Colombo M.,NiKem Research |
Bianchi A.,Consorzio Interdisciplinare di Studi Biomolecolari ed Applicazioni Industriali CISI
Molecules | Year: 2010
In the last few years click chemistry reactions, and in particular coppercatalyzed cycloadditions, have been used intensively for the preparation of new bioconjugate molecules and materials applicable to biomedical and pharmaceutical areas. This review will be focused on conjugates of the tripeptide Arg-Gly-Asp formed by means of click chemistry reactions. This sequence is a well known binding motif for specific transmembrane proteins and is involved in cellular adhesion to the extracellular matrix, allowing the selective recognition of the biomolecule or polymer in which it is incorporated.
Fariello R.G.,Neurotune AG |
Ghelardini C.,University of Florence |
Di Cesare Mannelli L.,University of Florence |
Bonanno G.,University of Genoa |
And 4 more authors.
Neuropharmacology | Year: 2014
Dimiracetam, a bicyclic 2-pyrrolidinone derivative originally developed as cognition enhancer, is a member of the nootropic family for which anecdotal efficacy in models of neuropathic pain has been reported. Its antineuropathic activity was evaluated in established models of neuropathic pain induced by nerve injury, chemotherapy or MIA-induced osteoarthritis. Acutely, dimiracetam was very effective in models of antiretroviral drug induced painful neuropathy, oxaliplatin-induced hyperalgesia and in the MIA-osteoarthritis. Chronic dimiracetam dosing in the MIA and ART- induced models completely reverted hyperalgesia back to the level of healthy controls. Once reached, the maximal effect was maintained despite dose diminution and increased inter-dose interval. The effect of the last dose outlasted dimiracetam half-life longer than 12 times. In synaptosomal preparations, dimiracetam counteracted the NMDA-induced release of glutamate with highest potency in the spinal cord, possibly via NMDA receptor isoforms containing pH-sensitive GluN1 and GluN2A subunits. Dimiracetam appears to be a promising and safe treatment for neuropathic pain conditions for which there are very limited therapeutic options. © 2014 Elsevier Ltd. All rights reserved.
Sangster T.,Charles River Associates |
Maltas J.,BASi |
Struwe P.,Celerion |
Hillier J.,Gen-Probe |
And 27 more authors.
Bioanalysis | Year: 2012
The 5th Global CRO Council for Bioanalysis (GCC) meeting, held in Barcelona, Spain, in November 2011, provided a unique opportunity for CRO leaders to openly share opinions, perspectives and to agree on bioanalytical recommendations on incurred sample reproducibility in multi-analyte assays, regulation of quality assurance/bioanalytical consultants and regulatory requirements for GCP. © 2012 Future Science Ltd.
Lowes S.,Quintiles |
Boterman M.,ABL |
Doig M.,ABS Laboratories |
Breda M.,Accelera |
And 86 more authors.
Bioanalysis | Year: 2012
An open letter written by the Global CRO Council for Bioanalysis (GCC) describing the GCC survey results on stability data from co-administered and co-formulated drugs was sent to multiple regulatory authorities on 14 December 2011. This letter and further discussions at different GCC meetings led to subsequent recommendations on this topic of widespread interest within the bioanalytical community over the past 2 years. © 2012 Future Science Ltd.
De Zani D.,NiKem Research |
Colombo M.,NiKem Research
Journal of Flow Chemistry | Year: 2012
O-Alkylation of phenol compounds was performed in a continuous flow apparatus under biphasic liquid/liquid conditions and promoted by tetrabutylammonium bromide (TBAB) as a phase-transfer catalyst. The segmented flow that is generated within the flow system is able to afford the desired ethers in high yield and in very short times. © 2012 Akadémiai Kiadó.