Giuseppe Caliendo
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View article: Novel 1,4-benzothiazepin-2-one modulators of NCX3 as a promising strategy for neuroprotection in cerebral ischemia
Novel 1,4-benzothiazepin-2-one modulators of NCX3 as a promising strategy for neuroprotection in cerebral ischemia Open
The Na+ /Ca2+ exchanger plays a key role in the regulation of calcium homeostasis in most excitable cells. Three mammalian isoforms, NCX1, NCX2, and NCX3, are described, and with their splice variant, they are express…
View article: Improved Synthesis of 5-Nitrohomovanillic Acid and 6-Nitrohomovanillic Acid as Probes for Metabolism Studies of Endothelium-Derived Dopamines: Identification in Human Amniotic Fluid
Improved Synthesis of 5-Nitrohomovanillic Acid and 6-Nitrohomovanillic Acid as Probes for Metabolism Studies of Endothelium-Derived Dopamines: Identification in Human Amniotic Fluid Open
6-Nitrodopamine is an endogenous catecholamine responsible for numerous biological activities. Here, an improved method for the synthesis of both 6-nitrohomovanillic acid (6-NHVA) and its regioisomer 5-nitrohomovanillic acid (5-NHVA) is re…
View article: 1,2,4-Thiadiazolidin-3,5-Diones as Inhibitors of Cysteine Proteases
1,2,4-Thiadiazolidin-3,5-Diones as Inhibitors of Cysteine Proteases Open
A focused library of 1,2,4-thiadiazolidin-3,5-diones (THIA-1–10), previously characterized as hydrogen sulfide (H2S) donors, was evaluated for inhibitory activity against cysteine proteases. We included two key cysteine proteases aiming at…
View article: Druggability of Sodium Calcium Exchanger (NCX): Challenges and Recent Development
Druggability of Sodium Calcium Exchanger (NCX): Challenges and Recent Development Open
Na+/Ca2+ exchangers (NCXs) are membrane transporters crucial for calcium homeostasis in excitable tissues, particularly in the central nervous system. Growing evidence indicates that NCX dysfunction contributes to calcium overload and neur…
View article: The identification of adenylyl cyclase modulators as potential receptors for 6-nitrodopamine in human-induced pluripotent stem cell (hiPSC)-derived cardiomyocytes and their relevance in heart inotropism
The identification of adenylyl cyclase modulators as potential receptors for 6-nitrodopamine in human-induced pluripotent stem cell (hiPSC)-derived cardiomyocytes and their relevance in heart inotropism Open
6-Nitrodopamine (6-ND) has potent positive chronotropic and inotropic effects. At a very low dose, i.e., 10 fM, it causes potentiation of the positive chronotropic effects induced by catecholamines in the rat atria, indicating a distinct m…
View article: Front Cover: Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents (ChemMedChem 15/2025)
Front Cover: Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents (ChemMedChem 15/2025) Open
View article: Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents
Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents Open
The synthesis of a new series of long‐chain arylpiperazine as serotoninergic ligands ( FG 1‐18 ) is described. The combination of structural elements including heterocyclic nucleus, propyl chain, and 4,5‐dihydrothiazol‐2‐ylphenylpiperazine…
View article: A new nano-encapsulated TSPO ligand reduces neuroinflammation and improves cognitive functions in Alzheimer's disease model
A new nano-encapsulated TSPO ligand reduces neuroinflammation and improves cognitive functions in Alzheimer's disease model Open
Rationale: The translocator protein 18 kDa (TSPO) is mainly expressed on the outer mitochondrial membrane and is implicated in inflammation, cell survival, and proliferation. TSPO expression in activated microglia is upregulated in …
View article: The PREVASC study: Prospective REgistry of Valve disease in Asymptomatic Italian elderly SubjeCts
The PREVASC study: Prospective REgistry of Valve disease in Asymptomatic Italian elderly SubjeCts Open
Aims Valvular heart disease (VHD) is the third leading cause of cardiovascular morbidity, with its incidence and public health impact projected to increase significantly. This study adopts a novel perspective, focusing on elderly individua…
View article: Retrospective Study on Short-Term Reverse Cardiac Remodeling in Obese Patients Undergoing Sleeve Gastrectomy
Retrospective Study on Short-Term Reverse Cardiac Remodeling in Obese Patients Undergoing Sleeve Gastrectomy Open
