Excitatory actions of adenosine on ventricular automaticity.

abstract：:The NLRP3 inflammasome is an intracellular multimeric protein complex which plays an important role in the pathogenesis of various human inflammatory diseases, such as diabetes, Alzheimer's disease and atherosclerosis. Recently, various G protein-coupled receptors (GPCRs) have been reported to be involved in the activ...

journal_title：Trends in pharmacological sciences

authors： Tang T,Gong T,Jiang W,Zhou R

更新日期：2018-09-01 00:00:00

abstract：:5-Hydroxytryptamine (5-HT), dopamine and norepinephrine are important monoamine neurotransmitters implicated in multiple brain mechanisms and regulated by high-affinity transmembrane monoamine transporters. Although knockout mice lacking 5-HT, dopamine or norepinephrine transporters are widely used to assess brain mon...

journal_title：Trends in pharmacological sciences

authors： Kalueff AV,Ren-Patterson RF,Murphy DL

更新日期：2007-03-01 00:00:00

abstract：:The characterization of P2 gamma purinoceptors on vascular endothelial cells has progressed rapidly since their existence was first demonstrated in 1983. They transduce the actions of extracellular ATP and ADP--endothelium-dependent relaxation, prostacyclin synthesis, endothelial cell mitogenesis--which play a vital r...

journal_title：Trends in pharmacological sciences

authors： Boeynaems JM,Pearson JD

更新日期：1990-01-01 00:00:00

abstract：:Recent developments in genetic research using Saccharomyces cerevisiae have provided rapid new methods for identifying the genes that control cellular responses to treatment with a wide variety of agents, including chemicals and radiation. This significantly increases the power of yeast as a model system for studying ...

journal_title：Trends in pharmacological sciences

authors： Game JC

更新日期：2002-10-01 00:00:00

abstract：:Five subtypes of muscarinic acetylcholine receptors have been identified in mammalian tissues, but the selectivity of ligands that are active at these receptors is low. It is possible, however, that selective compounds may be developed by targeting their allosteric site(s). Important new insights into the mechanism of...

journal_title：Trends in pharmacological sciences

authors： Tucek S,Proska J

更新日期：1995-06-01 00:00:00

abstract：:Mechanisms of opioid tolerance have focused on adaptive modifications within cells containing opioid receptors, defined here as cellular allostasis, emphasizing regulation of the opioid receptor signalosome. We review additional regulatory and opponent processes involved in behavioral tolerance, and include mechanisti...

journal_title：Trends in pharmacological sciences

authors： Cahill CM,Walwyn W,Taylor AMW,Pradhan AAA,Evans CJ

更新日期：2016-11-01 00:00:00

abstract：:Zn(2+) is the second most prevalent trace element in the body and is present in particularly large concentrations in the mammalian brain. Although Zn(2+) is a cofactor for many enzymes in all tissues, a unique feature of brain Zn(2+) is its vesicular localization in presynaptic terminals, where its release is dependen...

journal_title：Trends in pharmacological sciences

authors： Weiss JH,Sensi SL,Koh JY

更新日期：2000-10-01 00:00:00

abstract：:Daily rhythms in behavior, physiology, and metabolism are an integral part of homeostasis. These rhythms emerge from interactions between endogenous circadian clocks and ambient light-dark cycles, sleep-activity cycles, and eating-fasting cycles. Nearly the entire primate genome shows daily rhythms in expression in ti...

journal_title：Trends in pharmacological sciences

authors： Sulli G,Manoogian ENC,Taub PR,Panda S

更新日期：2018-09-01 00:00:00

abstract：:Nearly all molecules known to signal cells via G proteins have been assigned a cloned G-protein-coupled-receptor (GPCR) gene. This has been the result of a decade-long genetic search that has also identified some receptors for which ligands are unknown; these receptors are described as orphans (oGPCRs). More than 80 o...

journal_title：Trends in pharmacological sciences

authors： Marchese A,George SR,Kolakowski LF Jr,Lynch KR,O'Dowd BF

更新日期：1999-09-01 00:00:00

abstract：:Until recently, release studies have failed to indicate the existence of autoreceptors on motor nerves. Ignaz Wessler now reports on a refinement of the technique - the measurement of newly synthesized [3H]acetylcholine released from the phrenic nerve - which provides clear evidence in support of release-modulating au...

