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Beta3 adrenergic receptor

Nailliw Z Preite, Bruna P P Nascimento, Cynthia R Muller, Anna Laura V Americo, Talita S Higa, Fabiana S Evangelista, Carmen L Lancellotti, Felipe Dos Santos Henriques, Miguel Luiz Batista Júnior, Antonio C Bianco, Miriam Oliveira Ribeiro
The brown adipose tissue (BAT) mediates adaptive changes in metabolic rate by responding to the sympathetic nervous system (SNS) through β-adrenergic receptors (AR). Here we wished to define the role played by the ARβ3 isoform in this process. This study focused on the ARβ3 knockout mice (ARβ3KO), including responsiveness to cold exposure, diet-induced obesity, intolerance to glucose, dyslipidemia and lipolysis in white adipose tissue (WAT). ARβ3KO mice defend core temperature during cold exposure (4ºC for 5h), with faster BAT thermal response to Norepinephrine (NE) infusion when compared to wild-type (WT) mice...
September 26, 2016: Journal of Endocrinology
Heno F Lopes, Maria Lúcia Corrêa-Giannella, Fernanda M Consolim-Colombo, Brent M Egan
The association of anthropometric (waist circumference) and hemodynamic (blood pressure) changes with abnormalities in glucose and lipid metabolism has been motivation for a lot of discussions in the last 30 years. Nowadays, blood pressure, body mass index/abdominal circumference, glycemia, triglyceridemia, and HDL-cholesterol concentrations are considered in the definition of Metabolic syndrome, referred as Visceral adiposity syndrome (VAS) in the present review. However, more than 250 years ago an association between visceral and mediastinal obesity with hypertension, gout, and obstructive apnea had already been recognized...
2016: Diabetology & Metabolic Syndrome
Lubica Horvathova, Alexandra Padova, Andrej Tillinger, Jana Osacka, Jozef Bizik, Boris Mravec
Accumulated evidence indicates that sympathetic nerves may potentiate tumor growth, including melanoma. To elucidate possible mechanisms for this effect, we performed chemical sympathectomy by intraperitoneal (i.p.) injection of the neurotoxin 6-hydroxydopamine hydrobromide (100 mg/kg of body weight); in nine adult male C57BL/6J mice; nine control mice received i.p. vehicle (VEH). Seven days later, all mice were injected subcutaneously with 3 × 10(3) B16-F10 melanoma cells. Mice were euthanized 20 d after injection of melanoma cells, for measurement of tumor weight and expression of genes related to sympathetic signaling, apoptosis, hypoxia and angiogenesis in tumor tissue...
September 2016: Stress: the International Journal on the Biology of Stress
Jean-Luc Balligand
Overstimulation of the orthosympathetic system leads to cardiovascular cell and tissue damage through prolonged activation of β-1-2 adrenergic receptors (BARs). The more recent identification of the third isotype of BAR (B3AR) in cardiac myocytes and endothelial cells with a distinctive coupling and effect on cardiac function and remodelling introduced a new facet to this paradigm. In particular, B3AR is up-regulated in cardiac disease and less prone to homologous desensitization, which may reinforce its influence on the diseased myocardium...
July 15, 2016: Cardiovascular Research
China Chien, Hsi-Yang Wu
INTRODUCTION: Previous studies have suggested that the onset of alpha- (α) and beta- (β) adrenergic receptor activity is delayed in young animals. The use of alpha1- (α1-) antagonists for dysfunctional voiding, and beta3- (β3-) agonists for overactive bladder in younger children may not be indicated if maturation is required before bladder and urethral adrenergic receptors are active. OBJECTIVE: To determine the sex- and age-dependent responses of the bladder and external urethral sphincter (EUS) to α- and β-adrenergic agents in neonatal and young adult rats...
April 2016: Journal of Pediatric Urology
Hongyi Zhou, Xinnuo Lei, Tyler Benson, James Mintz, Xiaojing Xu, Ruth B Harris, Neal L Weintraub, Xiaoling Wang, Weiqin Chen
Mutations in BSCL2/SEIPIN cause Berardinelli-Seip congenital lipodystrophy type 2 (BSCL2), but the mechanisms whereby Bscl2 regulates adipose tissue function are unclear. Here, we generated adipose tissue (mature) Bscl2 knockout (Ad-mKO) mice, in which Bscl2 was specifically ablated in adipocytes of adult animals, to investigate the impact of acquired Bscl2 deletion on adipose tissue function and energy balance. Ad-mKO mice displayed reduced adiposity and were protected against high fat diet-induced obesity, but not insulin resistance or hepatic steatosis...
October 2015: Journal of Lipid Research
L H Petersen, M L Burleson, D B Huggett
β₃-adrenergic receptors (AR) are important in teleost cardiovascular regulation. To date, it is unknown whether temperature acclimation changes ß₃-AR functionality and consequently the involvement of this AR subtype in teleost cardiac regulation. Common carp (Cyprinus carpio) were acclimated at 12 °C or 23 °C (minimum 3 weeks) after which cardiovascular variables (cardiac output (Q), stroke volume (Sv) and heart rate (fH)) were measured upon injection of the ß₃-AR agonist, BRL(37344), and antagonist, SR(59230A)...