Severe obesity is closely associated with an increased risk of comorbidities and alterations in cardiac structure and function. The primary objective of this study was to investigate cardiovascular (CV) risk factors and ventricular remodel…
View article: Development and evaluation of nanostructured systems for cutaneous delivery of H2S-releasing corticosteroids for skin inflammatory diseases
Development and evaluation of nanostructured systems for cutaneous delivery of H2S-releasing corticosteroids for skin inflammatory diseases Open
Psoriasis is an immune-mediated chronic inflammatory disease that causes major psychosocial impact. Topical corticosteroids represent the standard pharmacological treatment for mild-to-moderate disease, but their local and systemic adverse…
View article: Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry
Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry Open
Background: In recent decades, there has been a startling rise in the number of cancer patients worldwide, which has led to an amazing upsurge in the development of novel anticancer treatment candidates. On a positive note, arylpiperazines…
View article: A New Process for the Synthesis of Budesonide 21-Phosphate and Evaluation in a Murine Model of Inflammation
A New Process for the Synthesis of Budesonide 21-Phosphate and Evaluation in a Murine Model of Inflammation Open
In this study, a new and straightforward process for the preparation of budesonide 21-phosphate (Bud-21P) and its disodium salt (Bud-21P-Na2) is described. The method results in a yield comparable to those obtained by diphosphoryl chloride…
View article: The negative chronotropic effects of (±)-propranolol and (±)- 4-NO 2 -propranolol in the rat isolated right atrium are due to blockade of the 6-nitrodopamine receptor
The negative chronotropic effects of (±)-propranolol and (±)- 4-NO 2 -propranolol in the rat isolated right atrium are due to blockade of the 6-nitrodopamine receptor Open
The positive chronotropic action induced by 6-mitrodopamine (6-ND) is selectively blocked by β1-adrenoceptor antagonists at concentrations that do not affect the positive chronotropic effect induced by dopamine, noradrenaline, a…
View article: Hydrogen Sulfide (H2S)-Donor Molecules: Chemical, Biological, and Therapeutical Tools
Hydrogen Sulfide (H2S)-Donor Molecules: Chemical, Biological, and Therapeutical Tools Open
This Special Issue aims to gather new research on hydrogen sulfide (H2S)-releasing compounds (Figure 1) as cutting-edge pharmacological tools and to advance the understanding of the critical role that H2S plays in physiological and patholo…
View article: Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry
Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry Open
In recent decades, there has been a startling rise in the number of cancer patients worldwide, which has led to an amazing upsurge in the development of novel anticancer treatment candidates. On a positive note, arylpiperazines have garner…
View article: Isothiocyanate-Corticosteroid Conjugates against asthma: Unity makes strength
Isothiocyanate-Corticosteroid Conjugates against asthma: Unity makes strength Open
Asthma is a major noncommunicable disease, affecting both children and adults, and represents one of the major causes leading to high health care costs due to the need for chronic pharmacological treatments. The standard gold therapy of in…
View article: Pills of Multi-Target H2S Donating Molecules for Complex Diseases
Pills of Multi-Target H2S Donating Molecules for Complex Diseases Open
Among the various drug discovery methods, a very promising modern approach consists in designing multi-target-directed ligands (MTDLs) able to modulate multiple targets of interest, including the pathways where hydrogen sulfide (H2S) is in…
View article: Newly Synthesized Indolylacetic Derivatives Reduce Tumor Necrosis Factor-Mediated Neuroinflammation and Prolong Survival in Amyotrophic Lateral Sclerosis Mice
Newly Synthesized Indolylacetic Derivatives Reduce Tumor Necrosis Factor-Mediated Neuroinflammation and Prolong Survival in Amyotrophic Lateral Sclerosis Mice Open
The debilitating neurodegenerative disease known as amyotrophic lateral sclerosis (ALS) is characterized by the progressive loss of motor neurons (MNs) in the brain, spinal cord, and motor cortex. The ALS neuroinflammatory component is bei…
View article: Vitamin D: A Bridge between Kidney and Heart
Vitamin D: A Bridge between Kidney and Heart Open
