Abstract:
:The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to provide sustained clinical benefit for a long period due to the appearance of side-effects such as augmentation, sleepiness, nausea, hypothension, and compulsive behaviors among others. New dopaminergic agonists with less side effects are being developed. These novel compounds offer an alternative when the disease progresses and patients fail to respond to standard dopaminergic treatments or side-effects increased. Chemistry, and in particular chemical synthesis, has played a major role in bringing synthetic dopaminergic agonists to the clinic and continues to be crucial for the development of new and necessary drugs for long-term treatments with less undesired side effects. A number of structural modifications of parent compounds have led to enhanced agonism but also partial agonism or even antagonism of one or more dopamine receptors. In some cases, these activities are accompanied by agonist effect at serotonin receptors which suggests a potential clinical application in the treatment of schizophrenia In this review, chemical synthesis of dopaminergic agents, their affinity, and the corresponding agonist/antagonist effects will be highlighted.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Matute MS,Matute R,Merino Pdoi
10.2174/0929867323666160504103621subject
Has Abstractpub_date
2016-01-01 00:00:00pages
2790-2825issue
25eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-75388journal_volume
23pub_type
杂志文章,评审abstract::Now cisplatin and its analogs are some of the most effective chemotherapeutic agents in clinical use as the first line of treatment in testicular and ovarian cancers. Unfortunately, they have several major drawbacks, such as cumulative toxicities of nephrotoxicity and ototoxicity, inherent or treatment-induced resista...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712800672067
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Chronic Liver Disorders (CLD), caused by the lifestyle patterns like alcoholism or by non-alcoholic fatty liver disease or because of virus-mediated hepatitis, affect a large population fraction across the world. CLD progresses into end-stage diseases with a high mortality rate. Liver transplant is the only ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666191004161802
更新日期:2020-01-01 00:00:00
abstract::Breast cancer arises in about 48% of patients older than 65 years and more than 30% occurs in those over 70 years being the leading cause of cancer-related death in women older than 65. Elderly patients tolerate chemotherapy poorly compared to their younger counterpart because of progressive reduction of organ functio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867053363261
更新日期:2005-01-01 00:00:00
abstract::A comprehensive outline for understanding and recommending the therapeutic use of ozone in combination with established therapy in diseases characterized by a chronic oxidative stress is currently available. The view of the absolute ozone toxicity is incorrect, because it has been based either on lung or on studies pe...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666151221150420
更新日期:2016-01-01 00:00:00
abstract::Receptor-binding peptides have attracted an enormous interest in targeting molecules for the development of tumour specific radiopharmaceutical compounds. The overexpression of many receptors on human tumour makes such peptide-ligands attractive agents for diagnostic imaging and therapy of cancers. The use of solid-ph...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/092986710791859388
更新日期:2010-01-01 00:00:00
abstract::Semicarbazide-sensitive amine-oxidase (SSAO) is present in various human tissues and in plasma. Oxidative deamination of short-chain aliphatic amines is catalyzed by this enzyme to afford the corresponding aldehydes, ammonia and hydrogen peroxide. Methylamine and aminoacetone have been recognized to be physiological s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043365305
更新日期:2004-05-01 00:00:00
abstract::The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:The therapeutic properties of cannabinoids are well-known since ancient years. Growing evidence exist on endocannabinoid system (ECS) modulation related with human tumorigenesis. OBJECTIVE:Taking into account the substantial role of ECS on immune cell regulation, the present review is aimed to summarize the...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160530144934
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. OBJECTIVE:Following a literature survey, we disc...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666200505092514
更新日期:2020-01-01 00:00:00
abstract::Human immunodeficiency virus (HIV) infection commonly results in a myriad of comorbid conditions secondary to immune deficiency. Infection also affects broad organ system function. Although current antiretroviral therapy (ART) reduces disease morbidity and mortality through effective control of peripheral viral load, ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666140826114135
更新日期:2014-01-01 00:00:00
abstract::Vitamins are dietary components which are necessary for life. They play a major role in health and their deficiency may be linked to symptoms of psychiatric disorders. B vitamins are required for proper functioning of the methylation cycle, monoamine oxidase production, DNA synthesis and the repair and maintenance of ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160920110810
更新日期:2016-01-01 00:00:00
abstract::HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounde...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711794839142
更新日期:2011-01-01 00:00:00
abstract::The discovery of the high-affinity, high-specificity folate receptor in mamalian kidney cells, coupled with the ability of folate to enter cells by folate receptor-mediated endocytosis and the subsequent elucidation of the folate receptor's overexpression in specific cancer cell types; heralded the arrival of the area...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180209143715
