Abstract：
:The regulation of G protein-coupled receptor expression is important in the physiology of an organism and can occur at any of the steps between gene transcription to turnover of the receptor protein itself. Agonist stimulation causes receptor desensitization, which is characterized by a rapid reduction in response to the agonist. Down-regulation often occurs after prolonged agonist treatment and is manifested as a decrease in receptor density. Short term desensitization results from a rapid (in minutes) and reversible uncoupling of the receptor-G protein complex, followed by sequestration and/or internalization of receptors from the cell surface. Receptors are not degraded as removal of agonist rapidly restores receptor function. Down-regulation, on the other hand, displays a much longer time-course (hours to days) and is characterized by a decrease in receptor density as determined by radioligand binding. Removal of agonist will only slowly reverse down-regulation, because new receptor synthesis is required in most cases (1;2). The mechanism of receptor down-regulation is not well understood, but may include an accelerated rate of removal of receptors, a decrease in the rate of appearance of receptors, or both. Our previous studies have shown significant differences in the concentration of agonist required to produce down-regulation of alpha-2 adrenergic receptor subtypes (3;4). Here we review the mechanisms and molecular determinants for receptor down-regulation as well as our own data exploring the subtype-specific differences in alpha-2 receptor down-regulation. We find that the extent and time-course of agonist-induced down-regulation occurs in a similar fashion regardless of the receptor subtype or the cell line in which it is expressed. The mechanism for receptor down-regulation in all cases is an increase in the rate of receptor disappearance.
journal_name
Life Scijournal_title
Life sciencesauthors
Heck DA,Bylund DBdoi
10.1016/s0024-3205(98)00091-5subject
Has Abstractpub_date
1998-01-01 00:00:00pages
1467-72issue
17-18eissn
0024-3205issn
1879-0631pii
S0024-3205(98)00091-5journal_volume
62pub_type
杂志文章,评审相关文献
LIFE SCIENCES文献大全abstract：AIMS:The present study aimed to verify changes in cerebellar and plasmatic expression of miRNAs after the chronic consumption of ethanol and caffeine in the UChB rat, an experimental model for alcoholism. MATERIAL AND METHODS:Male rats at 5 months of age, were divided into the following groups (n = 10/group): 1. Ethan...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2019.05.016
更新日期：2019-07-15 00:00:00
abstract：AIMS:The aim of this study is to determine whether Nkx2.5 transfection of transplanted bone marrow mesenchymal stem cells (MSCs) improves the efficacy of treatment of adriamycin-induced heart failure in a rat model. MAIN METHODS:Nkx2.5 was transfected in MSCs by lentiviral vector transduction. The expressions of Nkx2....
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2017.06.014
更新日期：2017-08-01 00:00:00
abstract：:The epicardial release of immunoreactive atrial natriuretic peptides (ir-ANPs) in inside-out perfused rabbit atria has been reported. In order to determine the presence of ir-ANPs in pericardial fluid and to evaluate their biochemical characteristics, we measured the concentration of ir-ANPs in pericardial fluid obtai...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(90)90514-r
更新日期：1990-01-01 00:00:00
abstract：:Neuron specific enolase (NSE), an isoenzyme of the glycolytic enzyme enolase, has been established by immunocytochemical means as a marker of morphological and functional maturation in central neurons and appears late in development. However, little is known about the presence of NSE in developing peripheral neurons a...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(84)90598-8
更新日期：1984-01-16 00:00:00
abstract：:Aberrant methylation of promoter CpG islands (CGIs) can inactivate the expression of many tumor suppressor genes and play an important role in the carcinogenesis of gastric cancer. The tumor suppressor gene RB1, which encodes a cell cycle regulator, is hypermethylated and downregulated in multiple kinds of cancer. Act...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.118580
更新日期：2020-12-15 00:00:00
abstract：:Examination was made of the effects of 17 synthetic and naturally occurring flavonoids on human lymphocyte proliferation in the presence of concanavalin A as a mitogen. Twelve of the flavonoids examined were mono-hydroxy or methoxy derivatives. The mitogen-induced response of lymphocytes was evaluated from the extent ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(89)90028-3
更新日期：1989-01-01 00:00:00
abstract：:Herba Epimedii is an important medicinal plant which has been used in various traditional Chinese formulations for thousands of years as well as in modern proprietary traditional Chinese medicine products. It has extensive clinical indications, especially for the treatment of sexual dysfunction and osteoporosis. There...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2015.01.006
