Search results for "evaluation"
showing 10 items of 1974 documents
Preclinical evidence of new opioid modulators for the treatment of addiction.
2010
Addiction to opiates is one of the most severe forms of substance dependence, and despite a variety of pharmacological approaches to treat it, relapse is observed in a high percentage of subjects. New pharmacological compounds are necessary to improve the outcome of treatments and reduce adverse side effects. Moreover, drugs that act on the opioid system can also be of benefit in the treatment of alcohol or cocaine addiction. AREA COVERED BY THIS REVIEW: Recent preclinical studies of pharmacological agents for the treatment of opiate addiction (2008 to the present date).The reader will be informed of the latest drugs shown in animal models to modify dependence on opiates and the reinforcing…
Covalent binding of drug metabolites to DNA ? a tool of predictive value?
1980
The presently available data suggest at least some correlation between covalent binding of drug metabolites to DNA and carcinogenicity of that drug. More data, however, are needed to establish the predictability of covalent DNA binding assays for extrahepatic cancer. A covalent binding assay requires administration of radioactively labelled compound to the experimental animals; the availability of labelled compound and requirements as to radiochemical purity, chemical and biochemical stability are limiting the applicability of this procedure. Many technical pitfalls accompany covalent DNA binding assays. It is concluded that at the present time DNA binding assays do not represent routine pr…
Inkjet printing methodologies for drug screening
2010
We show for the first time a contactless, low-cost, and rapid drug screening methodology by employing inkjet printing for molecular dispensing in a microarray format. Picoliter drops containing a model substrate (D-glucose)/ inhibitor (D-glucal) couple were accurately dispensed on a single layer consisting of the enzymatic target (glucose oxidase) covalently linked to a functionalized silicon oxide support. A simple colorimetric detection method allowed one to prove the screening capability of the microarray with the possibility to assay with high reproducibility at the single spot level. Measurements of the optical signal as a function of concentration and of time verified the occurrence a…
Mildronate: An Antiischemic Drug for Neurological Indications
2005
Mildronate (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; meldonium, quaterine) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. Mildronate was designed to inhibit carnitine biosynthesis in order to prevent accumulation of cytotoxic intermediate products of fatty acid beta-oxidation in ischemic tissues and to block this highly oxygen-consuming process. Mildronate is efficient in the treatment of heart ischemia and its consequences. Extensive evaluation of pharmacological activities of mildronate revealed its beneficial effect on cerebral circulation disorders and central nervous system (CNS) functions. The drug is used in neurological clinics for the trea…
Targeting apoptosis in solid tumors: the role of bortezomib from preclinical to clinical evidence.
2007
The ubiquitin-proteasome pathway is the main proteolytic system present in the nucleus and cytoplasm of all eukaryotic cells. Apoptosis activation induced by ubiquitin-proteasome pathway inhibition makes the proteasome a new target of anticancer therapy. Bortezomib is the first proteasome inhibitor to be approved by the US FDA; in 2003 as a third line and in 2005 as a second line therapy for the treatment of multiple myeloma only. This review focuses on the use of bortezomib, not only in its therapeutic role but also, more specifically, in its biologic role and discusses the most recent applications of the drug in solid tumors, both at a preclinical and clinical level.
Cell Lines: A Tool for In Vitro Drug Metabolism Studies
2008
Primary cultured hepatocytes are a valuable in vitro model for drug metabolism studies. However, their widespread use is greatly hindered by the scarcity of suitable human liver samples. Moreover, the well-known in vitro phenotypic instability of hepatocytes, the irregular availability of fresh human liver for cell harvesting purposes, and the high batch-to-batch functional variability of hepatocyte preparations obtained from different human liver donors, seriously complicate their use in routine testing. To overcome these limitations, different cell line models have been proposed for drug metabolism screening. Human liver-derived cell lines would be ideal models for this purpose given thei…
Le varietà di grano duro per le semine 2021. Sicilia
2021
Anche nel 2020-21, pur nelle difficili circostanze determinate per il secondo anno consecutivo dalla pandemia da Covid-19, sono state condotte in Sicilia le prove della Rete nazionale di confronto varietale di frumento duro. I campi sperimentali sono stati allestiti in 5 ambienti siciliani. La sperimentazione ha riguardato 30 varieta’, di cui ben 9 al primo anno di valutazione. I risultati produttivi riscontrati nelle diverse localita’ appaiono molto differenti e fortemente influenzati dall’andamento meteorologico verificatosi nelle diverse zone dell’Isola. At 2020-21, despite the difficult circumstances determined for the second consecutive year by the Covid-19 pandemic, the tests of the n…
Le varietà di grano duro per le semine 2020: Sicilia
2020
Nonostante le difficoltà operative dovute alla pandemia da Covid-19, anche nel corso del 2019-20 sono state condotte in Sicilia le prove di confronto varietale di frumento duro, allestite in 5 località della Sicilia: Libertinia (Catania), Catania, S. Stefano Quisquina (Agrigento), Caltagirone (Catania) e Ciminna (Palermo). La sperimentazione ha riguardato 30 varietà, di cui 5 al primo anno di valutazione, 9 cultivar al secondo anno di prova e 16 genotipi testati da oltre due anni. La resa media dell’areale siciliano è stata pari a 6,11 t/ha e i risultati produttivi registrati nei diversi ambienti di prova appaiono sensibilmente influenzati dall’andamento termo-pluviometrico. Despite the dif…
Sealing ability of five different retrograde filling materials.
1996
The sealing ability of Amalgam, Harvard-Cement, Diaket, gold-leaf, and Ketac-Endo as retrofilling materials was investigated. Paper cones were fixed with Harvard-Cement in the instrumented roots of 100 extracted human incisors. Apicectomy was performed and a 2-mm-deep retrograde cavity was prepared. Teeth were assigned to five groups (n = 20); each group received a different filling material. Surfaces of the roots were isolated with nail polish. Teeth, were stored in 1% methylene blue dye for 72 h. Roots were sectioned, and the depth of dye penetration was evaluated through a stereomicroscope. Retrofills with Ketac-Endo showed significantly less leakage compared with amalgam. There was no s…
Both Short- and Long-Acting D-1/D-2 Dopamine Agonists Induce Less Dyskinesia than l-DOPA in the MPTP-Lesioned Common Marmoset (Callithrix jacchus)
2002
Abstract The current concept of dyskinesia is that pulsatile stimulation of D-1 or D-2 receptors by l -DOPA or short-acting dopamine agonists is more likely to induce dyskinesia compared to long-acting drugs producing more continuous receptor stimulation. We now investigate the ability of two mixed D-1/D-2 agonists, namely pergolide (long-acting) and apomorphine (short-acting), to induce dyskinesia in drug-naive MPTP-lesioned primates, compared to l -DOPA. Adult common marmosets ( Callithrix jacchus ) were lesioned with MPTP (2 mg/kg/day sc for 5 days) and subsequently treated with equieffective antiparkinsonian doses of l -DOPA, apomorphine, or pergolide for 28 days. l -DOPA, apomorphine, …