Chronic kidney disease (CKD) and cardiovascular disease (CVD) are highly prevalent conditions, each significantly contributing to the global burden of morbidity and mortality. CVD and CKD share a great number of common risk factors, such a…
View article: GKT137831 and hydrogen peroxide increase the release of 6-nitrodopamine from the human umbilical artery, rat-isolated right atrium, and rat-isolated vas deferens
GKT137831 and hydrogen peroxide increase the release of 6-nitrodopamine from the human umbilical artery, rat-isolated right atrium, and rat-isolated vas deferens Open
Introduction: The human umbilical artery (HUA), rat-isolated right atrium, and rat-isolated vas deferens present a basal release of 6-nitrodopamine (6-ND). The basal release of 6-ND from these tissues was significantly decreased (but not a…
View article: 3-Nitroatenolol: First Synthesis, Chiral Resolution and Enantiomers’ Absolute Configuration
3-Nitroatenolol: First Synthesis, Chiral Resolution and Enantiomers’ Absolute Configuration Open
4-Nitro and 7-nitro propranolol have been recently synthesized and characterized by us. (±)-4-NO2-propranolol has been shown to act as a selective antagonist of 6-nitrodopamine (6-ND) receptors in the right atrium of rats. As part of our f…
View article: Vitamin D: A Bridge between Kidney and Heart
Vitamin D: A Bridge between Kidney and Heart Open
Chronic kidney disease (CKD) and cardiovascular disease (CVD) are highly prevalent conditions, each significantly contributing to the global burden of morbidity and mortality. CVD and CKD share a great number of common risk factor, such as…
View article: The effect of (±)-4-NO 2 -propranolol, (±)-7-NO 2 -propranolol, and (±)- propranolol on the rat isolated right atrium
The effect of (±)-4-NO 2 -propranolol, (±)-7-NO 2 -propranolol, and (±)- propranolol on the rat isolated right atrium Open
6-Nitrodopamine (6-ND) is released from rat isolated atria and has positive chronotropic action, which is selectively blocked by β 1 -adrenoceptor antagonists at concentrations that do not affect the positive chronotropic effect induced by…
View article: Isothiocyanate-Corticosteroid Conjugates Against Asthma: Unity Makes Strength
Isothiocyanate-Corticosteroid Conjugates Against Asthma: Unity Makes Strength Open
View article: 4-Nitro-propranolol selectively inhibits the positive chronotropic effect induced by 6-nitrodopamine in the rat isolated right atrium
4-Nitro-propranolol selectively inhibits the positive chronotropic effect induced by 6-nitrodopamine in the rat isolated right atrium Open
6-Nitrodopamine (6-ND) is released from isolated atria of rabbit, rat and mice and has significant positive chronotropic action. The positive chronotropic effect induced by 6-ND is selectively blocked by β1-adrenoceptor antagonists at conc…
View article: Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring
Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring Open
Arylpiperazines represent one of the most important classes of 5-HT1AR ligands and have attracted considerable interests for their versatile properties in chemistry and pharmacology, leading to the research of new derivatives that has been…
View article: Prednisone-hydrogen sulfide releasing hybrid shows improved therapeutic profile in asthma
Prednisone-hydrogen sulfide releasing hybrid shows improved therapeutic profile in asthma Open
Introduction: Hydrogen sulfide (H 2 S) is emerging as an important potential therapeutic option for respiratory inflammatory diseases. In this study, we investigated the effectiveness of a novel corticosteroid derivative, that is chemicall…
View article: Interventions to Address Cardiovascular Risk in Obese Patients: Many Hands Make Light Work
Interventions to Address Cardiovascular Risk in Obese Patients: Many Hands Make Light Work Open
Obesity is a growing public health epidemic worldwide and is implicated in slowing improved life expectancy and increasing cardiovascular (CV) risk; indeed, several obesity-related mechanisms drive structural, functional, humoral, and hemo…
View article: Beneficial Effects of Two Hydrogen Sulfide (H2S)-Releasing Derivatives of Dexamethasone with Antioxidant Activity on Atopic Dermatitis in Mice
Beneficial Effects of Two Hydrogen Sulfide (H2S)-Releasing Derivatives of Dexamethasone with Antioxidant Activity on Atopic Dermatitis in Mice Open
Hydrogen sulfide (H2S) is particularly produced in the skin, where it participates in the regulation of inflammation, pruritus, cytoprotection, scarring, and angiogenesis. In this study, we compared the effects of dexamethasone (Dex) with …