Development of beta 3-adrenoceptor agonists for the treatment of obesity and diabetes--an update.

No abstract is available for this paper.

• Publication year

  1999

• Venue

  Diabetes & Metabolism

• Publication date

  1999-03-01

• Fields of study

  Biology, Medicine

• Identifiers
  PMID 10335419
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• The occurrence of brown adipose tissue in outdoor workers

  2004cited by this paper
• β3-Adrenergic agonist induces a functionally active uncoupling protein in fat and slow-twitch muscle fibers.

  1998cited by this paper
• Mechanisms of the antidiabetic effects of the β3-adrenergic agonist CL-316243 in obese Zucker-ZDF rats.

  1998cited by this paper
• The Contribution of Classical (β1/2-) and Atypical β-Adrenoceptors to the Stimulation of Human White Adipocyte Lipolysis and Right Atrial Appendage Contraction by Novel β3-Adrenoceptor Agonists of Differing Selectivities

  1998cited by this paper
• Increase in insulin action and fat oxidation after treatment with CL 316,243, a highly selective beta3-adrenoceptor agonist in humans.

  1998cited by this paper
• Treatment with CL 316,243, a β3-adrenoceptor agonist, reduces serum leptin in rats with diet- or aging-associated obesity, but not in Zucker rats with genetic (fa/fa) obesity

  1998cited by this paper
• Emergence of brown adipocytes in white fat in mice is under genetic control. Effects on body weight and adiposity.

  1998cited by this paper
• Mice expressing human but not murine beta3-adrenergic receptors under the control of human gene regulatory elements.

  1998cited by this paper
• A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.

  1998cited by this paper
• (-)-CGP 12177 causes cardiostimulation and binds to cardiac putative beta 4-adrenoceptors in both wild-type and beta 3-adrenoceptor knockout mice.

  1998cited by this paper
• Obesity research continues to spring leaks.

  1997cited by this paper
• Appearance of brown adipocytes in white adipose tissue during CL 316,243-induced reversal of obesity and diabetes in Zucker fa/fa rats

  1997cited by this paper
• CL-316,243, a β3-Specific Adrenoceptor Agonist, Enhances Insulin-Stimulated Glucose Disposal in Nonobese Rats

  1997cited by this paper
• PROPOSAL FOR THE INTERACTION OF NON‐CONVENTIONAL PARTIAL AGONISTS AND CATECHOLAMINES WITH THE ‘PUTATIVE (β‐ADRENOCEPTOR’ IN MAMMALIAN HEART

  1997cited by this paper
• Hypertrophy of brown adipocytes in brown and white adipose tissues and reversal of diet-induced obesity in rats treated with a beta3-adrenoceptor agonist.

  1997cited by this paper
• Uncoupling protein-2: a novel gene linked to obesity and hyperinsulinemia

  1997cited by this paper
• Uncoupling protein‐3: a new member of the mitochondrial carrier family with tissue‐specific expression

  1997cited by this paper
• Mice lacking mitochondrial uncoupling protein are cold-sensitive but not obese

  1997cited by this paper
• Obesity and diabetes and the beta-3 adrenergic receptor.

  1997cited by this paper
• Beta3-adrenergic receptors on white and brown adipocytes mediate beta3-selective agonist-induced effects on energy expenditure, insulin secretion, and food intake. A study using transgenic and gene knockout mice.

  1997cited by this paper
• UCP3: an uncoupling protein homologue expressed preferentially and abundantly in skeletal muscle and brown adipose tissue.

  1997cited by this paper
• Beta 3-adrenergic receptor-mediated lipolysis and oxygen consumption in brown adipocytes from cynomolgus monkeys.

  1997cited by this paper
• Uncoupling Protein-3 Is a Mediator of Thermogenesis Regulated by Thyroid Hormone, β3-Adrenergic Agonists, and Leptin*

  1997cited by this paper
• Clinical pharmacology of b 3-adrenoceptors

  1996cited by this paper
• (—)‐CGP 12177‐induced increase of human atrial contraction through a putative third β‐adrenoceptor

  1996cited by this paper
• Activation of beta(3) adrenergic receptors suppresses leptin expression and mediates a leptin-independent inhibition of food intake in mice.

  1996cited by this paper
• Clinical pharmacology of beta 3-adrenoceptors.

