Adregergic Receptor



Adrenergic Receptor

肾上腺素受体(Adrenergic Receptor)，是G蛋白耦联受体超家族中最具代表性的成员之一。作为交感神经递质的去甲肾上腺素(Noradrenaline)及内分泌激素的肾上腺素(Adrenaline)，正是通过与靶器官上的肾上腺素受体结合，激发一系列的细胞内信号传递与物质合成，从而完成化学信号的转导，参与体内多数器官生理功能的调节。受体结构、分布与功能的异常，往往与相应器官的病理改变紧密相联。因此，对于肾上腺素受体的研究，一直是分子生物学、生物物理学、细胞生物学、生理学、病理学、乃至药理学等诸多学科共同关注的焦点。特别是由于肾上腺素受体在心血管系统及肾脏的广泛分布，使得它对心脏及血管功能的调节作用显得尤为突出，它与各种心血管疾病的发生发展关系尤为密切，因此也成为心血管疾病基础研究与药物开发的重点与热点之一。本月初，北京大学心血管研究所肖瑞平教授领导的实验室，在The Journal of Clinical Investigation (IF=14.118)发表了β受体激活与心肌细胞凋亡研究的重要成果。该工作第一次将β1肾上腺素受体与调节细胞内钙的激酶分子(CaMKII)联系到了一起，证明了β受体激活引起的凋亡，与经典的PKA途径无关。这也进一步向我们展示了细胞内各种信号传递通路之间的Cross Talk的复杂性，为肾上腺素受体信号系统的研究又开辟了一个新的领域。CMBI特在平时工作积累的基础上，于近期特别收集整理了一系列与肾上腺素受体相关的综述及原著论文，供大家参考。更多的资料，请用相关的关键词通过CMBI文献查询获取。

Special Presentation: Linkage of β1-adrenergic stimulation to apoptotic heart cell death through protein kinase A (Zhu, WZ. Xiao,RP et al. J. Clin. Invest. 2003 111: 617-625, Partially supported by 973 Project,China) Calcium and the heart:a question of life and death (Andrew R. Marks. JCI Commentary. J. Clin. Invest. 2003 111: 597-600)

Reviews Original Papers: Subtypes Genetics/Molecular Cellular/Singaling Physiology Pathology Pharmacology Structural / Bioinformatics	Reviews β Adrenergic Receptor Signaling Pathways Mediating Cell Survival in Cardiomyocytes α1-Adrenergic Receptor Subtype Function in Cardiomyocytes α1-Adrenergic Receptors- New Insights and Directions β3-Adrenergic System and β3-Adrenergic Agonists adrenergic activation of cardiac phospholipase D： role of α1-adrenoceptor subtypes β-Adrenergic Receptors, Transgenic Mice, and Pharmacological Model Systems Adrenergic regulation of bone metabolism Adrenergic regulation of cardiac myocyte apoptosis Modification of β-adrenoceptor signal transduction pathway by genetic manipulation and heart failure Age-related changes in adrenergic neuroeffector transmission Aging and calcium buffering in adrenergic neurons Alpha1-adrenoceptors and vascular smooth muscle cell growth Apoptosis and Heart Failure：Mechanisms and Therapeutic Implications Development of β3-adrenoceptor agonists as antiobesity and antidiabetes drugs in humans Endocytosis and downregulation of G protein-coupled receptors Noradrenergic regulation of hippocampal place cells Norepinephrine and β2-Adrenergic Receptor Stimulation Regulate CD4+ T and B Lymphocyte Function Norepinephrine and the control of food intake Radioiodinated α1-adrenergic receptor ligands Role of adrenoceptor subtypes in memory consolidation Transgenic Studies of Cardiac Adrenergic Receptor Regulation Use of β-Blockers in Atrial Fibrillation Vascular neuroeffector mechanisms:the next 30 years Vascular α1D-Adrenoceptors:Are They Related to Hypertension? α1-Adrenergic receptor regulation: basic science and clinical implications α1-Adrenoceptors- Subtypes, Signaling, and Roles in Health and Disease α1-Adrenoceptors-function and phosphorylation β3-Adrenoceptor agonists- potential, pitfalls and progress β3-Adrenoceptors in the heart Adrenergic Receptors- From Molecular Structure to in vivo Function Localization and trafficking of α2-adrenergic receptor subtypes in cells and tissues [beta]-Blocker Therapy in Heart Failure [beta]-Blockers in Chronic Heart Failure [beta]-Blockers in Heart Failure- Clinical Applications TOP Subtypes Adrenoceptor subclassification- an approach to improved cardiovascular therapeutics adrenergic activation of cardiac phospholipase D： role of α1-adrenoceptor subtypes adrenergic receptor subtypes in heart cell culture Affinity profile at α1- and α2-adrenoceptor subtypes Differences in the subcellular localization of α1-adrenoceptor subtypes can affect the subtype selectivity of drugs Differential down-regulation of α-2 adrenergic receptor subtypes Distribution