A5021058541- Drug Transport and Resistance Mechanisms
- Pharmacological Receptor Mechanisms and Effects
- Receptor Mechanisms and Signaling
- Pharmacological Effects and Toxicity Studies
- Cancer therapeutics and mechanisms
- HIV/AIDS drug development and treatment
- Neurotransmitter Receptor Influence on Behavior
- Neuropeptides and Animal Physiology
- Radiopharmaceutical Chemistry and Applications
- Neuroscience and Neuropharmacology Research
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Computational Drug Discovery Methods
- Phenothiazines and Benzothiazines Synthesis and Activities
- Alzheimer's disease research and treatments
- Nicotinic Acetylcholine Receptors Study
- Trace Elements in Health
- Synthesis and Biological Evaluation
- Cannabis and Cannabinoid Research
- Chemical Synthesis and Analysis
- Cholinesterase and Neurodegenerative Diseases
- Amino Acid Enzymes and Metabolism
- Metal complexes synthesis and properties
- DNA and Nucleic Acid Chemistry
- Epilepsy research and treatment
- Axial and Atropisomeric Chirality Synthesis
University of Bari Aldo Moro
2015-2024
Consorzio Interuniversitario per lo Sviluppo dei Sistemi a Grande Interfase
2024
Deaconess Hospital
2023
University of Vienna
2010
Mario Negri Institute for Pharmacological Research
2008
University of Pisa
2006-2008
Institute of Molecular Bioimaging and Physiology
2005
University of Milano-Bicocca
2005
sigma Ligands have recently been shown to cytotoxic activity, induce ceramide-dependent/caspase-independent apoptosis, and down-regulate P-glycoprotein (P-gp) mRNA levels in some mouse human models. In this study, we verified whether a mixed sigma(2) agonist/sigma(1) antagonist, PB28, was able antitumor activity enhance anthracycline efficacy two breast cancer cell lines, MCF7 ADR, both characterized by significant receptor expression, high low sigma(1) P-gp respectively. PB28 showed...
Nor-BNI, GNTI and JDTic induce selective κ opioid antagonism that is delayed extremely prolonged, but some other effects are of rapid onset brief duration. The transient these compounds differ, suggesting them may be mediated by targets.In binding assays, the three antagonists showed no detectable affinity (K(i)≥10 µM) for most non-opioid receptors transporters (26 43 tested). There was target which all shared affinity, or any two sub-micromolar affinity. All low nanomolar receptors, with...
Anthrax is an infectious disease caused by Bacillus anthracis, a bioterrorism agent that develops resistance to clinically used antibiotics. Therefore, alternative mechanisms of action remain challenge. Herein, we disclose deoxy glycosides responsible for specific carbohydrate-phospholipid interactions, causing phosphatidylethanolamine lamellar-to-inverted hexagonal phase transition and acting over B. anthracis cereus as potent selective bactericides. Biological studies the synthesized...
Abstract With the aim of contributing to development novel antitumor agents, high‐affinity σ 2 receptor agonists were developed, with 6,7‐dimethoxy‐2‐[4‐[1‐(4‐fluorophenyl)‐1 H ‐indol‐3‐yl]butyl]‐1,2,3,4‐tetrahydroisoquinoline ( 15 ) and 9‐[4‐(6,7‐dimethoxy‐1,2,3,4‐tetrahydroisoquinolin‐2‐yl)butyl]‐9 ‐carbazole 25 showing exceptional selectivity for subtype. Most compounds displayed notable antiproliferative activity in human MCF7 breast adenocarcinoma cells, similar corresponding...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTHigh Affinity and Selectivity on 5-HT1A Receptor of 1-Aryl-4-[(1-tetralin)alkyl]piperazines. 2Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Marcello Leopoldo, Vincenzo Tortorella, Fiorentini, Olgiati, Alberto Ghiglieri, Stefano GovoniCite this: J. Med. Chem. 1995, 38, 6, 942–949Publication Date (Print):March 1, 1995Publication History Published online1 May 2002Published inissue 1 March...
Starting from the previously reported 5-HT 7 receptor agents 4-7 with N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamide structure, 1-(2-methylthiophenyl)-, 1-(2-diphenyl)-, 1-(2-isopropylphenyl)-, and 1-(2-methoxyphenyl)piperazine derivatives 8-31 were designed primary aim to obtain new compounds endowed suitable physicochemical properties for rapid extensive penetration into brain. The affinities 7, 1A, D 2 receptors of assessed, several displayed in nanomolar range. Among...
The benzamide PB12 (N-[2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide) (1), already reported as potent and selective dopamine D4 receptor ligand, has been modified searching for structural features that could lead to D3 affinity. Changes in the aromatic ring linked N-1 piperazine led identification of 2-methoxyphenyl 2,3-dichlorophenyl derivatives (compounds 6 13) displaying moderate affinity (Ki = 145 31 nM, respectively). Intermediate alkyl chain elongation compounds 1, 6,...
Several 1-cyclohexylpiperazine derivatives related to σ2 receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (33, Ki = 0.34 nM) were synthesized and tested in radioligand binding assays, attempt a structure−affinity relationship study. Intermediate alkyl chain length methoxyl group position on the tetralin nucleus varied. A few naphthalene analogues also prepared. High affinities found for almost all compounds, some of which displayed values...
A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT7, 5-HT(1A), 5-HT(2A) receptors measured by in vitro binding assays. In relation to 5-HT7 receptor affinity, studies indicated that (i) the optimal alkyl chain length five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus preferred, (iii) substitution pattern aryl ring linked piperazine played a crucial role....
Here we report the synthesis of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides 16−29 that were designed to elucidate both structure−affinity and −activity relationships for 5-HT7 receptor, by targeting substituent in 2-position aryl linked piperazine ring. The affinities 5-HT7, 5-HT1A, 5-HT2A, D2 receptors assessed radioligand binding assays. intrinsic activities at receptor most potent compounds determined. A series substituents covering a wide range electronic,...
P-glycoprotein (P-gp) is an ATP-dependent efflux pump protecting the body against xenobiotics. A P-gp substrate (7) and inhibitor (6) were labeled with (11)C, resulting in potential tracers of function expression.6 7 using (11)CH(3)I. (11)C-verapamil was prepared as published previously, (11)C-methyl triflate. MicroPET scans (with arterial sampling) biodistribution studies performed rats pretreated saline, cyclosporin (CsA, 50 mg/kg), or cold 6 (15 mg/kg).The radiochemical yields (11)C-6...