Luciano De Petrocellis
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View article: The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids
The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids Open
Phytocannabinoids (pCBs) from Cannabis sativa represent an important class of bioactive molecules, potentially useful for the treatment of a wide range of diseases. Their efficacy is due to their ability to interact with multiple targets o…
View article: Indole-2-Carboxamide as an Effective Scaffold for the Design of New TRPV1 Agonists
Indole-2-Carboxamide as an Effective Scaffold for the Design of New TRPV1 Agonists Open
Due to its central role in pain, inflammation, and related disorders, the Transient Receptor Potential (TPR) Vanilloid Type-1 (TRPV1) ion channel represents an attractive target for the development of novel antinociceptive and anti-inflamm…
View article: Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV Open
The first detailed phytochemical analysis of the cannabigerol (CBG)-rich chemotype IV of Cannabis sativa L. resulted in the isolation of the expected cannabigerolic acid/cannabigerol (CBGA/CBG) and cannabidiolic acid/cannabidiol (CB…
View article: Diurnal and circadian regulation of opsin-like transcripts in the eyeless cnidarian <i>Hydra</i>
Diurnal and circadian regulation of opsin-like transcripts in the eyeless cnidarian <i>Hydra</i> Open
Opsins play a key role in the ability to sense light both in image-forming vision and in non-visual photoreception (NVP). These modalities, in most animal phyla, share the photoreceptor protein: an opsin-based protein binding a light-sensi…
View article: <i>In Silico</i>-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists
<i>In Silico</i>-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists Open
We describe an in silico-guided rational drug design and the synthesis of the suggested ligands, aimed at improving the TRPV1-ligand binding properties and the potency of N-(4-hydroxy-3-methoxybenzyl)-4-(thiophen-2-yl) butana…
View article: Lipoic/Capsaicin-Related Amides: Synthesis and Biological Characterization of New TRPV1 Agonists Endowed with Protective Properties against Oxidative Stress
Lipoic/Capsaicin-Related Amides: Synthesis and Biological Characterization of New TRPV1 Agonists Endowed with Protective Properties against Oxidative Stress Open
α-Lipoic acid is a sulfur-containing nutrient endowed with pleiotropic actions and a safe biological profile selected to replace the unsaturated alkyl acid of capsaicin with the aim of obtaining lipoic amides potentially active as a TRPV1 …
View article: The Combined Effect of Branching and Elongation on the Bioactivity Profile of Phytocannabinoids. Part I: Thermo-TRPs
The Combined Effect of Branching and Elongation on the Bioactivity Profile of Phytocannabinoids. Part I: Thermo-TRPs Open
The affinity of cannabinoids for their CB1 and CB2 metabotropic receptors is dramatically affected by a combination of α-branching and elongation of their alkyl substituent, a maneuver exemplified by the n-pentyl -> α,α-dimethylheptyl (DMH…
View article: Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation
Identification and Characterization of Cannabidiol as an OX1R Antagonist by Computational and In Vitro Functional Validation Open
The potential, multifaceted therapeutic profile of cannabidiol (CBD), a major constituent derived from the Cannabis sativa plant, covers a wide range of neurological and psychiatric disorders, ranging from anxiety to pediatric epilepsy and…
View article: A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator Open
Palmitoylethanolamide (PEA) is an endogenous anti-inflammatory lipid mediator and a widely used nutraceutical. In this study, we designed, realized, and tested a drug-carrier conjugate between PEA (the active drug) and glucuronic acid (the…
View article: Discovery of a Remarkable Methyl Shift Effect in the Vanilloid Activity of Triterpene Amides
Discovery of a Remarkable Methyl Shift Effect in the Vanilloid Activity of Triterpene Amides Open
As part of a study on triterpenoid conjugates, the dietary pentacyclic triterpenoids oleanolic (2a) and ursolic acids (3a) were coupled with vanillamine, and the resulting amides (2b and 3b, respectively) were a…
View article: Design, Synthesis and In Vitro Experimental Validation of Novel TRPV4 Antagonists Inspired by Labdane Diterpenes
Design, Synthesis and In Vitro Experimental Validation of Novel TRPV4 Antagonists Inspired by Labdane Diterpenes Open
Labdane diterpenes are widespread classes of natural compounds present in variety of marine and terrestrial organisms and plants. Many of them represents “natural libraries” of compounds with interesting biological activities due to differ…
View article: Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, <i>Cannabis sativa</i> L., Is a Selective Thermo-TRP Modulator
Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, <i>Cannabis sativa</i> L., Is a Selective Thermo-TRP Modulator Open
Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural c…
View article: Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity Open
View article: Identification and Characterization of Cannabimovone, a Cannabinoid from Cannabis sativa, as a Novel PPARγ Agonist via a Combined Computational and Functional Study
Identification and Characterization of Cannabimovone, a Cannabinoid from Cannabis sativa, as a Novel PPARγ Agonist via a Combined Computational and Functional Study Open
Phytocannabinoids (pCBs) are a large family of meroterpenoids isolated from the plant Cannabis sativa. Δ9-Tetrahydrocannabinol (THC) and cannabidiol (CBD) are the best investigated phytocannabinoids due to their relative abundance and inte…
View article: Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro
Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro Open
Moringa oleifera Lam. is a tropical plant widely used in traditional medicines and as a food supplement. It is characterized by the presence of glucosinolates and isothiocyanates; the stable isothiocyanate 4-[(α-l-rhamnosyloxy)benzyl]isoth…