of α(1)-adrenoceptor subtype proteins in different tissues of neonatal and adult rats Does segmental difference in α1-adrenoceptor subtype explain contractile difference in rat abdominal and thoracic aortae Failure of AH11110A to functionally discriminate between α1-adrenoceptor subtypes A, B and D or between α1- and α2-adrenoceptors In Vivo Gene Modification Elucidates Subtype-Specific Functions of α2-Adrenergic Receptors Subtypes of functional α1- and α2-adrenoceptors α1-Adrenoceptor subtypes Adrenergic Receptor Subtypes Differentially Control the Cell Cycle of Transfected CHO Cells through a cAMP-dependent Mechanism Involving p27Kip1 TOP Genetics/Molecular A line item approach to the identification of genes involved in polygenic behavioral disorders- The Adrenergic 2A (ADRA2A) gene adrenergic receptor subtypes in heart cell culture Altered levels of mRNA expression and pharmacological reactivity of α1-adrenergic receptor subtypes Association analysis of polymorphism in the promoter region of the α2a-adrenoceptor gene with schizophrenia Biological efficacy of antisense oligonucleotides complementary to overlapping regions of the mRNA target Cloning, pharmacological characterization, and polymorphism screening of the guinea pig β2-adrenoceptor Determination of β2-adrenergic receptor (ADRB2) haplotypes by a multiplexed polymerase chain reaction assay Distribution of α1A adrenergic receptor mRNA in the rat brain Effect of the (C825T) Gβ(3) polymorphism on adrenoceptor-mediated lipolysis in human fat cells Effects of Single and Repeated Restraint Stresses on the Expression of β(1)-Adrenoceptor mRNA Functional Immobilization of a Ligand-Activated G-Protein-Coupled Receptor Gene expression of α1A-adrenoceptor but not α1B-adrenoceptor in cultured myoblast C2C12 cells Genomic cloning and species-specific properties of the recombinant canine β3-adrenoceptor Identification and functional characterization of α2-adrenoceptor polymorphisms Identification of α1-adrenergic receptors and their involvement in phosphoinositide hydrolysis in the frog heart Identification of an interactive effect of β3- and α2b-adrenoceptor gene polymorphisms on fat mass Linkage study of the α2A adrenergic receptor in attention-deficit hyperactivity disorder families Norepinephrine transporter and α2c adrenoceptor allelic variants and personality factors PCR-based mutagenesis of a GC-rich DNA template-application to the human α2C-adrenoceptor cDNA Polymorphism of the β2-adrenoceptor in COPD in Chinese subjects Racial differences in the frequencies of cardiac 1-adrenergic receptor polymorphisms Regulation of α2A-adrenoceptor expression by chronic stress in neurons of the brain stem Repeated imipramine and electroconvulsive shock increase α1A-adrenoceptor mRNA level in rat prefrontal cortex Transcription of the β2-adrenergic receptor gene in rat liver is regulated during early postnatal development by an upstream repressor element Transcriptional regulation of α1-adrenoceptor gene in the rat liver β2 adrenoceptor promoter polymorphisms- Extended haplotypes and functional effects in monouclear cells N-terminal truncation of human α1D-adrenoceptors increases expression of binding sites but not protein β2-Adrenergic Receptor Gene Polymorphism, Age, and Cardiovascular Phenotypes Determination of 2-adrenergic receptor (ADRB2) haplotypes by a multiplexed polymerase chain reaction assay Changes in mRNA expression induced by noradrenaline stimulation TOP Cellular/Singaling Alterations of cardiac β-adrenoceptor mechanisms due to calcium depletion and repletion Modification of β-adrenoceptor signal transduction pathway by genetic manipulation and heart failure Analysis of inhibition by H89 of UCP1 gene