更新日期：2015-04-01 00:00:00
abstract：:Acute and chronic opiate exposure impairs the emptying of bile from the gallbladder. In this study, the effects of a 4-day morphine regimen on bile composition were examined. Bile acids and phospholipids concentration of bile obtained from the gallbladder of female morphine-treated (MT) guinea pigs were reduced by 60%...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(93)90231-q
更新日期：1993-01-01 00:00:00
abstract：:Cystic fibrosis (CF) remains a major problem in human genetics and cell pathophysiology. It is a single gene trait caused by a mutation on the long arm of chromosome 7. Among its expressions are abnormal regulation of chloride channels and/or microobstructions in exocrine tissues. Here, evidence is presented that mito...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/0024-3205(89)90389-5
更新日期：1989-01-01 00:00:00
abstract：:This study examines the influence of ovariectomy and administration of a pharmacologic dose of estradiol on amylase release from isolated-dispersed rat pancreatic acini and cholecystokinin receptors on rat acinar cell membranes. Rats were sham ovariectomized (intact) or ovariectomized (Ovx) and 21 day timed release pe...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(91)90281-f
更新日期：1991-01-01 00:00:00
abstract：:The role of serotonin (5-HT) in the regulation of steroidogenesis in the ovary via 5-HT2 receptor was studied in normal cycling rats and their preovulatory follicles. Oral administration of ketanserin (KET), a selective 5-HT2 antagonist, at 10 mg/kg BW at 1100h on the day of proestrus resulted in a marked decrease in ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(93)90713-d
更新日期：1993-01-01 00:00:00
abstract：:Chronic voluntary running of mice is known to increase the circadian peak of plasma corticosterone without change in the level of adrenocorticotropic hormone (ACTH). In order to investigate how chronic exercise modulates the circadian HPA axis, we used two weeks of voluntary wheel running of mice and confirmed the sig...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2006.10.023
更新日期：2007-01-30 00:00:00
abstract：:Despite the considerable number of published studies in the field of S-nitrosothiols (RSNO), the determination of these compounds in biological samples still represents an analytical challenge, due to several technical obstacles and often long sample preparation procedures. Other problems derive from the intrinsic lab...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2010.10.024
更新日期：2011-01-17 00:00:00
abstract：:The kinetic parameters of serotonin (5-HT) uptake and imipramine binding of the synaptosomes and blood platelets of male Fawn-hooded rats, which have a 5-HT storage abnormality, and normal Sprague-Dawley rats were compared. The Vmax for 5-HT uptake of synaptosomes from Fawn-hooded rats was significantly greater than t...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90792-0
更新日期：1983-08-01 00:00:00
abstract：:More than 140 thousands of women suffer from endometrial carcinoma in the worldwide, and over 40 thousand of the patients die before and after in surgery and chemoradiotherapy because of its metastasis. However, its molecular mechanism is much less known compared to other cancers. In this study, we demonstrated that l...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117295
更新日期：2020-02-15 00:00:00
abstract：:The additive effects of combined valsartan and spironolactone on plasma and cardiac aldosterone escape were evaluated in spontaneously hypertensive rats (SHRs). Twenty-four SHRs were treated with valsartan (30 mg/kg body weight per day), spironolactone (20 mg/kg body weight per day) and a combination of both for 4 mon...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2004.04.012
更新日期：2004-08-27 00:00:00
abstract：:Net water, Na+, Cl- and HCO3- fluxes were measured in in vivo rabbit ileal loops, while mucus secretion was assessed by measuring the glycoprotein or total sialic acid secreted into the lumen, or by measuring the luminal fluid viscosity. Inoculating loops with cholera enterotoxin (CT) produced a sustained secretion of...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90220-5
更新日期：1983-02-21 00:00:00
abstract：:From the fruiting bodies of the edible mushroom Flammulina velutipes a single-chained ribosome inactivating protein with a molecular weight of 13.8 kDa was isolated with a procedure involving ion exchange chromatography on DEAE-cellulose and SP-Sepharose and affinity chromatography on Affi-gel blue gel. The protein wa...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(01)01023-2
更新日期：2001-03-23 00:00:00
