Preclinical models of antipsychotic drug-induced metabolic side effects.

abstract：:For many years the prevailing view of how steroid hormone receptors exert their effects on gene transcription has been that these intracellular receptor proteins, upon association with their specific cognate ligands, undergo a transformation to a state where they are capable of interacting with chromatin and regulatin...

journal_title：Trends in pharmacological sciences

authors： Power RF,Conneely OM,O'Malley BW

更新日期：1992-08-01 00:00:00

abstract：:Pharmacology as a modern science was introduced in China approximately 150 years ago, and has been used since then to study traditional Chinese medicine (TCM). Pharmacology has experienced its own development over this time and continues to provide new tools for the study of TCM. In the present review, three models fo...

journal_title：Trends in pharmacological sciences

authors： Liu X,Wu WY,Jiang BH,Yang M,Guo DA

更新日期：2013-11-01 00:00:00

abstract：:The current classification for 5-HT2 receptors accommodates three subtypes. In addition to the originally defined 5-HT2 receptor, sanctuary is now provided for the structurally related 5-HT1c receptor (now 5-HT2c) and at least one atypical 5-HT receptor subtype. The strong functional union of this family is reflected ...

journal_title：Trends in pharmacological sciences

authors： Baxter G,Kennett G,Blaney F,Blackburn T

更新日期：1995-03-01 00:00:00

abstract：:Insect nicotinic acetylcholine (nACh) receptors are molecular targets of insecticides such as neonicotinoids that are used to control disease-carrying insects and agricultural pests. To date, several insect nACh receptor subunits have been identified, indicating different nACh receptor subtypes and pharmacological pro...

journal_title：Trends in pharmacological sciences

authors： Thany SH,Lenaers G,Raymond-Delpech V,Sattelle DB,Lapied B

更新日期：2007-01-01 00:00:00

abstract：:Receptors, enzymes, and ion channels are traditional targets of therapeutic development. A common strategy is to target these proteins with agents that either activate or suppress their activity with ligands or substrates that occupy orthosteric sites or have allosteric interactions. An alternative approach involves r...

journal_title：Trends in pharmacological sciences

authors： Conn PM,Spicer TP,Scampavia L,Janovick JA

更新日期：2015-08-01 00:00:00

abstract：:Pairing orphan G-protein-coupled receptors (GPCRs) to potential ligands found in tissue extracts or in libraries of synthetic compounds has identified an ever-increasing number of transmitters, some of which are novel, some of which were previously known and, more recently, some of which are unexpected. These discover...

journal_title：Trends in pharmacological sciences

authors： Civelli O

更新日期：2005-01-01 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 alpha-adrenoceptor was subdivided into three subtypes: alpha 2A-, alpha 2B- and alpha 2C-adrenoceptors almost ten years ago. Since then, the search has been on to discover and develop subtype-selective agonists and antagonists, but as yet no major breakthrough has been made. In the past year, several strains of ge...

journal_title：Trends in pharmacological sciences

authors： MacDonald E,Kobilka BK,Scheinin M

更新日期：1997-06-01 00:00:00

abstract：:This year marks the 90th anniversary of the publication of Hans Horst Meyer's classic paper in which he proposed that the ability of a substance to produce narcosis or anesthesia is governed by its partition coefficient. In this article, Robert Lipnick describes the experiments carried out by Meyer and his colleagues ...

journal_title：Trends in pharmacological sciences

authors： Lipnick RL

更新日期：1989-07-01 00:00:00

abstract：:Toll-like receptors (TLRs) play a crucial role in innate immunity by recognizing conserved motifs predominantly found in microorganisms. Increasing evidence supports a role for TLRs in sterile inflammation as observed in neurodegenerative disorders. This includes work suggesting a contribution for these receptors to t...

journal_title：Trends in pharmacological sciences

authors： Drouin-Ouellet J,Cicchetti F

更新日期：2012-10-01 00:00:00

abstract：:Hormesis is a generalizable dose-response relationship characterized by low-dose stimulation and high-dose inhibition. Despite debate over this biphasic dose-response curve, hormesis is challenging central beliefs in the evaluation of chemicals or drugs and has influenced biological model selection, concentration rang...

journal_title：Trends in pharmacological sciences

authors： Sun H,Calabrese EJ,Lin Z,Lian B,Zhang X

更新日期：2020-08-01 00:00:00

abstract：:Oxidative stress is a key pathologic factor in neurodegenerative diseases such as Alzheimer and Parkinson diseases (AD, PD). The failure of free-radical-scavenging antioxidants in clinical trials pinpoints an urgent need to identify and to block major sources of oxidative stress in neurodegenerative diseases. As a maj...

journal_title：Trends in pharmacological sciences

authors： Gao HM,Zhou H,Hong JS

更新日期：2012-06-01 00:00:00

abstract：:Spinal and bulbar muscular atrophy is a hereditary motor neuron disease caused by trinucleotide repeat expansion in the androgen receptor gene. The disease mechanism probably involves a toxic gain of function in the mutant protein, because other mutations that cause a loss of androgen receptor function result in a dif...

journal_title：Trends in pharmacological sciences

authors： Ranganathan S,Fischbeck KH

更新日期：2010-11-01 00:00:00

abstract：:Clinical implementation of two recently approved antisense RNA therapeutics - Exondys51® to treat Duchenne muscular dystrophy (Duchenne MD) and Spinraza® as a treatment for spinal muscular atrophy (SMA) - highlights the therapeutic potential of antisense oligonucleotides (ASOs). As shown in the Duchenne and Becker cas...