July 2015: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
Robin Hertzberg, Guillermo Monreal Santiago, Christina Moberg
A novel methodology to produce highly enantioenriched N-(2-ethylamino)-β-amino alcohols was developed. These compounds were obtained from O-(α-bromoacyl) cyanohydrins, which were synthesized by the minor enantiomer methodology employing a Lewis acid and a biocatalyst, followed by nucleophilic substitution with amines and reduction. The importance of the developed methodology was demonstrated by completing a highly enantioselective total synthesis of the β3-adrenergic receptor agonist Solabegron.
March 6, 2015: Journal of Organic Chemistry
Nichola Thompson, Korinna Huber, Mirijam Bedürftig, Kathrin Hansen, Jennifer Miles-Chan, Bernhard H Breier
BACKGROUND: A number of different pathways to obesity with different metabolic outcomes are recognised. Prenatal undernutrition in rats leads to increased fat deposition in adulthood. However, the form of obesity is metabolically distinct from obesity induced through other pathways (e.g. diet-induced obesity). Previous rat studies have shown that maternal undernutrition during pregnancy led to insulin hyper-secretion and obesity in offspring, but not to systemic insulin resistance. Increased muscle and liver glycogen stores indicated that glucose is taken up efficiently, reflecting an active physiological function of these energy storage tissues...
2014: Nutrition & Metabolism
E Montaudon, M A Abdelkrim, J-C Desfontis, M Y Mallem
PURPOSE: To analyze vascular reactivity changes in response to immunization protocols with antigens corresponding to the second extracellular loop of -β3 and -β1 and 3 adrenergic receptors (AR). METHODS: Lewis rats were immunized for 3months with peptidic sequences corresponding to the second extracellular loop of β3-AR or β1 and 3-AR. Specific β3-AR antibodies were characterized by Elisa and purified using "Proteus Protein G" kit. Their functionality were tested in rabbit isolated ventricular cardiomyocytes...
June 2014: Annales de Cardiologie et D'angéiologie
Claudius Füllhase, Roberto Soler, Christian Gratzke
PURPOSE OF REVIEW: Improved understanding of the pathogenesis of lower urinary tract symptoms (LUTS) has led to the development of new drugs to treat male LUTS. The review aims to give an overview to the new drugs and to compounds in the pipeline. RECENT FINDINGS: Tadalafil, a phosphodiesterase type 5 inhibitor, is a drug newly approved for the treatment of male LUTS and a true new challenger for the current standard treatment with alpha1 blockers, particularly in men with concomitant erectile dysfunction...
January 2014: Current Opinion in Urology
Yan-Hui Gao, Hai-Bo Gao, Ning-Ning Di, Yi-Hui Kong, Wei-Min Li
OBJECTIVE: To observe the effects of beta3-adrenergic receptor(beta3-AR) antagonist on myocardial uncoupling protein 2 (UCP2) expression and energy metabolism in chronic heart failure rats. METHODS: Seven weight-matched normal adult rats (control group), 18 isoproterenol (ISO) induced heat failure (HR) rats (ISO group) and 21 ISO induced heart failure rats but received specific beta3-AR inhibitor SR59230A (ISO+ SR59230A group) for 6 weeks were included in this research...
July 2013: Chinese Journal of Applied Physiology
Pelin Tanyeri, Mehmet Emin Buyukokuroglu, Oguz Mutlu, Guner Ulak, Furuzan Yildiz Akar, Ipek Komsuoglu Celikyurt, Bekir Faruk Erden
Anxiety disorders are the most common behavioral disorders, and they exhibit high comorbidity rates. The aim of the present study was to confirm the effects of Amibegron, the first selective beta 3 adrenergic agent, on anxiety and to demonstrate that different serotoninergic receptor subtypes are involved in this effect. We administered the serotonin 5-HT1A receptor antagonist WAY-100635, the serotonin 5-HT2A receptor antagonist Ketanserin and the serotonin 5-HT3 receptor antagonist Ondansetron in mice and evaluated their performance in the elevated plus-maze test...
September 2013: Pharmacology, Biochemistry, and Behavior
Vabren L Watts, Fernando M Sepulveda, Oscar H Cingolani, Alice S Ho, Xiaolin Niu, Rosa Kim, Karen L Miller, Koenraad Vandegaer, Djahida Bedja, Kathleen L Gabrielson, Gerald Rameau, Brian O'Rourke, David A Kass, Lili A Barouch
RATIONALE: Stimulation of β3-adrenoreceptors (β3-AR) blunts contractility and improves chronic left ventricular function in hypertrophied and failing hearts in a neuronal nitric oxide synthase (nNOS) dependent manner. nNOS can be regulated by post-translational modification of stimulatory phosphorylation residue Ser1412 and inhibitory residue Ser847. However, the role of phosphorylation of these residues in cardiomyocytes and β3-AR protective signaling has yet to be explored. OBJECTIVE: We tested the hypothesis that β3-AR regulation of myocyte stress requires changes in nNOS activation mediated by differential nNOS phosphorylation...