journal_title：Trends in pharmacological sciences

authors： Wessler I

更新日期：1989-03-01 00:00:00

abstract：:Cyclic AMP (cAMP) steers the generation of basal heart beat in the sinoatrial node. It also induces sinoatrial tachycardia and increased cardiac force, elicited through activation of Gs-protein-coupled receptors (GsPCRs). Phosphodiesterases (PDEs) hydrolyse cAMP. In the heart mainly PDE3 and PDE4 would be expected to ...

journal_title：Trends in pharmacological sciences

authors： Kaumann AJ

更新日期：2011-07-01 00:00:00

abstract：:The disruption of large protein-protein (PP) interfaces remains a challenge in targeted therapy. Designing drugs that compete with binding partners is daunting, especially when the structure of the protein complex is unknown. To address the problem we propose a deep protein databank (PDB) learning platform to discover...

journal_title：Trends in pharmacological sciences

authors： Fernández A

更新日期：2019-08-01 00:00:00

abstract：:Gastroesophageal reflux disease (GERD) is very common and advances in drug development over recent years have markedly improved GERD management. A wide range of medications are currently used in GERD treatment, including antacids, Gaviscon, sucralfate, histamine-2 receptor antagonists and prokinetics. However, proton ...

journal_title：Trends in pharmacological sciences

authors： Hershcovici T,Fass R

更新日期：2011-04-01 00:00:00

abstract：:The genotoxicity of the most potent carcinogen in cigarette smoke [4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)] is dependent on the relationship between its activation by cytochrome P450 enzymes and its detoxification by carbonyl reduction to NNK alcohol (NNAL) followed by glucuronidation. Recently, '11 beta-...

journal_title：Trends in pharmacological sciences

authors： Maser E

更新日期：1997-08-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) have been considered for treatment and prevention of Alzheimer's disease (AD) for more than two decades. Biochemical markers in the brains of individuals with AD suggest that inflammation might be a driving cause of the disease that can be suppressed by drug treatment. In...

journal_title：Trends in pharmacological sciences

authors： Weggen S,Rogers M,Eriksen J

更新日期：2007-10-01 00:00:00

abstract：:Current medicines for the clinical management of inflammatory diseases act by inhibiting specific enzymes or antagonising specific receptors or blocking their ligands. In the past decade, a new paradigm in our understanding of the inflammatory process has emerged with the appreciation of genetic, molecular, and cellul...

journal_title：Trends in pharmacological sciences

authors： Perretti M,Leroy X,Bland EJ,Montero-Melendez T

更新日期：2015-11-01 00:00:00

abstract：:Advances in the understanding of the sense of smell have increased awareness of the role of olfaction in human life. Odors are perceived via specific G protein-coupled receptors (GPCRs) with cAMP as the second messenger. Drugs that interact with this signaling cascade, such as opioids, cannabinoids and sildenafil, are...

journal_title：Trends in pharmacological sciences

authors： Lötsch J,Geisslinger G,Hummel T

更新日期：2012-04-01 00:00:00

abstract：:Neuromodulin is a neurospecific calmodulin binding protein that is implicated in neurite extension, axonal elongation and long-term potentiation. Yuechueng Liu and Daniel Storm propose that neuromodulin binds and concentrates calmodulin on growth cone membranes and that stimulation of protein kinase C releases high lo...

journal_title：Trends in pharmacological sciences

authors： Liu YC,Storm DR

更新日期：1990-03-01 00:00:00

abstract：:Intercellular transfer of proteins is a mode of communication between cells that is crucial for certain physiological processes. Chemotherapy is the treatment of choice for approximately 50% of all cancers. However, multidrug resistance mediated by drug-efflux pumps such as P-glycoprotein (Pgp) minimizes the effective...

journal_title：Trends in pharmacological sciences

authors： Ambudkar SV,Sauna ZE,Gottesman MM,Szakacs G

更新日期：2005-08-01 00:00:00

abstract：:The enzyme methylenetetrahydrofolate reductase (MTHFR) directs folate species either to DNA synthesis or to homocysteine (Hcy) remethylation. The common MTHFR C677T polymorphism affects the activity of the enzyme and hence folate distribution. Under conditions of impaired folate status, the homozygous TT genotype has ...

