Search results for "Zole"
showing 10 items of 2482 documents
Review of Pharmacokinetics and Pharmacogenetics in Atypical Long-Acting Injectable Antipsychotics
2021
Over the last two decades, pharmacogenetics and pharmacokinetics have been increasingly used in clinical practice in Psychiatry due to the high variability regarding response and side effects of antipsychotic drugs. Specifically, long-acting injectable (LAI) antipsychotics have different pharmacokinetic profile than oral formulations due to their sustained release characteristics. In addition, most of these drugs are metabolized by CYP2D6, whose interindividual genetic variability results in different metabolizer status and, consequently, into different plasma concentrations of the drugs. In this context, there is consistent evidence which supports the use of therapeutic drug monitoring (TD…
Zn2+ and Cu2+ complexes of a fluorescent scorpiand-type oxadiazole azamacrocyclic ligand: crystal structures, solution studies and optical properties
2020
A ligand comprised of a macrocyclic pyridinophane core having a pendant arm containing a secondary amine group linked through a methylene spacer to a pyridyl–oxadiazole–phenyl (PyPD) fluorescent system has been prepared (L). The crystal structures of [ZnL](ClO4)2 and [CuL](ClO4)2 show that M2+ is coordinated to all the nitrogen atoms of the macrocyclic core, the secondary amine of the pendant arm and the nitrogen atom of the pyridine group of the fluorescent moiety, the latter bond being clearly weaker than the one with the pyridine of the macrocycle. Solution studies showed the formation of a highly stable Cu2+ complex with 1 : 1 stoichiometry, whereas with Zn2+ least stable complexes were…
Compliance and arthralgias in clinical therapy (COMPACT): Assessment of the incidence of arthralgia, therapy costs, and compliance in the first year …
2012
e11040^ Background: Aromatase Inhibitors (AI) are well established as adjuvant endocrine treatment for postmenopausal women with HR+ early breast cancer (EBC). However, clinical trial data show higher frequently of arthralgia with AI than tamoxifen. As arthralgia may be greatly influencing compliance to adjuvant therapy, we designed a prospective trial to collect real world data on the effects of AI-associated arthralgia on patient compliance, patient outcomes and treatment costs of arthralgia. Methods: COMPACT is an open, prospective non-interventional study (NCT00857012) assessing the incidence of arthralgia, therapy costs, and compliance within the first year of adjuvant anastrozole (AN…
COX-2 expression in chondrosarcoma: A role for celecoxib treatment?
2010
Chondrosarcomas are resistant to conventional chemo- and radiotherapy. A subset of chondrosarcomas arises secondarily in the benign tumour syndromes enchondromatosis (EC) and multiple osteochondromas (MO), and prevention of tumour development would greatly improve prognosis. We therefore investigated the effect of selective COX-2 inhibition on chondrosarcoma growth. COX-2 expression was studied in central- and peripheral cartilaginous tumours. The effect of COX-2 inhibition was assessed in four high-grade chondrosarcoma cell lines using celecoxib and NS-398 treatment. COX-2 activity (prostaglandin E-2 (PGE(2)) ELISA) and cell viability were measured. The (prophylactic) effect of celecoxib o…
COMPliance and Arthralgia in Clinical Therapy: the COMPACT trial, assessing the incidence of arthralgia, and compliance within the first year of adju…
2014
5 Office-based Professional Association Gynecologic Oncologists e.V. in Germany (BNGO e.V.), Berlin; 6 Background: This prospective study evaluated the relationship between arthralgia and compliance during the first year of adjuvant anastrozole therapy in postmenopausal women with hormone receptor-positive early breast cancer. Patients and methods: COMPliance and Arthralgia in Clinical Therapy (COMPACT) was an open-label, multicenter, noninterventional study conducted in Germany. Patients had started adjuvant anastrozole 3-6 months before the study start. The primary end points were arthralgia, compliance, and the relationship between compliance and arthralgia, assessed at specific time poi…
AB1394 Compliance and arthralgias in clinical therapy (compact): Assessment of the incidence of arthralgia, therapy costs and compliance within the f…
2013
Background Aromatase inhibitors (AI) are well established as adjuvant endocrine treatment for postmenopausal women with hormone receptor-positive (HR+) early breast cancer (EBC). Drug-induced myalgia or arthralgia is among the most frequently reported adverse drug reactions to AIs. Objectives Little is known about the pathomechanism by which AIs cause muscle and joint injury. The literature on skeletal muscle complaints with AIs is confusing, in part because of a lack of clear definitions. Myalgia/arthralgia is defined as muscle/joint pain and is likely to affect patients’ quality of life and compliance with AI medication . We designed a prospective trial to collect real world data on the e…
Síntesis y caracterización de compuestos de Cu(II) con derivados triazólicos. Estudio de su actividad como potenciales nucleasas químicas
2014
The main goal of this PhD thesis concerns the development of artificial metallonucleases based on copper(II)-1,2,4-triazole compounds. In order to do so, we have obtained metal compounds of different nuclearities by reaction of a new family of 1,2,4-triazole ligands with copper(II) salts. The ligands own the characteristic triazole properties upon coordinating to metals and also integrate DNA binding units (aromatic moieties) with the aim of increasing the affinity of the corresponding metal complexes to double strand DNA. We have also chosen the copper(II) ion due to its intrinsic redox and coordination properties. Here we present our conclusions in relation with their structure/activity a…
Electrophysiological and neurochemical characterization of 7-nitroindazole and molsidomine acute and sub-chronic administration effects in the dopami…
2009
Nicotine, the main psychoactive ingredient in tobacco, stimulates dopamine (DA) function, increasing DA neuronal activity and DA release. DA is involved in both motor control and in the rewarding and reinforcing effects of nicotine; however, the complete understanding of its molecular mechanisms is yet to be attained. Substantial evidence indicates that the reinforcing properties of drugs of abuse, including nicotine, can be affected by the nitric oxide (NO) system, which may act by modulating central dopaminergic function. In this study, using single cell recordings in vivo coupled with microiontophoresis and microdialysis in freely moving animals, the role of NO signaling on the hyperacti…
DNA binding and biological activity of Cu(II) and Zn(II) complexes of a 2,5-diphenyl[1,3,4]oxadiazole macrocycle ligand.
2011
Synthesis of Amino-1,2,4-triazoles by Reductive ANRORC Rearrangements of 1,2,4-Oxadiazoles
2010
The reaction of various 1,2,4-oxadiazoles with an excess of hydrazine in DMF has been investigated. 3-Amino- 1,2,4-triazoles are produced through a reductive ANRORC pathway consisting of the addition of hydrazine to the 1,2,4-oxadiazole followed by ring-opening, ring-closure, and final reduction of the 3-hydroxylamino-1,2,4-triazole intermediate. The general applicability of 1,2,4-oxadiazoles ANRORC reactivity is demonstrated also in the absence of C(5)-linked electron-withdrawing groups.