expression and thermogenesis indicates protein kinase A mediation of β3-adrenergic signalling rather than β3-adrenoceptor antagonism by H89 Attenuation of KATP Channel-Opener Induced Shortening of Repolarization Time by α1-adrenoceptor Blockade of Hyperpolarization-Activated Channels Modifies the Effect of β-adrenoceptor Stimulation Colocalization of β-adrenergic receptors and caveolin within the plasma membrane C-Terminal exchange between Gα0 and Gαi3 proteins differently modulates α2A-adrenoceptor Distinct interactions of Gsα-long, Gsα-short, and Gαolf with GTP, ITP, and XTP Diversity and specificity in the regulated endocytic membrane trafficking of G-protein-coupled receptors Effects of Ca2+ influx through nonselective cation channel on noradrenaline-induced mitogenic responses Evidence for protean agonism of RX 831003 at α2A-adrenoceptors by co-expression with different Gα protein subunits Ligand modulation of [35S]GTPγS binding at human α2A, α2B and α2C adrenoceptors Noradrenaline induces brown adipocytes cell growth via β-receptors by a mechanism dependent on ERKs but independent of cAMP and PKA Norepinephrine induces slow calcium signalling in murine brown preadipocytes through the β-adrenoceptor-cAMP-protein kinase A pathway Reciprocal mutations of highly conserved residues in transmembrane helices 2 and 7 of the α2A-adrenoceptor restore agonist activation of Gi1α Similarities and differences in the coupling of human β1- and β2-adrenoceptors to Gsα splice variants β3-Adrenergic regulation of an ion channel in the heart—inhibition of the slow delayed rectifier potassium current IKs in guinea pig Stimulated Apoptosis in Cardiac Myocytes Is Mediated by Reactive Oxygen A macromolecular complex of 2 adrenergic receptor, CFTR, and ezrinradixinmoesin- is regulated by PKA Antidepressant-induced Switch of 1-Adrenoceptor Trafficking as a Mechanism for Drug Action α1-Adrenoceptor effects mediated by protein kinase C TOP Physiology α1-adrenergic stimulation mediates Ca2+-dependent inositol phosphate formation through the α1B-like adrenoceptor subtype in adult rat cardiac myocytes β-Adrenergics enhance brain extraction of levodopa Oxytocin/Alpha(2)-adrenoceptor interactions in feeding responses Behavioral and neurochemical characterization of α2A-adrenergic receptor knockout mice Behaviorally conditioned immunosuppression in the rat is regulated via noradrenaline and β-adrenoceptors Central α1-adrenoceptors：Their role in the modulation of attention and memory formation Developmental regulation of α1A-adrenoceptor function in rat brain oligodendrocyte cultures Does segmental difference in α1-adrenoceptor subtype explain contractile difference in rat abdominal and thoracic aortae Interaction between brain L-type calcium channels and α2-adrenoceptors in the inhibition of sodium appetite Interaction between α2-autoreceptors and receptors mediating the effects of angiotensin II and bradykinin in the heart Involvement of adrenoceptors in the angiotensin II-induced expression of inducible transcription factors in the rat forebrain and hypothalamus Peculiarities of Adrenergic Regulation of Smooth Muscles in Rabbit Pulmonary Arteries Role of α2A-adrenoceptors of Locus Coeruleus in Regulation of Plasma Corticosterone Content in Male Rats Sepsis causes presynaptic histamine H3 and α2-adrenergic dysfunction in canine myocardium Stimulation of β-adrenoceptors activates astrocytes and provides neuroprotection Toxic cardiac effects of catecholamines： role of β-adrenoceptor downregulation Influence of T-type Ca(2+)and Cl channel antagonists on α(1)-adrenoceptor in aorta α2a and α2c adrenoceptors on spinal neurons controlling penile erection α2-Adrenoceptors control the release of noradrenaline