View article: Isothiocyanates and Glucosinolates from Sisymbrium officinale (L.) Scop. (“the Singers’ Plant”): Isolation and in Vitro Assays on the Somatosensory and Pain Receptor TRPA1 Channel
Isothiocyanates and Glucosinolates from Sisymbrium officinale (L.) Scop. (“the Singers’ Plant”): Isolation and in Vitro Assays on the Somatosensory and Pain Receptor TRPA1 Channel Open
Sisymbrium officinale (L.) Scop. is a wild common plant of the Brassicaceae family. It is known as “the singers’ plant” for its traditional use in treating aphonia and vocal disability. Despite its wide use in herbal preparations, the mole…
View article: Physiological and Pathological Role of TRPV1, TRPV2 and TRPV4 Channels in Heart
Physiological and Pathological Role of TRPV1, TRPV2 and TRPV4 Channels in Heart Open
Transient receptor potential vanilloid channel 2 (TRPV2) is required for normal cardiac contractility. The stimulation of TRPV1 in isolated cardiomyocytes can aggravate the effect of hypoxia/ reoxygenation (H/R) on H9C2 cells. The knockout…
View article: Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists
Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists Open
The transient receptor potential vanilloid type-2 (TRPV2) protein is a nonselective Ca2+ permeable channel member of the TRPV subfamily, still considered an orphan TRP channel due to the scarcity of available selective and poten…
View article: Effects of non‐euphoric plant cannabinoids on muscle quality and performance of dystrophic mdx mice
Effects of non‐euphoric plant cannabinoids on muscle quality and performance of dystrophic mdx mice Open
Background and Purpose Duchenne muscular dystrophy (DMD), caused by dystrophin deficiency, results in chronic inflammation and irreversible skeletal muscle degeneration. Moreover, the associated impairment of autophagy greatly contributes …
View article: TRPA1 Modulating C14 Polyacetylenes from the Iranian Endemic Plant Echinophora platyloba
TRPA1 Modulating C14 Polyacetylenes from the Iranian Endemic Plant Echinophora platyloba Open
Phytochemical investigation of the apolar extract obtained from aerial parts of the Iranian endemic plant Echinophora platyloba DC (Apiaceae) resulted in the characterization of the polyacetylene fraction of this plant. This resulted to be…
View article: Iodine-Promoted Aromatization of <i>p</i>-Menthane-Type Phytocannabinoids
Iodine-Promoted Aromatization of <i>p</i>-Menthane-Type Phytocannabinoids Open
Treatment with iodine cleanly converts various p-menthane-type phytocannabinoids and their carboxylated precursors into cannabinol (CBN, 1a). The reaction is superior to previously reported protocols in terms of simplicity and substrate ra…
View article: Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474
Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474 Open
A clue to a drug's neurotoxicity? The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment f…
View article: Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity Open
The cannabinoid CB 2 receptor (CB 2 R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB 2 R, their selectiv…
View article: Neuroactive and Anti-inflammatory Frankincense Cembranes: A Structure–Activity Study
Neuroactive and Anti-inflammatory Frankincense Cembranes: A Structure–Activity Study Open
An expeditious isolation method for the cembrane diterpene alcohols incensol (1a) and serratol (2) has been developed from respectively African and Indian frankincense. The two native alcohols and a series of semisynthetic derivatives of i…
View article: Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents
Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents Open
Tetrahydroisoquinoline derivatives containing embedded urea functions were identified as selective TRPM8 channel receptor antagonists. Structure-activity relationships were investigated, with the following conclusions: (a) The urea functio…
View article: Chalcone Derivatives Activate and Desensitize the Transient Receptor Potential Ankyrin 1 Cation Channel, Subfamily A, Member 1 TRPA1 Ion Channel: Structure-Activity Relationships in vitro and Anti-Nociceptive and Anti-inflammatory Activity in vivo
Chalcone Derivatives Activate and Desensitize the Transient Receptor Potential Ankyrin 1 Cation Channel, Subfamily A, Member 1 TRPA1 Ion Channel: Structure-Activity Relationships in vitro and Anti-Nociceptive and Anti-inflammatory Activity in vivo Open
Eleven compounds belonging to the chalcone family were tested for their ability to activate and subsequently desensitize the rat transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 (TRPA1) in a heterologous express…
View article: Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates
Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates Open
Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects. Different approaches have been applied to develop strong ana…
View article: Design and Synthesis of New Transient Receptor Potential Vanilloid Type-1 (TRPV1) Channel Modulators: Identification, Molecular Modeling Analysis, and Pharmacological Characterization of the<i>N</i>-(4-Hydroxy-3-methoxybenzyl)-4-(thiophen-2-yl)butanamide, a Small Molecule Endowed with Agonist TRPV1 Activity and Protective Effects against Oxidative Stress
Design and Synthesis of New Transient Receptor Potential Vanilloid Type-1 (TRPV1) Channel Modulators: Identification, Molecular Modeling Analysis, and Pharmacological Characterization of the<i>N</i>-(4-Hydroxy-3-methoxybenzyl)-4-(thiophen-2-yl)butanamide, a Small Molecule Endowed with Agonist TRPV1 Activity and Protective Effects against Oxidative Stress Open
4-(Thiophen-2-yl)butanoic acid was identified as a cyclic substitute of the unsaturated alkyl chain of the natural ligand, capsaicin. Accordingly, a new class of amides was synthesized in good yield and high purity and their molecular reco…
View article: Arylboronic acids as dual-action FAAH and TRPV1 ligands
Arylboronic acids as dual-action FAAH and TRPV1 ligands Open
View article: TRPA1 channels as targets for resveratrol and related stilbenoids
TRPA1 channels as targets for resveratrol and related stilbenoids Open