Abstract:
:It has long been suggested that some of the neuropharmacological, neurochemical and behavioural effects of ethanol are mediated by its first metabolite, acetaldehyde. In spite of the well documented psychoactivity of acetaldehyde, the precise role of this compound in alcohol abuse remains a matter of intense debate among scientists devoted to the study of alcoholism. Very frequently, the main drawback has been related to the presence of adequate levels of acetaldehyde or its derivatives inside the brain after ethanol ingestion. Since penetration into the central nervous system from blood of peripherically derived acetaldehyde is very low due to the high aldehyde dehydrogenase activity at the blood-brain barrier, several authors called into question the acetaldehyde implication in the toxicity and neurobehavioral effects of ethanol. The confirmation in several laboratories of the existence of enzymatic mechanisms of ethanol oxidation in the brain has revitalized the old theories supporting the acetaldehyde contribution to alcohol abuse and alcoholism. In this paper, we review current data on the brain metabolism of ethanol. We focused on the description of the enzymatic mechanisms involved in this metabolic process, reviewing the constitutive expression, catalytic activity and inhibition and inducibility of the enzymes involved in brain ethanol metabolism. We also analyze old and recent data on their regional distribution and cellular localization in the central nervous system, with special reference to the mesocorticolimbic system, a dopaminergic brain pathway that plays an important role in drug and ethanol reinforcement.
journal_name
Curr Drug Metabjournal_title
Current drug metabolismauthors
Hipólito L,Sánchez MJ,Polache A,Granero Ldoi
10.2174/138920007782109797subject
Has Abstractpub_date
2007-10-01 00:00:00pages
716-27issue
7eissn
1389-2002issn
1875-5453journal_volume
8pub_type
杂志文章,评审abstract::Brain, the centre of the nervous system and an integral part the body, is protected by two anatomical and physiological barriers- Blood-Brain Barrier (BBB) and Blood-Cerebrospinal Fluid Barrier (BCSFB). Blood-Brain Barrier is a very complex and highly organized multicellular structure that shields the brain from harmf...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200218666170113125132
更新日期:2017-01-01 00:00:00
abstract::Graphene possesses a wide range of potential biomedical applications because of the unique physical and chemical properties. However, the side effects of grapheme and its derivatives on a number of biological models even on human body are still not very clear. Therefore, to properly assess the potential risk of graphe...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920021131400108
更新日期:2013-10-01 00:00:00
abstract:OBJECTIVES:Induction or inhibition of cytochrome P450 (CYP) enzyme activities, enzymes that activate or detoxify xenobiotics, is one mechanism by which vegetables may alter cancer risk. As the effect of food on CYP enzyme activities have not been studied in the Jordanian population, we examined the effect of supplement...
journal_title:Current drug metabolism
pub_type: 临床试验,杂志文章
doi:10.2174/138920007779315080
更新日期:2007-01-01 00:00:00
abstract::We report here a comprehensive evaluation of the effects of culture duration on the gene expression of P450 isoforms, uptake transporters and efflux transporters in human hepatocyte cultured in the absence and presence of the prototypical proinflammatory cytokine, interleukin-6 (IL-6). Primary collagen-matrigel sandwi...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/138920012802138570
更新日期:2012-09-01 00:00:00
abstract:BACKGROUND:Mutation in the B RAF at V600E has been well implicated in the carcinogenesis that makes it as an attractive therapeutictarget. In the present study, we sought to identify the basis of V600E mutation at functional and structural grounds. The study also endeavors in identification of small molecule as a poten...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1389200218666170503114611
更新日期:2017-07-21 00:00:00
abstract:BACKGROUND:Drug-induced cholestasis is a risk factor in the progression of drug candidates, and poses a serious health hazard if not detected before going into a human. Intrahepatic accumulation of Bile Acids (BAs) represents a characteristic phenomenon associated with drug-induced cholestasis. METHODS:This review wil...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200219666180427165035
更新日期:2018-01-01 00:00:00
abstract::We present a review of recent investigations of anticancer drug bexarotene in this article. As one of the novel synthetic analogs of retinoids, bexarotene selectively binds to and activates the retinoid X receptor (RXRs) subfamilies, exerting a prophylactic and therapeutic effect on a large series of tumors in vitro a...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920021702160114121706
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Nobel laureate Sir James Black's molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of prop...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1389200221666200414094644
更新日期:2020-01-01 00:00:00
abstract::Arachidonic acid (AA) is metabolized by enzymes of the cytochrome P450 (CYP) 4A and CYP4F subfamilies to 20- hydroxyeicosatetraeonic acid (20-HETE), which plays an important role in the cardiovascular system. In the current work, we reviewed the formation of 20-HETE in different species by different CYPs; 20-HETE meta...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200211314060007
更新日期:2013-07-01 00:00:00
abstract::Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920011796504527
更新日期:2011-09-01 00:00:00
abstract::The possibility to treat central nervous system (CNS) disorders is strongly limited by the poor access of many therapeutic agent to the target tissues. This is mainly due to the presence of the blood-brain barrier (BBB), formed by a complex interplay of endothelial cells, astrocyte and pericytes, through which only se...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920012798356943
更新日期:2012-01-01 00:00:00
abstract::In the recent decades, the use of herbal products has been rapidly growing in the Western countries. While their use in many cases causes adverse effects, to date, safety issues of herbal products have not been adequately addressed. It is rarely determined whether the non-purported bioactive constituents in the herbs ...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920011797470119
更新日期:2011-11-01 00:00:00
abstract::In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole a...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920007781368908
更新日期:2007-08-01 00:00:00
abstract:BACKGROUND:Neuropsychiatric diseases primarily characterized by dementia stand third in the global list of diseases causing disability. The poor water solubility, erratic oral absorption, low bioavailability, poor intestinal absorption, and the impeding action of the blood-brain barrier (BBB) are the major factors limi...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1573399816666200627214129
更新日期:2020-01-01 00:00:00
abstract::The combined treatment with anticonvulsant and antidepressant drugs is reported in both neurologic and psychiatric practice; it is, therefore, evident that the issue of managing such type of polytherapy is frequently encountered by clinicians. To review current literature on pharmacokinetic interactions between antico...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920008786049311
更新日期:2008-10-01 00:00:00
abstract:BACKGROUND:Medical application of nanotechnology is termed as Nanomedicine and is widely used in healthcare industries. Nanotechnology has helped Physicians, Scientists and Technologists to understand the changes in cellular levels to develop nanomedicines and address the challenges faced by the healthcare sectors. Nan...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200219666180305154119
更新日期:2018-01-01 00:00:00
abstract:: ...