but not neuropeptide Y α-Adrenergic control of ANG II-induced drinking in the rat median preoptic nucleus β1/β2/β3-adrenoceptor knockout mice are obese and cold-sensitive but have normal lipolytic responses to fasting β3-adrenoceptors in human detrusor muscle β-adrenoceptor Modulation and Heart Rate Variability—The Value of Scatterplot Measures of Compactness α2 Adrenoceptor-mediated vasoconstriction in porcine palmar lateral vein Hormonal influence on expression and functionality of α1-adrenoceptor in rat submandibular gland Alpha-2 adrenergic receptors stimulate actin organization in developing fetal rat cardiac myocytes Central α2 adrenergic receptors and cholinergic-induced salivation Doxazosin Induces Apoptosis in Cardiomyocytes by a Mechanism- [alpha]1-Adrenergic Blockade β3-Adrenergic regulation of an ion channel in the heart Evidence against β3-adrenoceptors or low affinity state ofβ1-adrenoceptors mediating relaxation in rat isolated aorta TOP Pathology Down regulation of myocardial β1-adrenoceptor signal transduction system in pacing-induced failure in dogs with aortic stenosis-induced left ventricular hypertrophy Alpha-adrenergic coronary vasoconstriction and myocardial ischemia in humans Cellular and molecular aspects of myocardial dysfunction Differentially altered cerebral metabolism in ischemic rats by α2-adrenoceptor blockade and its relation to improved limb-placing reactions Effect of adrenergic stimulation on Rb+ uptake in normal and ischemic areas of isolated pig hearts Effects of β3-adrenoceptor stimulation on prostaglandin E2-induced bladder hyperactivity and on the cardiovascular system Effects of α1-adrenoceptor (1-AR) antagonists on cell proliferation and apoptosis in the prostate Enhanced Interaction Between α(2)-Adrenoceptors and AGT Receptors in Hypertension Expression of a β-Adrenergic Receptor Kinase Inhibitor Reverses Dysfunction in Failing Cardiomyocytes A fluctuation in adrenocepter- and muscarinic receptor-mediated blood pressure responses in acute hyperthyroid rats Increased expression of G protein-coupled receptor kinases in cystic fibrosis lung Linkage study of the α2A adrenergic receptor in attention-deficit hyperactivity disorder families Mechanistic investigation of the adrenergic induction of ventral prostate hyperplasia Possible Mechanism of Regression of Myocardial Hypertrophy Skeletal muscle hypertrophy and anti-atrophy effects of clenbuterol are mediated by the β2-adrenergic receptor Vascular β-adrenoceptor function in hypertension and in ageing β-Adrenergic Receptor Signaling- An Acute Compensatory Adjustment—Inappropriate for the Chronic Stress of Heart Failure The α1-adrenoceptor profile in human skeletal muscle resistance arteries in critical limb ischaemia Cytokines down-regulate α1-adrenergic receptor expression during endotoxemia Gene expression profiling of α1b-adrenergic receptor-induced cardiac hypertrophy by oligonucleotide arrays Effects of propranolol on recovery of heart rate variability following acute myocardial infarction β1-Adrenoceptor autoimmunity in cardiomyopathy TOP Pharmacology & Therapy Benefits of β-Blocker Therapy for Heart Failure β-Adrenergic Receptors, Transgenic Mice, and Pharmacological Model Systems Use of β-Blockers in Atrial Fibrillation Development of β3-adrenoceptor agonists as antiobesity and antidiabetes drugs in humans β3-Adrenoceptor agonists- potential, pitfalls and progress [beta]-Blocker Therapy in Heart Failure [beta]-Blockers in Chronic Heart Failure [beta]-Blockers in Heart Failure- Clinical Applications β-Adrenoceptor agonists and asthma-100 years of development Imidazoline antihypertensive drugs- a critical review on their mechanism of action Pharmacological characterisation