  1996cited by this paper
• Biphasic effects of the β‐adrenoceptor agonist, BRL 37344, on glucose utilization in rat isolated skeletal muscle

  1996cited by this paper
• Effects of several putative beta 3-adrenoceptor agonists on lipolysis in human omental adipocytes.

  1996cited by this paper
• Prospects for beta 3-adrenoceptor agonists in the treatment of obesity and diabetes.

  1996cited by this paper
• Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes.

  1996cited by this paper
• Apparent lack of beta 3-adrenoceptors and of insulin regulation of glucose transport in brown adipose tissue of guinea pigs.

  1995cited by this paper
• Demonstration of an in vivo functional beta 3-adrenoceptor in man.

  1995cited by this paper
• Pharmacological characteristics and species‐related variations of β3‐adrenergic receptors

  1995cited by this paper
• The beta 3-adrenergic receptor--a cause and cure of obesity?

  1995cited by this paper
• Effects on metabolic rate and fuel selection of a selective beta-3 agonist (ICI D7114) in healthy lean men.

  1995cited by this paper
• Targeted Disruption of the β3-Adrenergic Receptor Gene *

  1995cited by this paper
• The potential significance of beta 3 adrenergic receptors.

  1995cited by this paper
• Metabolic alterations associated with the antidiabetic effect of beta 3-adrenergic receptor agonists in obese mice.

  1995cited by this paper
• Immunohistochemical identification of the uncoupling protein in human hibernoma

  1994cited by this paper
• Effect of CL 316,243, a novel beta 3-adrenoceptor agonist, on insulin secretion in perfused mouse pancreas.

  1994cited by this paper
• Cardiac effects of the beta 3-adrenoceptor agonist BRL35135 in man.

  1994cited by this paper
• Antidiabetic and antiobesity effects of a highly selective β3‐adrenoceptor agonist (CL 316,243)

  1994cited by this paper
• Anti-obesity effect of CL 316,243, a highly specific beta 3-adrenoceptor agonist, in mice with monosodium-L-glutamate-induced obesity.

  1994cited by this paper
• Beta-3 adrenoceptor selectivity of the dioxolane dicarboxylate phenethanolamines.

  1994cited by this paper
• Effect of a novel beta-adrenoceptor agonist (Ro 40-2148) on resting energy expenditure in obese women.

  1994cited by this paper
• Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific beta 3-adrenoceptor agonist, in yellow KK mice.

  1994cited by this paper
• Effect of CL-316,243, a thermogenic beta 3-agonist, on energy balance and brown and white adipose tissues in rats.

  1994cited by this paper
• Development of obesity in transgenic mice after genetic ablation of brown adipose tissue

  1993cited by this paper
• Development of morbid obesity in transgenic mice following the genetic ablation of brown adipose tissue

  1993cited by this paper
• The quantitative contributions of mitochondrial proton leak and ATP turnover reactions to the changed respiration rates of hepatocytes from rats of different thyroid status.

  1993cited by this paper
• Evidence for a functional β3‐adrenoceptor in man

  1993cited by this paper
• Tissue distribution of beta 3-adrenergic receptor mRNA in man.

  1993cited by this paper
• Expression of the beta 3-adrenergic receptor in human white adipose tissue.

  1993cited by this paper
• Long-term agonist exposure induces upregulation of beta 3-adrenergic receptor expression via multiple cAMP response elements.

  1992cited by this paper
• Brown adipose tissue and obesity

  1992cited by this paper
• Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.

  1992cited by this paper
• ICI D7114: a novel selective adrenoceptor agonist of brown fat and thermogenesis.

  1992cited by this paper
• Metabolic effects of three weeks administration of the beta-adrenoceptor agonist BRL 26830A.

  1992cited by this paper
• Molecular cloning and expression of the rat beta 3-adrenergic receptor.

  1991cited by this paper
• Tremor and the anti-obesity drug BRL 26830A.

  1990cited by this paper
• Molecular characterization of the human beta 3-adrenergic receptor.

  1989cited by this paper
• Effects of BRL 35135, a beta-adrenoceptor agonist with novel selectivity, on glucose tolerance and insulin sensitivity in obese subjects.

  1989cited by this paper
• Two-week stimulation or blockade of the sympathetic nervous system in man: influence on body weight, body composition, and twenty four-hour energy expenditure.