journal_title:Current drug metabolism
pub_type: 社论
doi:10.2174/138920022006190617104713
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Wound healing is a composite and vital process in which devitalized tissue layers and cellular structures repair themselves. Bronchiolitis is generally prompted by respiratory syncytial virus or human metapneumovirus; this condition is an acute inflammatory injury of bronchioles. Heart problems that develop ...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200217666151210124713
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Colorectal cancer is the third important cause of cancer-associated deaths across the world. Hence, there is an urgent need for understanding the complete mechanism associated with colorectal cancer, which in turn can be utilized toward early detection as well as the treatment of colorectal cancer in humans....
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200220666191007153238
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Drug-metabolizing enzymes and transporters play key roles in drug disposition and drug interactions. The alterations of their expression will influence drug pharmacokinetics and pharmacodynamics. However, the changes in the expression of enzymes and transporters in the disease state are still unclear. OBJEC...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1389200221666200512113731
更新日期:2020-01-01 00:00:00
abstract::The in vivo hepatic clearance of tanshinone IIA in the rat was predicted using microsome, cytosol and S9 fractions combined with two different cofactor systems, NADPH-regenerating and UDPGA system. Two different models, the well stirred model and the parallel-tube model, were used in predicting the in vivo clearance i...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/138920008783331103
更新日期:2008-01-01 00:00:00
abstract::Talin is an intracellular cytoskeletal protein and one of the major components of the focal adhesion complex. It mainly acts as an interlink between transmembrane integrin receptors and cytosolic F-actin. Apart from integrins and actin, it also interacts with various other proteins in the adhesion complex to regulate ...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1389200221666200214114018
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:The metabolic/biotransformation pathways of atypical antipsychotics (aripiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, and ziprasidone) have been characterized and reviewed. However, comparisons of excretory pathways remain unexplored. OBJECTIVE:To analyze the excretio...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920010791636202
更新日期:2010-07-01 00:00:00
abstract::Work on human immortalized cell lines is not considered research on human subjects, but does involve biohazards. It has also been estimated that about 80% of human cell lines are the kind of cells that they are expected. Cells that are cultured directly from a subject are referred to as primary cells. Clonetics is the...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/138920008783884768
更新日期:2008-03-01 00:00:00
abstract:BACKGROUND:Despite recent therapeutic advances, osteoarthritis continues to be a challenging health problem, especially in the elderly population. Opioids, which are potent analgesics, have shown an extraordinary ability to reduce intense pain in many osteoarthritic clinical trials; however, there is an increased need ...
journal_title:Current drug metabolism
pub_type: meta分析
doi:10.2174/1389200221666200514130441
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Clinical studies during pregnancy are rare due to ethical and practical limitations. Giving pregnant females the same dosing regimen used in adult males or nonpregnant females is inappropriate. Pregnancy physiologically-based pharmacokinetic modeling is a powerful tool that can be used to refine pharmacother...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200219666180702104034
更新日期:2018-01-01 00:00:00
abstract::For the pharmaceutical industry, one of the challenges in evaluating the risk of future compound attrition at the discovery stage is the successful prediction of the major routes of clearance in humans. For compounds cleared by metabolism, such information will help to avoid the development of compounds that will exhi...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200033489235
更新日期:2003-12-01 00:00:00
abstract::Membrane transporters play an important role in intestinal absorption, distribution and clearance of drugs. Additionally transporters along with enzymes regulate tissue exposures (e.g. liver, kidney and brain), which are important for safety and efficacy considerations. Early identification of transporters involved gu...
journal_title:Current drug metabolism
pub_type: 杂志文章
doi:10.2174/1389200221999210101233340
更新日期:2021-01-01 00:00:00
abstract:BACKGROUND:The administration of multiple drugs for the treatment of diseases is an integral aspect of modern medicine. Though its purpose is to create the intended therapeutic effect, the unintended consequences of drug interactions can cause severe side effects and subsequent economic losses. Likewise, herbal extract...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/1389200216666151103121253
更新日期:2016-01-01 00:00:00
abstract::Fluoropyrimidines and oxaliplatin continued to be the mainstay of therapeutic regimens in the treatment of colorectal cancer (CRC). For this reason, pharmacokinetic and metabolism of these drugs were analyzed and the identification of accurate and validated predictive, prognostic and toxicity markers became necessary ...
journal_title:Current drug metabolism
pub_type: 杂志文章,评审
doi:10.2174/138920011798062300
更新日期:2011-12-01 00:00:00