fluoro-cannabidiol --- cannabinoid tetrad --- elevated plus maze --- catalepsy --- marble bury --- HUF-101 --- equilibrative nucleoside transporter --- CB1 --- biased signaling --- functional selectivity --- G-protein --- β-arrestin --- cannabigerol --- anti-inflammatory --- obesity --- cannabinoid receptor 2 (CB2R) --- microglia --- inflammaging --- memory --- lipofuscin --- aminoalkylindole --- allodynia --- antinociception --- cannabinoid receptor --- CP55940 --- JWH-018 --- K2 --- pravadoline --- spice --- WIN55212-2 --- type 1 cannabinoid receptor CB1 --- cholesterol --- hippocampus --- frontal cortex --- synaptosomes --- rescue model --- anti-CB1 antibody --- cannabinoids --- GPR55 receptors --- VCE-006.1 --- chromenopyrazole --- Parkinson's disease --- 6-hydroxydopamine --- lipopolysaccharide --- amyotrophic lateral sclerosis --- mSOD1 mice --- TDP-43 transgenic mice --- PPARs --- gut microbiome --- intestine --- ghrelin --- LEAP2 --- cannabinoid --- MRI-1867 --- hybrid ligand --- CB1 receptor antagonist --- iNOS inhibitor --- rimonabant --- intracerebroventricular administration --- alcohol craving --- two-bottle paradigm --- drinking in the dark --- N-acyltransferase --- anandamide --- endocannabinoid --- phospholipase A2 --- cannabichromene --- cannabidiolic acid --- cannabidivarin --- cannabidivarinic acid --- phytocannabinoids --- tetrahydrocannabivarin --- 4'-fluoro-cannabidiol --- cannabinoid tetrad --- elevated plus maze --- catalepsy --- marble bury --- HUF-101 --- equilibrative nucleoside transporter --- CB1 --- biased signaling --- functional selectivity --- G-protein --- β-arrestin --- cannabigerol --- anti-inflammatory --- obesity --- cannabinoid receptor 2 (CB2R) --- microglia --- inflammaging --- memory --- lipofuscin --- aminoalkylindole --- allodynia --- antinociception --- cannabinoid receptor --- CP55940 --- JWH-018 --- K2 --- pravadoline --- spice --- WIN55212-2 --- type 1 cannabinoid receptor CB1 --- cholesterol --- hippocampus --- frontal cortex --- synaptosomes --- rescue model --- anti-CB1 antibody --- cannabinoids --- GPR55 receptors --- VCE-006.1 --- chromenopyrazole --- Parkinson's disease --- 6-hydroxydopamine --- lipopolysaccharide --- amyotrophic lateral sclerosis --- mSOD1 mice --- TDP-43 transgenic mice --- PPARs --- gut microbiome --- intestine --- ghrelin --- LEAP2


Book
Opioids and Their Receptors : Present and Emerging Concepts in Opioid Drug Discovery II
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

Few neurotransmitter systems have fascinated as much as the opioid system (i.e., opioid ligands and their receptors). Over the years, scientific studies of the endogenous opioid system have uncovered a complex and subtle system that exhibits impressive diversity, based on its critical role in modulating a large number of sensory, motivational, emotional and cognitive functions. Additionally, its important therapeutic value for the treatment of many human disorders, including pain, affective and addictive disorders, and gastrointestinal motility disorders, has been of persistent interest. This book specifically covers a broad area of the opioid research, offering up-to-date and new perspectives about opioid drug discovery. The diversity among the discussed topics ranging from medicinal chemistry to opioid pharmacology, from basic science to translational research, is a testimony to the complexity of the opioid system that results from the expression, regulation and functional role of opioid ligands and their receptors. This book will serve as a useful reference to scientists while also stimulating continuous research in the chemistry and pharmacology of the opioid system, with the prospective for finding improved therapies of human diseases where the opioid system plays a central role.

Keywords

Research & information: general --- Chemistry --- thiazole --- piperazine --- tail-clip --- hot-plate --- acetic acid-induced writhing test --- opioid --- prodynorphin --- epigenetics --- transcription --- human brain --- morphine dosing --- behavior --- locomotor activity --- tolerance --- µ-opioid receptor --- DAMGO --- SR-17018 --- buprenorphine --- nalbuphine --- kappa opioid receptor agonist --- pruritis --- scratching --- mice --- TAT-HIV --- cholestasis --- chloroquine --- deoxycholic acid --- analgesic --- δ opioid receptor --- G-protein-biased agonist --- opioid peptide --- rubiscolins --- µ-opioid analgesics --- angiotensin receptors --- chronic pain --- neuropathic pain --- delta opioid receptor --- inverse agonist --- irreversible antagonist --- non-competitive antagonist --- molecular pharmacology --- free fatty acid receptors --- lipids --- opioid receptor --- colitis --- chemotype --- high-throughput screen --- allosteric modulation --- beta-arrestin --- molecular dynamics --- opioid receptors --- β-amino acids --- peptide synthesis --- receptor binding studies --- functional assay --- nociceptin/orphanin FQ receptor --- NOP receptor --- ligands --- nociceptin --- N/OFQ --- analgesia --- GPCR --- HS-731 --- peripheral opioid agonist --- binding --- selectivity --- molecular docking --- molecular dynamics simulations --- fluorescence cross-correlation spectroscopy (FCCS) --- G protein-coupled receptor (GPCR) --- serotonin --- thiazole --- piperazine --- tail-clip --- hot-plate --- acetic acid-induced writhing test --- opioid --- prodynorphin --- epigenetics --- transcription --- human brain --- morphine dosing --- behavior --- locomotor activity --- tolerance --- µ-opioid receptor --- DAMGO --- SR-17018 --- buprenorphine --- nalbuphine --- kappa opioid receptor agonist --- pruritis --- scratching --- mice --- TAT-HIV --- cholestasis --- chloroquine --- deoxycholic acid --- analgesic --- δ opioid receptor --- G-protein-biased agonist --- opioid peptide --- rubiscolins --- µ-opioid analgesics --- angiotensin receptors --- chronic pain --- neuropathic pain --- delta opioid receptor --- inverse agonist --- irreversible antagonist --- non-competitive antagonist --- molecular pharmacology --- free fatty acid receptors --- lipids --- opioid receptor --- colitis --- chemotype --- high-throughput screen --- allosteric modulation --- beta-arrestin --- molecular dynamics --- opioid receptors --- β-amino acids --- peptide synthesis --- receptor binding studies --- functional assay --- nociceptin/orphanin FQ receptor --- NOP receptor --- ligands --- nociceptin --- N/OFQ --- analgesia --- GPCR --- HS-731 --- peripheral opioid agonist --- binding --- selectivity --- molecular docking --- molecular dynamics simulations --- fluorescence cross-correlation spectroscopy (FCCS) --- G protein-coupled receptor (GPCR) --- serotonin

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