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Serotonin reuptake inhibitors (SRIs) and cognitive-behavioral psychotherapy (CBT) are first-line treatments for obsessive-compulsive disorder (OCD). Since response is often inadequate, in recent years researchers investigated whether combining CBT and SRIs, either ab initio or sequentially, results in a grea...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170712114445
更新日期:2018-01-01 00:00:00
abstract::Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867023371030
更新日期:2002-02-01 00:00:00
abstract::Hereditary amyloidogenic transthyretin (TTR) (ATTR) amyloidosis is an autosomal dominant form of fatal hereditary amyloidosis. Owing to progress in biochemical and molecular genetic analyses, this disease is now believed to occur worldwide. As of today, reports of about 120 different points of single or double mutatio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712800269317
更新日期:2012-01-01 00:00:00
abstract::Many of the currently available treatments for obsessive-compulsive and related disorders (OCRDs) such as pharmacotherapy augmentation strategies, partial hospitalization programs, deep brain stimulation, and neurosurgery are efficacious for individuals suffering from more severe forms of these conditions. Unfortunate...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180104150854
更新日期:2018-01-01 00:00:00
abstract::TB drug development pipeline represents varied structural classes of molecules. Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR. They act by inhibiting translation at the initiation phase of protein...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666151106125759
更新日期:2015-01-01 00:00:00
abstract::It is well accepted that inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is one of high risk factors for colorectal cancer (CRC). This supports the notion that inflammation plays a key role in cancer development. Epidemiologic studies have shown that vitamin D (Vit D) deficiency is ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867323666161202153028
更新日期:2017-01-01 00:00:00
abstract::The role of cell adhesion molecules (CAMs), such as intercellular cell adhesion molecule-1 (ICAM-1), vascular endothelial cell adhesion molecule-1 (VCAM-1), E-selectin, and P-selectin, has been studied extensively in the process of inflammation. These molecules are responsible for recruiting leukocytes onto the vascul...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707779941032
更新日期:2007-01-01 00:00:00
abstract:BACKGROUND:Pregnancy specific β1-glycoproteins (PSGs) have long been recognized as trophoblast quality and embryo viability markers. However, biological roles of PSGs remain obscure, and structure/function relationships to other feto-placental proteins as well as implications for drug design have not been reviewed. Thi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666161123090554
更新日期:2017-01-01 00:00:00
abstract::Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666171116124255
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Histone deacetylases (HDAC) are an important class of enzymes that play a pivotal role in epigenetic regulation of gene expression that modifies the terminal of core histones leading to remodelling of chromatin topology and thereby controlling gene expression. HDAC inhibitors (HDACi) counter this action and ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180530094120
更新日期:2019-01-01 00:00:00
abstract::There is increasing evidence that statins, inhibitors of 3-hydroxyl-3-methylglutaryl coenzyme A reductase, can effectively be used not only in the treatment of hypercholesterolemia, but also in other human disorders; indeed, statins have strong anti-inflammatory and immunomodulatory effects, so that they can influence...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711798184244
更新日期:2011-01-01 00:00:00
abstract::The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311320030009
更新日期:2013-01-01 00:00:00
abstract::Ten years elapsed since the discovery by Sanofi of SR141716A the first selective CB(1) cannabinoid receptor antagonist. Shortly after, Sanofi also reported the synthesis of the first selective CB(2) cannabinoid receptor antagonist, SR144528. Since these two milestones in the cannabinoid field, many other compounds, mo...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867054020891
更新日期:2005-01-01 00:00:00
abstract::Several lines of defense maintain the surface integrity of the delicate airway epithelium which is regularly subjected to severe trauma. These defense mechanisms include protection by the mucus layer, rapid repair by restitution (cell migration) and regeneration via proliferation and differentiation. Luminal surveilla...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2007-01-01 00:00:00
abstract::Multitarget-directed ligands (MTDLs), an emerging and appealing drug discovery strategy, utilizing a single chemical entity to inhibit multitargets, was confirmed to be effective in reducing the likelihood of drug resistance, diminishing problems of dosing complexity, drug-drug interactions and toxicities, as well as ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2013-01-01 00:00:00
abstract::The focus of this review is the cellular internalisation mechanism of nanostructured systems (NSs) and their endosomal escape for targeted drug delivery. Endocytosis is a cellular process of internalisation of different molecules and foreign microorganisms. It is currently being studied for drug delivery through nanos...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170214111205
更新日期:2017-01-01 00:00:00
abstract::In healthy individuals, natural and adaptive immune responses are able to control virus entry into the host. In particular, CD8(+)-mediated cytotoxicity, sustained by the intervention of CD4+ cells, represents the major key event leading to virus eradication. On the other hand, viruses are able to evade from host immu...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706775476106
更新日期:2006-01-01 00:00:00