September 2013: Journal of Molecular and Cellular Cardiology
Tarik Hadi, Marina Barrichon, Pascal Mourtialon, Maeva Wendremaire, Carmen Garrido, Paul Sagot, Marc Bardou, Frédéric Lirussi
The beta3 adrenergic receptor (B3-AR) reportedly induces cell proliferation, but the signaling pathways that were proposed, involving either Gs or Gi coupling, remain controversial. To further investigate the role of G protein coupling in B3-AR induced proliferation, we stimulated primary human myometrial smooth muscle cells with SAR150640 (B3-AR agonist) in the absence or presence of variable G-protein inhibitors. Specific B3-AR stimulation led to an Erk1/2 induced proliferation. We observed that the proliferative effects of B3-AR require two Erk1/2 activation peaks (the first after 3min, the second at 8h)...
May 2013: Biochimica et Biophysica Acta
Massimo Dal Monte, Luca Filippi, Paola Bagnoli
Beta-adrenergic receptors (β-ARs) play a role in angiogenic processes that characterize neovascularization-associated retinal diseases, but the role of β3-ARs has not been disclosed yet. We used ex vivo retinal explants to investigate the role of β3-ARs in regulating vascular endothelial growth factor (VEGF) release associated with hypoxia. Whether nitric oxide (NO) mediates β3-AR regulation of VEGF release was also investigated. β3-AR activation was obtained using BRL 37344, whereas SR59230A, L-748,337, or specific siRNAs were used to block β3-ARs...
April 2013: Naunyn-Schmiedeberg's Archives of Pharmacology
Kazuo Oguri, Toshiki Tachi, Toshio Matsuoka
AIM: To investigate the association between Trp64Arg polymorphism of the beta3-adrenergic receptor (ADRB3) gene and total fat mass, abdominal fat distribution, other metabolic derangements and metabolic syndrome (MS) in Japanese children. METHODS: Molecular screening of the ADRB3 gene polymorphism (Trp64Trp, Trp64Arg and Arg64Arg) was carried out in 132 children aged 6-12 years: 73 were obese (45 boys) and 59 were not obese (27 boys). Visceral fat (VF) and subcutaneous fat (SF) area were measured using magnetic resonance imaging, blood pressure, lipid and glucose profiles...
June 2013: Acta Paediatrica
Jean-Luc Balligand
Beta3-adrenoreceptors (B3AR) are traditionally known as metabolic receptors in adipose tissue, but came into focus in the cardiovascular field after our demonstration of their expression in human cardiac myocytes and endothelial cells, where they mediate endothelium-dependent relaxation of coronary resistance vessels through production of both nitric oxide and endothelium-dependent hyperpolarization factor(s) (EDHF). B3AR are also expressed at the plasma membrane of rodent and human cardiac myocytes. Notably, their expression is increased in several forms of human cardiomyopathies, which raises questions about their adaptive or maladaptive role in myocardial remodelling...
February 2013: Current Drug Delivery
Akiko Takenaka, Shin Nakamura, Fusako Mitsunaga, Miho Inoue-Murayama, Toshifumi Udono, Bambang Suryobroto
UNLABELLED: Adrenergic-receptor beta2 (ADRB2) and beta3 (ADRB3) are obesity genes that play a key role in the regulation of energy balance by increasing lipolysis and thermogenesis. The Glu27 allele in ADRB2 and the Arg64 allele in ADRB3 are associated with abdominal obesity and early onset of non-insulin-dependent diabetes mellitus (NIDDM) in many ethnic groups. Peroxisome proliferator-activated receptor γ (PPARG) is required for adipocyte differentiation. Pro12Ala mutation decreases PPARG activity and resistance to NIDDM...
2012: PloS One
Sirirat Likanonsakul, Tippawan Rattanatham, Siriluk Feangvad, Sumonmal Uttayamakul, Wisit Prasithsirikul, Somkid Srisopha, Ravee Nitiyanontakij, Pimrapat Tengtrakulcharoen, Maciej Tarkowski, Agostino Riva, Emi E Nakayama, Tatsuo Shioda
The present study aimed to evaluate the role of genetic polymorphisms in the emergence of lipoatrophy or lipodystrophy in HIV-infected patients with antiretroviral therapy (ART) in Thailand. Position 455 upstream of the Apolipoprotein C3 gene (ApoC3 T-455C, rs2854116), codon 64 of the Beta3 adrenergic receptor gene (ARβ3 Tcod64C, rs4994), and position 670 upstream of the Fas gene (Fas A-670G, rs1800682) were genotyped in 829 HIV-infected Thai patients who had started ART. Crude and adjusted incidence rate ratios (IRR) were calculated using Poisson regression...
January 2013: AIDS Research and Human Retroviruses
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