  1988cited by this paper
• An investigation of the beta-adrenoceptor that mediates metabolic responses to the novel agonist BRL28410 in rat soleus muscle.

  1988cited by this paper
• Substrate supply for thermogenesis induced by the beta-adrenoceptor agonist BRL 26830A.

  1987cited by this paper
• Brown adipose tissue in patients with phaeochromocytoma.

  1986cited by this paper
• Contribution of BAT and skeletal muscle to thermogenesis induced by ephedrine in man.

  1985cited by this paper
• Effects of Chronic Beta Receptor Stimulation on Glucose Metabolism

  1984cited by this paper
• The antiobesity and metabolic activities of LY79771 in obese and normal mice.

  1984cited by this paper
• Treatment of obesity with thermogenic beta-adrenoceptor agonists: studies on BRL 26830A in rodents.

  1984cited by this paper
• Thermogenic and antiobesity activity of a novel beta-adrenoceptor agonist (BRL 26830A) in mice and rats.

  1983cited by this paper
• Ultrastructural and biochemical characterization of human brown adipose tissue in pheochromocytoma.

  1982cited by this paper
• Heat Production and Temperature Regulation

  1978cited by this paper
• Thermogenic mechanisms and their control.

  1978cited by this paper
• Mitochondrial protein alteration in active brown fat: a soidum dodecyl sulfate-polyacrylamide gel electrophoretic study.

  1976cited by this paper
• [Clinical pharmacology].

  1968cited by this paper
• The adrenergic receptor.

  1966cited by this paper
• The glucose fatty-acid cycle. Its role in insulin sensitivity and the metabolic disturbances of diabetes mellitus.

  1963cited by this paper

• Two'-Fucosyllactose, a Human Milk Oligosaccharide, Promotes Intestinal Remodeling and Enhances Nutrient and Functional Component Absorption.

  2026cites this paper
• Sympathetic activation of white adipose tissue recruits neutrophils to limit energy expenditure

  2025cites this paper
• Neutrophils preserve energy storage in sympathetically activated adipocytes

  2025cites this paper
• Fatty Acylcarnitine Metabolism in Brown/Beige and White Fats by 13C HRMAS NMR Spectroscopy With Metabolic Interventions

  2025cites this paper
• Role of Brown Adipose Tissue in Metabolic Health and Efficacy of Drug Treatment for Obesity

  2024cites this paper
• Protein kinase D1 (Prkd1) deletion in brown adipose tissue leads to altered myogenic gene expression after cold exposure, while thermogenesis remains intact

  2023cites this paper
• Uncoupling Protein 1 Does Not Produce Heat without Activation

  2022cites this paper
• Comparison of beta-ligands used in cattle production: structures, safety, and biological effects

  2021cites this paper
• The beta2‐adrenergic receptor – a re‐emerging target to combat obesity and induce leanness?

  2021cites this paper
• Effects of Caffeine on Brown Adipose Tissue Thermogenesis and Metabolic Homeostasis: A Review

  2021cites this paper
• Effect of Beta 3 Adrenoreceptor Modulation on Patency of the Ductus Arteriosus

  2020cites this paper
• Adrenal cortex hypoxia modulates aldosterone production in heart failure.

  2020cites this paper
• Animal models: bridging cross-species variation through animal biotechnology

  2020cites this paper
• Investigation Trp64Arg polymorphism of the beta 3-adrenergic receptor gene in nonobese women with polycystic ovarian syndrome

  2020cites this paper
• Quassinoids in Brucea javanica are potent stimulators of lipolysis in adipocytes.

  2019cites this paper
• Translational Pharmacology and Physiology of Brown Adipose Tissue in Human Disease and Treatment.

  2019cites this paper
• Physiology and pathophysiology of the β3-adrenergic receptor.

  2019cites this paper
• Brown adipocytes and β3-stimulant-induced brown-like adipocytes contribute to the prevention of renal crystal formation.

  2019cites this paper
• Duration of a ”Brown-Like” Phenotype of White Adipose Tissue Induced by the β3 Agonist CL-316,243

  2018cites this paper
• Acute metabolic and cardiovascular effects of mirabegron in healthy individuals

  2018cites this paper
• Browning of white adipose tissue induced by the ß3 agonist CL-316,243 after local and systemic treatment - PK-PD relationship.

