Search results for "Drugs"

Development and biological investigations of hypoxia-sensitive prodrugs of the tyrosine kinase inhibitor crizotinib

2019

Despite the huge success of tyrosine kinase inhibitors as anticancer agents, severe side effects are a major problem. In order to overcome this drawback, the first hypoxia-activatable 2-nitroimidazole-based prodrugs of the clinically approved ALK and c-MET inhibitor crizotinib were developed. The 2-aminopyridine functionality of crizotinib (essential for target kinase binding) was considered as ideal position for prodrug derivatization. Consequently, two different prodrugs were synthesized with the nitroimidazole unit attached to crizotinib either via carbamoylation (A) or alkylation (B) of the 2-aminopyridine moiety. The successful prodrug design could be proven by docking studies and a dr…

Anti-endothelin drugs in solid tumors

2010

Importance of the field: The endothelin (ET) axis, which includes the biological functions of ETs and their receptors, has played a physiological role in normal tissue, acting as a modulator of vasomotor tone, tissue differentiation and development, cell proliferation and hormone production. Interestingly, it also functions in the growth and progression of various tumors. Several researchers have identified the blockade of the ET-1 receptor as a promising therapeutic approach. Areas covered in this review: The clinical investigation of an orally bioavailable ET antagonist, atrasentan, in prostate cancer, is encouraging. In this neoplasia, it has shown antitumor activity, bone metastasis con…

Effects of Different Anxiety Levels on the Behavioral Patternings Investigated through T-pattern Analysis in Wistar Rats Tested in the Hole-Board App…

2021

The Hole-Board is an ethologically based tool for investigating the anxiety-related behavior of rats following manipulation of the central anxiety level. The present paper aims to assess behavioral patterning following pharmacological manipulation of emotional assets in Wistar rats tested in this experimental apparatus. For this purpose, the behavior of three groups of rats injected with saline, diazepam or FG7142 was evaluated using conventional quantitative and multivariate Tpattern analyses. The results demonstrate that quantitative analyses of individual components of the behavior, disjointed from the comprehensive behavioral structure, are of narrow utility in the understanding of the …

Traditional Chinese medicine research in the post-genomic era: good practice, priorities, challenges and opportunities.

2012

Abstract Background and aims GP-TCM is the 1st EU-funded Coordination Action consortium dedicated to traditional Chinese medicine (TCM) research. This paper aims to summarise the objectives, structure and activities of the consortium and introduces the position of the consortium regarding good practice, priorities, challenges and opportunities in TCM research. Serving as the introductory paper for the GP-TCM Journal of Ethnopharmacology special issue, this paper describes the roadmap of this special issue and reports how the main outputs of the ten GP-TCM work packages are integrated, and have led to consortium-wide conclusions. Materials and methods Literature studies, opinion polls and di…

Level of response and safety of pharmacological monotherapy in the treatment of acute bipolar I disorder phases: a systematic review and meta-analysi…

2010

In recent years, combinations of pharmacological treatments have become common for the treatment of bipolar disorder type I (BP I); however, this practice is usually not evidence-based and rarely considers monotherapy drug regimen (MDR) as an option in the treatment of acute phases of BP I. Therefore, we evaluated comparative data of commonly prescribed MDRs for both manic and depressive phases of BP I. Medline, PsycINFO, EMBASE, the Cochrane Library, the ClinicalStudyResults.org and other data sources were searched from 1949 to March 2009 for placebo and active controlled randomized clinical trials (RCTs). Risk ratios (RRs) for response, remission, and discontinuation rates due to adverse …

The impact of psychopharmacology on contemporary clinical psychiatry.

2014

Clinical psychiatric evaluations of patients have changed dramatically in recent decades. Both initial assessments and follow-up visits have become brief and superficial, focused on searching for categorical diagnostic criteria from checklists, with limited inquiry into patient-reported symptomatic status and tolerability of treatments. The virtually exclusive therapeutic task has become selecting a plausible psychotropic, usually based on expert consensus guidelines. These guidelines and practice patterns rest mainly on published monotherapy trials that may or may not be applicable to particular patients but are having a profound impact, not only on modern psychiatric practice but also on…

Psychiatric and behavioural symptoms and the use of psychotropic medication in Special Care Units and Regular Units in Norwegian nursing homes

2008

Background:  In a number of countries Special Care Units (SCUs) have been established to meet the particular needs of patients with dementia. The criteria for SCUs are poorly defined and often not met. Aim:  To assess the frequency distributions of dementia, psychiatric and behavioural symptoms and the use of psychotropic medication in SCUs and Regular Units (RUs) across different regions. Methods and material:  By means of a structured interview, comprising the Neuropsychiatric Inventory, the Clinical Dementia Rating Scale and Lawton’s Physical Self-maintenance scale, a representative sample of 1163 nonselected nursing home patients was assessed. In addition, information was collected from…

The necessity of placebo application in psychotropic drug trials.

1990

MORBILIDAD PSÍQUICA, EXISTENCIA DE DIAGNÓSTICO Y CONSUMO DE PSICOFÁRMACOS. DIFERENCIAS POR COMUNIDADES AUTÓNOMAS SEGÚN LA ENCUESTA NACIONAL DE SALUD …

2010

Background: Most of the studies on sychological distress in Spain have been conducted in small geographical areas or specific population groups. However, there are no studies that provide representative data for each Autonomous Community (AC). The objectives of this paper are to determine, both in Spain and in the AC, the prevalence of psychological distress, diagnosis, use of psychoactive medication, social support and self-perceived health, as well as to study the association between psychological distress and the rest of the variables. Methods: Cross-sectional study, using data from the 2006 National Health Survey, that was completed by 29,478 persons. Variables studied: sociodemographic…

Cocaine and MDMA Induce Cellular and Molecular Changes in Adult Neurogenic Systems: Functional Implications

2011

The capacity of the brain to generate new adult neurons is a recent discovery that challenges the old theory of an immutable adult brain. A new and fascinating field of research now focuses on this regenerative process. The two brain systems that constantly produce new adult neurons, known as the adult neurogenic systems, are the dentate gyrus (DG) of the hippocampus and the lateral ventricules/olfactory bulb system. Both systems are involved in memory and learning processes. Different drugs of abuse, such as cocaine and MDMA, have been shown to produce cellular and molecular changes that affect adult neurogenesis. This review summarizes the effects that these drugs have on the adult neurog…