of the β-adrenoceptor expressed by human lung mast cells Pharmacological characterization of α1-adrenoceptor in mouse iliac artery Species-specific pharmacological properties of human α(2A)-adrenoceptors Structure–activity relationship studies with (±)-nantenine derivatives for α1-adrenoceptor antagonist activity Synthesis, Structure, and Binding of Some 2-Imidazolines to Rat Brain Alfa-1 and Alfa-2-Adrenergic Receptors The indirect negative inotropic effect of carbachol in β1-adrenoceptor antagonist-treated human right atria Vascular actions of 3,4-methylenedioxymethamphetamine in α2A-D-adrenoceptor knockout mice α1-Adrenoceptor activation- A comparison of 4-(Anilinomethyl)imidazoles and 4-(Phenoxymethyl)imidazoles to related 2-imidazolines α1-Adrenoceptor Agonists- The Identification of Novel α1A Subtype Selective 2′-Heteroaryl-2-(phenoxymethyl)imidazolines α1-Adrenoceptor antagonists. rational design, synthesis and biological evaluation of new trazodone-like compounds α1L-, but not α1H-, adrenoceptor antagonist prevents allergic bronchoconstriction in guinea pigs in vivo Alternative Mechanisms for Long-Acting β2-Adrenergic Agonists in COPD (±)-Domesticine, a novel and selective α1D-adrenoceptor antagonist in animal tissues and human α1-adrenoceptors ABT-866, a novel α1A-adrenoceptor agonist with antagonist properties at the α1B- and α1D-adrenoceptor subtypes Efficient synthesis of the optically active dihydropyrimidinone of a potent α1A-selective adrenoceptor antagonist Celiprolol inhibits mitogen-activated protein kinase and endothelin-1 and transforming growth factor-β1 gene in rats Characterization of some novel α1-adrenoceptor antagonists in human hyperplastic prostate Current treatment and future directions in heart failure Denopamine, a selective β1-receptor agonist and a new coronary vasodilator Differences in the subcellular localization of α1-adrenoceptor subtypes can affect the subtype selectivity of drugs Effect of antisense knock-down of α2a- and α2c-adrenoceptors on the antinociceptive action of clonidine on trigeminal nociception Effects of cortisol on brain α2-adrenoceptors Effects of medullary α2-adrenoceptor blockade Enhancement of memory consolidation in chicks by β3-adrenoceptor agonists Evaluation of the α2C-adrenoceptor as a neuropsychiatric drug target Inhaled β-2 adrenergic receptor agonists and primary cardiac arrest Involvement of central KATP channels in the gastric antisecretory action of α2-adrenoceptor agonists KUR-1246, a novel β2-adrenoceptor agonist, as a tocolytic agent the binding of β-adrenoceptor blockers to Na(+)K(+)-ATPase in pig heart Atipamezole, an α2-adrenoceptor antagonist, augments the effects of l-DOPA on evoked dopamine release Contractile actions of imidazoline α-adrenoceptor agonists and effects of noncompetitive α1-adrenoceptor antagonists α2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs β1-adrenoceptor selectivity of nebivolol and bisoprolol β1-adrenoceptor selectivity of nebivolol and bisoprolol The effect of β-adrenergic blockers on the prognostic value of peak exercise oxygen uptake in patients with heart failure α-Adrenergic blockade- a possible mechanism of tocolytic action of certain benzodiazepines TOP Structural / Bioinformatics Modeling the 3D structure of GPCRs from sequence Theoretical evidence of a salt bridge disruption as the initiating process for the α1d-adrenergic receptor activation Theoretical study on receptor-G protein recognition- New insights into the mechanism of the α1b-adrenergic receptor activation Agonist-induced conformational changes in the β2 adrenergic receptor Identification of an Allosteric Binding Site for Zn2+ on the 2 Adrenergic Receptor TOP
Last Modified:2003.3.10