  2018cites this paper
• Bioresponsive Drug Delivery by Microneedle Patches.

  2018cites this paper
• 5-Ene-4-thiazolidinones – An efficient tool in medicinal chemistry

  2017cites this paper
• Molecular Docking and Drug Discovery in β-Adrenergic Receptors.

  2017cites this paper
• β 3 -AR Agonists for the Treatment of Overactive Bladder

  2017cites this paper
• The importance of translatability in drug discovery

  2017cites this paper
• Metabolic actions of secretin

  2017cites this paper
• Locally Induced Adipose Tissue Browning by Microneedle Patch for Obesity Treatment.

  2017cites this paper
• Hypermetabolic Response to Burn Injury

  2016cites this paper
• Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.

  2016cites this paper
• Chapter 36 – Role of the Adipocyte in Metabolism and Endocrine Function

  2016cites this paper
• Pharmacotoxicological screening on new derivatives of beta-phenylethylamine, potential agonists of beta3-adrenergic receptors.

  2016cites this paper
• Short report Open Access

  2015cites this paper
• Activation of Classical Brown Adipocytes in the Adult Human Perirenal Depot Is Highly Correlated with PRDM16–EHMT1 Complex Expression

  2015cites this paper
• The "Skinny" on brown fat, obesity, and bone.

  2015cites this paper
• Burn Induces Browning of the Subcutaneous White Adipose Tissue in Mice and Humans

  2015cites this paper
• Anti-obesity and metabolic efficacy of the β3-adrenergic agonist, CL316243, in mice at thermoneutrality compared to 22°C

  2015cites this paper
• Animal models in translational medicine: Validation and prediction

  2014cites this paper
• Increased Metabolic Activity of Brown Adipose Tissue (BAT) in Patients with Hyperthyroidism

  2014cites this paper
• The Regulation of Brown Adipose Tissue Activation by Multiple Phosphodiesterases

  2013cites this paper
• OBESITY: PATHOPHYSIOLOGY AND MANAGEMENT-A PHARMACOLOGICAL PERSPECTIVE

  2013cites this paper
• Obesity Pharmacotherapy: Current Perspectives and Future Directions

  2013cites this paper
• PDE3 and PDE4 Isozyme-Selective Inhibitors Are Both Required for Synergistic Activation of Brown Adipose Tissue

  2013cites this paper
• In vitro Antioxidant Properties of Novel β3-Adrenoceptor Agonists Bearing Benzenesulfonamide Fragment

  2013cites this paper
• Catechol-O-methyltransferase and pain in rodents and humans

  2013cites this paper
• PDE 3 and PDE 4 Isozyme-Selective Inhibitors Are Both Required for Synergistic Activation of Brown Adipose Tissue s

  2013cites this paper
• Metabolic Syndrome Bioactivity in Whey Proteins Influencing Energy Balance

  2012cites this paper
• Mitochondria as pharmacological targets: the discovery of novel anti-obesity mitochondrial uncouplers from Africa's medicinal plants.

  2012cites this paper
• Bioactivity in Whey Proteins Influencing Energy Balance

  2012cites this paper
• EXPERIMENTAL PHARMACOLOGICAL RESEARCH REGARDING THE ANTI-OBESITY EFFECT AND THE MOTOR BEHAVIOR INDUCED BY SOME NEWLY SYNTHETIZED β3 ADRENERGIC RECEPTORS AGONISTS IN NORMAL MICE

  2012cites this paper
• Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists.

  2011cites this paper
• Histamine H3 receptor as a drug discovery target.

  2011cites this paper
• Association of beta3-adrenergic receptor (ADRB3) Trp64Arg gene polymorphism with obesity and metabolic syndrome in the Balinese: a pilot study

  2011cites this paper
• Distribution and quantification of β-3 adrenergic receptor in tissues of sheep.

  2011cites this paper
• Systemic Side Effects of Glaucoma Medications

  2010cites this paper
• Investigating energy homeostasis using in vivo imaging techniques

  2010cites this paper
• GPR40 is partially required for insulin secretion following activation of beta3-adrenergic receptors.

  2010cites this paper
• Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.

  2010cites this paper
• Mesenchymal stem cells as trophic mediators of neural differentiation

  2010cites this paper
• Comparative 3D QSAR study on β1-, β2-, and β3-adrenoceptor agonists

  2009influential citation
• Insulin-Sensitizing Therapy Attenuates Type 2 Diabetes–Mediated Mammary Tumor Progression

  2009cites this paper
• The beta3-adrenoceptor as a therapeutic target: current perspectives.