abstract：:Thirty-four novel, diaryl ω-(isothiocyanato)alkylphosphonates with chlorine atom and methoxy, dimethoxy, methylsulfanyl, or methoxycarbonyl groups at ortho, meta, or para positions of the phenyl ring, and with an unbranched alkyl chain (n = 2-6) were designed and synthesized in a one-pot reaction in 11-76% yields. All...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2019.01.020
更新日期：2019-02-15 00:00:00
abstract：:Our previous indirect evidences suggested that the adrenergic nervous system is involved in the mechanisms responsible for the time-dependent changes in the effects of furosemide in Wistar rats. In the present study, the role of this system was examined more directly by means of 6-hydroxydopamine-induced sympathectomy...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(90)90111-4
更新日期：1990-01-01 00:00:00
abstract：:Alterations in the cyclic AMP-dependent protein kinase activity ratio in response to putative neurotransmitters and other cyclic AMP-elevating agents in intact cerebral cortical slices and Krebs-Ringer particulate preparations from cerebral cortex were examined. Both norepinephrine (30 microM) and forskolin (20 microM...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(85)90629-0
更新日期：1985-07-08 00:00:00
abstract：:Male, adult mice of the Binghamton heterogeneous stock received one of two doses of ethanol (1.0 g/kg or 2.0 g/kg in saline) alone or in combination with the calcium (Ca2+) slow channel blocker, verapamil (5.45 mg/kg in 25% v/v ethanol in saline). Hypothermic responses and motor incoordination were assessed in terms o...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(86)90357-7
更新日期：1986-12-01 00:00:00
abstract：:Nitric oxide (NO) may play an important regulatory role in airway function. We have, thus, investigated in vitro whether epithelium derived NO may modulate cholinergic neurotransmission, via release of NO in guinea pig trachea, by using L-arginine (L-ARG), a precursor of NO synthesis, and L-N(G)-nitro-arginine-methyl-...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(95)00053-9
更新日期：1995-02-17 00:00:00
abstract：:We find a significantly lower level of specific [3H]nicotine binding in the fetal rat forebrain of 20 day gestational age as compared to adult rat tissue, and a progressive increase in the [3H]nicotine binding in the early neonatal forebrain, reaching adult level at 14-28 days of age. The maximal binding sites (Bmax) ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(86)90057-3
更新日期：1986-02-17 00:00:00
abstract：AIMS:The aim of this study was to find out a mesenchymal stem cells (MSCs) source from human dental tissues of the same donor (follicle, papilla and pulp), which exhibits higher neurogenic differentiation potential in vitro. MAIN METHODS:MSCs were isolated from dental tissues (follicle, papilla and pulp) by digestion ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2016.04.026
更新日期：2016-06-01 00:00:00
abstract：:Rats administered cocaine 10 mg/kg i.p. exhibited hyperlocomotion which occurred within 5 min post injection. Subsequently, rats were injected with 10 mg/kg cocaine and brain and serum concentrations of cocaine were measured at 5, 10, and 20 min post injection. Within this time frame, cocaine concentration in limbic b...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(94)00339-4
更新日期：1994-01-01 00:00:00
abstract：:The regions of muscarinic receptors that specify G-protein-coupling and ligand-binding have been defined in several recent studies. Overall, these studies have shown that amino acids within the third cytoplasmic loop of the receptors define their selectivity for different G-proteins, and that multiple, discontinuous e...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/0024-3205(93)90295-e
更新日期：1993-01-01 00:00:00
abstract：:Based on the finding of decreased mitochondrial complex I activity in the substantia nigra of patients with Parkinson's disease, we propose that the consequent reduction of ATP synthesis and increased generation of reactive oxygen species may be a possible cause of nigrostriatal cell death. Since sulfhydryl groups are...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/s0024-3205(98)00472-x
更新日期：1999-01-01 00:00:00
abstract：:The thyrotropin receptor is proposed to contain both a glycoprotein and a ganglioside component. Monoclonal antibodies have been developed against soluble thyroid TSH receptor preparations and using Graves' lymphocytes. These show that initial recognition of thyrotropin requires the glycoprotein component, but that mo...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90170-4
更新日期：1983-01-03 00:00:00
abstract：:Repeated, low-intensity electrical stimulation of the heart gradually leads to the development of electrocardiographic abnormalities that culminate in cardiac arrhythmias, mainly A-V block in the isolated heart frog and ventricular and supraventricular tachyarrhythmias in the canine heart in situ. The pattern of devel...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(88)90437-7
更新日期：1988-01-01 00:00:00
