A5083488643- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Nicotinic Acetylcholine Receptors Study
- Pharmacological Receptor Mechanisms and Effects
- Ion channel regulation and function
- Asymmetric Synthesis and Catalysis
- Drug Transport and Resistance Mechanisms
- Cholinesterase and Neurodegenerative Diseases
- Cancer therapeutics and mechanisms
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Asymmetric Hydrogenation and Catalysis
- Neuropeptides and Animal Physiology
- Synthesis and biological activity
- Mass Spectrometry Techniques and Applications
- Sleep and related disorders
- Protein Kinase Regulation and GTPase Signaling
- Analytical Chemistry and Chromatography
- Molecular spectroscopy and chirality
- Chemical Synthesis and Analysis
- Sleep and Wakefulness Research
- Pain Mechanisms and Treatments
- Axial and Atropisomeric Chirality Synthesis
- Synthesis and Biological Evaluation
- DNA and Nucleic Acid Chemistry
- Structural and Chemical Analysis of Organic and Inorganic Compounds
University of Florence
2008-2020
University of Bologna
1995-2016
University of Perugia
2015
Università di Camerino
2006-2007
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStructure-activity relationship studies in the field of calcium(II) antagonists. Effect modifications at tetrasubstituted carbon verapamil-like compoundsFulvio Gualtieri, Elisabetta Teodori, Cristina Bellucci, Edilio Pesce, and Giuseppe PiacenzaCite this: J. Med. Chem. 1985, 28, 11, 1621–1628Publication Date (Print):November 1, 1985Publication History Published online1 May 2002Published inissue 1 November...
Several compounds with a 4-aminopiperidine scaffold decorated on both nitrogen atoms by alkyl or acyl moieties containing the structural motifs of verapamil and flunarizine, as well those that are more frequent in known N-type calcium channel antagonists, have been synthesized. Antinociceptive activity mouse hot-plate test was used to select molecules be submitted further studies. Active were tested vitro PC12 rat pheochromocytoma clonal cell line, evaluate their action channels, model...
Several 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones have been synthesized and tested in vivo on mouse passive avoidance test, to evaluate their nootropic activity. The results show that they represent a new class of drugs with pharmacological profile very similar piracetam, showing much higher potency respect the reference. Among compounds studied, 7 (DM 232) shows outstanding potency, being active at dose 0.001 mg kg-1 sc.
By further steric complication of previously studied highly chiral muscarinic agonists, we have obtained a small library enantiomeric and diasteromeric 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxides. Binding studies on cloned human receptors expressed in CHO cells show that the introduction fourth stereogenic center gives undetectable affinity for hm1, hm3, hm4 hm5 subtypes while leaving quite modest only hm2 subtypes. However, functional model M1−M4 tissues shown three...
Starting from a previously studied muscarinic ligand, characterized by 1,3-oxathiolane nucleus, new series of antagonists were designed increasing the stereochemical complexity molecules. A small library enantiomeric and diastereomeric 2,2-diphenyl- 2-cyclohexyl-2-phenyl substituted compounds was thus obtained. All tested show high affinity toward cloned human hm1−hm5 receptors expressed in CHO cells good antagonistic activity on functional assays, with modest selectivity rabbit vas deferens.
Starting from a hydroxylactone anhydrosugar available catalytic cellulose pyrolysis, five new muscarine-like compounds have been synthesized and studied for their binding affinity to human subtype muscarine receptors, obtaining results supported by docking calculation.
AG-4 has been characterized as a nicotinic agonist by binding (Ki = 26 ± 1.4 μM) and in vitro functional assays. The antinociceptive effect of was examined mice rats, using the hot plate, abdominal constriction, paw-pressure tests. In both species, (25–150 μg per mouse icv; 100–150 rat icv) produced significant antinociception which prevented mecamylamine (2 mg kg–1 ip) pempidine (3 i.p.), but not atropine (5 ip), naloxone (1 CGP 35348 (100 ip). dose range, did impair motor coordination...