  2009cites this paper
• Anti-diabetic therapy inhibits mammary tumor progression Insulin sensitizing therapy attenuates type 2 diabetes-mediated mammary tumor progression Running Title: Anti-diabetic therapy inhibits mammary tumor progression

  2009cites this paper
• Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.

  2009cites this paper
• Promising strategies for obesity pharmacotherapy: melanocortin-4 (MC-4) receptor agonists and melanin concentrating hormone (MCH) receptor-1 antagonists.

  2009cites this paper
• Obesity: pathophysiology and clinical management.

  2009cites this paper
• Beta 3 adrenergic receptors: molecular, histological, functional and pharmacological approaches

  2009cites this paper
• Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.

  2009cites this paper
• Ventricular fibrillation associated with use of synephrine containing dietary supplement.

  2009cites this paper
• Central Integration of Environmental and Endogenous Signals Important in the Regulation of Food Intake and Energy Expenditure

  2009cites this paper
• Pharmacotherapy of obesity: emerging drugs and targets

  2009cites this paper
• Studies of adipose tissue in humans with special reference to innervation by the sympathetic nervous system

  2009cites this paper
• Beta 3 adrenergic receptors: molecular, histological, functional and pharmacological approaches.

  2009cites this paper
• Design and Testing of an Infrared Temperature System to Test the Effects of Chemical Stimulation on Heat Production in Cell Cultures

  2008cites this paper
• Catecholamine regulation of local lactate production in vivo in skeletal muscle and adipose tissue: role of -adrenoreceptor subtypes.

  2008cites this paper
• Anti‐inflammatory effects of β3‐adrenoceptors: the burgeoning field of neurogastroimmunology

  2008cites this paper
• Mobilisation des lipides et dépense énergétique : apports des développements cellulaires et moléculaires dans le traitement de l'obésité

  2008cites this paper
• The novel polymorphism of the beta 3-adrenergic receptor gene and its distribution in domestic pigs and wild boars in Asia

  2007cites this paper
• Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.

  2007cites this paper
• Potential Role of New Therapies in Modifying Cardiovascular Risk in Overweight Patients with Metabolic Risk Factors

  2006cites this paper
• Agonist effects of zinterol at the mouse and human beta(3)-adrenoceptor.

  2006cites this paper
• Obesity: new perspectives and pharmacotherapies.

  2006cites this paper
• Antiobesity therapy: emerging drugs and targets.

  2006cites this paper
• Role of Energy Expenditure in Regulation of Energy Homeostasis

  2006cites this paper
• Agonist effects of zinterol at the mouse and human β3-adrenoceptor

  2006cites this paper
• Recent developments in the design of orally bioavailable beta3-adrenergic receptor agonists.

  2006cites this paper
• Citrus aurantium and synephrine alkaloids in the treatment of overweight and obesity: an update

  2006cites this paper
• New Perspectives and Pharmacotherapies

  2006cites this paper
• Systemic reactions associated with ophthalmic medications.

  2005cites this paper
• Searching for obesity genes: progress and prospects.

  2005cites this paper
• DNA microarray analysis of white adipose tissue from obese (fa/fa) Zucker rats treated with a beta3-adrenoceptor agonist, KTO-7924.

  2005cites this paper
• Discovery of a novel and potent human and rat beta3-adrenergic receptor agonist, [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid.

  2005cites this paper
• Peripheral targets for antiobesity drugs.

  2004cites this paper
• Synthesis, biological evaluation, and structural studies on N1 and C5 substituted cycloalkyl analogues of the pyrazole class of CB1 and CB2 ligands.

  2004cites this paper
• BMS-201620: a selective beta 3 agonist.

  2004cites this paper
• 80 – Weight Reduction Therapies: Anorectants, Thermogenics, and Lipolytics

  2004cites this paper
• Role of Mitochondrial Uncoupling Protein 2 (UCP2) in Modulation of Adiposity

  2004cites this paper
• Hypoglycemic mechanism of ginseng glycopeptide.

  2003cites this paper
• Molecular and genetic mechanisms of obesity: implications for future management.

  2003cites this paper
• Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.

  2003cites this paper