journal_title：Trends in pharmacological sciences

authors： Li D,Mastaglia FL,Fletcher S,Wilton SD

更新日期：2018-11-01 00:00:00

abstract：:Dimerization is fairly common in the G-protein-coupled receptor (GPCR) superfamily. First attempts to rationalize this phenomenon gave rise to an idea that two receptors in a dimer could be necessary to bind a single molecule of G protein or arrestin. Although GPCRs, G proteins and arrestins were crystallized only in ...

journal_title：Trends in pharmacological sciences

authors： Gurevich VV,Gurevich EV

更新日期：2008-05-01 00:00:00

abstract：:During the past decade, translocator protein 18 kDa (TSPO), previously named peripheral benzodiazepine receptor, has gained a great deal of attention based on its use as a clinical biomarker of neuroinflammation with therapeutic potential. However, there is a paucity of knowledge on the function(s) of TSPO in glial ce...

journal_title：Trends in pharmacological sciences

authors： Guilarte TR,Loth MK,Guariglia SR

更新日期：2016-05-01 00:00:00

abstract：:Seven-transmembrane receptors are prototypic allosteric proteins with the ability to adopt numerous conformations, many of which interact with cellular partners to initiate cellular biochemical processes. Defining efficacy as the ability of ligands to stabilize some of these conformations (which, in turn, possess phys...

journal_title：Trends in pharmacological sciences

authors： Kenakin T

更新日期：2007-08-01 00:00:00

abstract：:A diet low in carbohydrates helps to reduce the amount of ingested calories and to maintain a healthy weight. With this in mind, food and beverage companies have reformulated a large number of their products, replacing sugar or high fructose corn syrup with several different types of zero-calorie sweeteners to decreas...

journal_title：Trends in pharmacological sciences

authors： Servant G,Tachdjian C,Li X,Karanewsky DS

更新日期：2011-11-01 00:00:00

abstract：:Approximately 27 million people are living with a tumour in which the tumour suppressing activity of p53 has been inactivated. In half of these tumours, p53 itself is not mutated but the pathway is partially abrogated. Mechanisms include the overexpression of negative regulators of p53, such as MDM2 and MDM4, and dele...

journal_title：Trends in pharmacological sciences

authors： Brown CJ,Cheok CF,Verma CS,Lane DP

更新日期：2011-01-01 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：: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：:There is a variety of pressures on pharmacology teachers to replace real laboratory practicals with simulations but do they help students achieve the required learning objectives? In this article, the marks obtained by students in a variety of assessments using 'wet' or simulated practicals are analysed. Poorer perfor...

journal_title：Trends in pharmacological sciences

authors： Hughes IE

更新日期：2001-02-01 00:00:00

abstract：:The importance of the inhibitory neurotransmitter, GABA, within higher centres of the mammalian brain is unquestionable. However, its role within the spinal cord is of equal significance. There have been numerous studies over the past two decades that have established GABA as a neurotransmitter at both post- and presy...

journal_title：Trends in pharmacological sciences

authors： Malcangio M,Bowery NG

更新日期：1996-12-01 00:00:00

abstract：:There is increasing awareness of the compartmentalization of cAMP signalling--the means by which cAMP levels change in discrete domains of the cell with discrete local consequences. Current developments in understanding the organization of adenylyl cyclases in the plasma membrane are illuminating how the earliest part...

journal_title：Trends in pharmacological sciences

authors： Cooper DM,Crossthwaite AJ

更新日期：2006-08-01 00:00:00

abstract：:The physiological roles of chemokine receptors have expanded beyond host defense and now represent important targets for intervention in several disease indications. Chemokine receptors have joined the ranks of other members of the G-protein-coupled receptor (GPCR) family in therapeutic potential as small-molecule che...

journal_title：Trends in pharmacological sciences

authors： Onuffer JJ,Horuk R

更新日期：2002-10-01 00:00:00

abstract：:14-3-3 Proteins enact a range of cellular functions through protein-protein interactions (PPIs) with client proteins. Kaplan and colleagues recently demonstrated that a semisynthetic compound was able to selectively stabilize or disrupt specific interactions, depending on the binding partner. This finding presents an ...

journal_title：Trends in pharmacological sciences

authors： Gannon M,Yacoubian TA

更新日期：2020-07-01 00:00:00

abstract：:Drugs of abuse are very powerful reinforcers, and even in conditions of limited access (where the organism is not dependent) these drugs will motivate high rates of operant responding. This presumed hedonic property and the drugs' neuropharmacological specificity provide a means of studying the neuropharmacology and n...

journal_title：Trends in pharmacological sciences

authors： Koob GF

更新日期：1992-05-01 00:00:00

abstract：:Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subt...

journal_title：Trends in pharmacological sciences

authors： Buisson B,Bertrand D

更新日期：2002-03-01 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：:The breast cancer resistance protein [BCRP (also known as ABCG2)] belongs to the ATP binding cassette (ABC) family of transmembrane drug transporters. BCRP has a broad substrate specificity and actively extrudes a wide variety of drugs, carcinogens and dietary toxins from cells. Situated in the apical plasma membrane ...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,Schinkel AH

更新日期：2006-01-01 00:00:00