journal_title：Trends in pharmacological sciences

authors： Ueland PM,Hustad S,Schneede J,Refsum H,Vollset SE

更新日期：2001-04-01 00:00:00

abstract：:Recent molecular cloning studies have identified several genes encoding alpha and beta subunits of the nicotinic acetylcholine receptor. These genes have distinct, although overlapping, patterns of expression in the brain and peripheral ganglia. Multiple nicotinic receptors with distinct pharmacological and functional...

journal_title：Trends in pharmacological sciences

authors： Deneris ES,Connolly J,Rogers SW,Duvoisin R

更新日期：1991-01-01 00:00:00

abstract：:During the past decade remarkable progress in molecular genetics and the possibility of manipulating cells so that the expression of genes can directly 'report' on drug activity has produced major changes in drug development strategies. The recent description and pharmacological validation of reporter mice for in vivo...

journal_title：Trends in pharmacological sciences

authors： Maggi A,Ottobrini L,Biserni A,Lucignani G,Ciana P

更新日期：2004-06-01 00:00:00

abstract：:The 5-hydroxytryptamine (5-HT)(2C) receptor has received considerable attention as a target for treating drug addiction. 5-HT(2C)-receptor agonism, however, also induces side-effects. In this article, we review recent findings regarding the involvement of 5-HT(2C) receptors in behaviours related to drug addiction in a...

journal_title：Trends in pharmacological sciences

authors： Müller CP,Carey RJ

更新日期：2006-09-01 00:00:00

abstract：:Salvinorin A, a neoclerodane diterpene, is the most potent naturally occurring hallucinogen known and rivals the synthetic hallucinogen lysergic acid diethylamide in potency. Recently, the molecular target of salvinorin A was identified as the kappa opioid receptor (KOR). Salvinorin A represents the only known non-nit...

journal_title：Trends in pharmacological sciences

authors： Sheffler DJ,Roth BL

更新日期：2003-03-01 00:00:00

abstract：:The United States is experiencing an epidemic of opioid overdose deaths. Many of the recent fatalities are associated with illicitly manufactured fentanyl, which is being added to heroin and counterfeit pain pills. The crisis is further exacerbated by the emergence of an increasing number of novel synthetic opioids (N...

journal_title：Trends in pharmacological sciences

authors： Baumann MH,Kopajtic TA,Madras BK

更新日期：2018-12-01 00:00:00

abstract：:Chronic inflammation is the basis of various chronic illnesses including cancer and vascular diseases. However, much has yet to be learned how inflammation becomes chronic. Prostaglandins (PGs) are well established as mediators of acute inflammation, and recent studies in experimental animals have provided evidence th...

journal_title：Trends in pharmacological sciences

authors： Aoki T,Narumiya S

更新日期：2012-06-01 00:00:00

abstract：:The hypothalamic neuropeptide oxytocin (OT) has attracted the attention both of the scientific community and a general audience because of its prosocial effects in mammals, and OT is now seen as a facilitator of mammalian species propagation. Furthermore, OT is a candidate for the treatment of social deficits in sever...

journal_title：Trends in pharmacological sciences

authors： Chini B,Verhage M,Grinevich V

更新日期：2017-11-01 00:00:00

abstract：:The discovery of neuropeptides as signaling molecules with paracrine or hormonal regulatory functions has led to trailblazing advances in physiology and fostered the characterization of numerous neuropeptide-binding G protein-coupled receptors (GPCRs) as potential drug targets. The impact on human health has been trem...

journal_title：Trends in pharmacological sciences

authors： Romanova EV,Sweedler JV

更新日期：2015-09-01 00:00:00

abstract：:For almost 70 years, children have received stimulants for the treatment of attention deficit hyperactivity disorder [ADHD (initially called hyperkinetic syndrome)], with little understanding of the long-term effects of these drugs on brain development. The maturation and refinement of the brain during childhood and a...

journal_title：Trends in pharmacological sciences

authors： Andersen SL

更新日期：2005-05-01 00:00:00

abstract：:The metabotropic glutamate type 7 (mglu(7)) receptor is a widely distributed, mainly presynaptic Group III mglu receptor that can regulate glutamate release. Recently, largely as a result of the identification of specific proteins that interact with the C-terminal domain of this receptor, considerable progress has bee...

journal_title：Trends in pharmacological sciences

authors： Dev KK,Nakanishi S,Henley JM

更新日期：2001-07-01 00:00:00