Abstract:
:The distribution and binding characteristics of the radioligand (-)-[125I]-cyanopindolol (CYP) have been examined in slide mounted mouse kidney sections, using the technique of in vitro labelling and autoradiography. (-)-[125I]-CYP binding to sections was of high affinity (KD = 55.8 pmol/l, s.e.m. = 8.1, n = 4) to a single population of non-interacting sites (nH = 0.95, s.e.m. = 0.01, Bmax = 0.74 fmol/section, s.e.m. = 0.12, n = 4) and stereoselective with respect to the (-)- and (+)-isomers of both propranolol and pindolol. Autoradiographic studies showed that (-)-[125I]-CYP binding was localized to areas in the renal cortex and medulla. Both cortical and medullary binding were abolished by the inclusion of (-)-propranolol (1 mumol/l) in the incubation medium, whereas (-)-isoprenaline (200 mumol/l) selectively abolished cortical binding. Medullary binding could be prevented by the inclusion of the lipophilic compounds cinanserin (10 mumol/l), haloperidol (10 mumol/l) or phentolamine (10 mumol/l), either alone or together or by washing at 37 degrees C. These results suggest that medullary binding sites are lipid rather than receptor-related. In conclusion, in mouse kidney sections, (-)-[125I]-CYP binds to discrete areas in the cortex and medulla. Cortical binding sites have the molecular characteristics of beta-adrenoceptors while medullary binding sites are lipid-related. Caution should therefore be exercised when defining non-specific binding of lipophilic radioligands. The autoradiographic technique is useful for discriminating between receptor and non-receptor binding sites.
journal_name
Clin Exp Pharmacol Physioljournal_title
Clinical and experimental pharmacology & physiologyauthors
Lew R,Summers RJdoi
10.1111/j.1440-1681.1986.tb00339.xsubject
Has Abstractpub_date
1986-03-01 00:00:00pages
211-21issue
3eissn
0305-1870issn
1440-1681journal_volume
13pub_type
杂志文章abstract::1. Hepatic sulphobromophthalein (BSP) transport was studied in guinea-pigs pretreated intraperitoneally with 0.7 ml of diethyl maleate to depress hepatic glutathione levels. 2. Diethyl maleate depressed the hepatic transport of infused conjugated BSP from hepatocytes into bile without influencing hepatic uptake. 3. Un...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1980.tb00117.x
更新日期:1980-11-01 00:00:00
abstract::1. The actions of lidocaine on cardiac pacemaker rhythms were studied in anaesthetized dogs and in Purkinje fibres from hearts of the same animals. 2. In vivo, lidocaine (1 mg/kg, intravenously) slowed the sino-atrial (SA) node rhythm (-5.0%), and (during vagal stimulation) prolonged ventricular standstill by +25.1% a...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1991.tb01429.x
更新日期:1991-03-01 00:00:00
abstract::1. Heterogeneity in the receptors for the neuropeptide calcitonin gene-related peptide (CGRP) has been apparent for nearly 20 years. This is most clearly manifested in the observation of CGRP(8-37)-sensitive and -insensitive populations of CGRP-activated receptors. The pA(2) values for CGRP(8-37) in excess of 7 are wi...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1111/j.1440-1681.2007.04703.x
更新日期:2007-10-01 00:00:00
abstract::The circulating miRNAs are dysregulated in non-small cell lung cancer (NSCLC) and have great promise for clinical diagnosis. The aim of this study was to screen and evaluate the reliability and diagnostic efficiency of candidate serum miRNAs for NSCLC diagnosis. We found that miR-21 and let-7a were significantly dysre...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 信件
doi:10.1111/1440-1681.12977
更新日期:2018-10-01 00:00:00
abstract::β-Glucans have been reported to be potent adjuvants in stimulating innate and adaptive immune responses. The aim of the present study was to determine the immunohematopoietic effects of Imunoglucan (HEBRON) following its oral administration to normal and Ehrlich ascites tumour (EAT)-bearing mice. Mice were treated wit...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2011.05655.x
更新日期:2012-03-01 00:00:00
abstract::1. Mast cells cultured from human peripheral blood have been used as a cell model for functional studies of human mast cells, particularly human lung mast cells. However, the beta-adrenoceptor subtype expressed by these cultured cells has not been identified. The aim of the present study was to characterize pharmacolo...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2006.04435.x
更新日期:2006-08-01 00:00:00
abstract::1. The purpose of this study was to determine whether hepatic mitochondria of guinea-pigs with spontaneous diabetes mellitus differ from those of non-diabetic guinea-pigs in the oxidation of fatty acids, the activity of beta-hydroxybutyrate dehydrogenase, or respiration-linked oxidative phosphorylation. During the cou...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1978.tb00674.x
更新日期:1978-05-01 00:00:00
abstract::Both opiates and dopamine play important roles in learning and memory. Although synergistic action between these two neurotransmitters has been found, their functional roles remain unclear. Here, low dose morphine (2.5 mg/kg) and low dose dopamine receptor agonists (apomorphine 0.05 mg/kg; SKF38393 0.01 mg/kg; bromocr...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/1440-1681.12889
更新日期:2018-04-01 00:00:00
abstract::The beta-receptor stimulant effects of Sm220Cl, dl-N-(1,1-dimethyl-3-phenylpropyl)-2-hydroxy-2-(3,4-dihydroxy-2-methoxyphenyl)ethylamine, and (-)-isoprenaline have been compared in isolated atrial (beta1) and tracheal (beta2) preparations from guinea-pigs and cats. 2. The compounds were also tested for their ability t...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1977.tb02672.x
更新日期:1977-07-01 00:00:00
abstract::We evaluated the role of deferasirox therapeutic drug monitoring in order to avoid toxicity or treatment failure. Plasma concentrations, measured between two consecutive liver iron determinations, were determined at the end of dosing interval. Fifty-four β-thalassemic adult patients were enrolled: 50% were males; medi...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 信件
doi:10.1111/1440-1681.12879
更新日期:2018-02-01 00:00:00
abstract::Hypoxia-inducible factor-1 alpha (HIF-1α) and nuclear receptor related-1 (Nurr1) play pivotal roles in the development and survival of dopaminergic neurons, and deficiencies in these genes may be involved in Parkinson's disease (PD) pathogenesis. Recently, anthelminthic benzimidazoles were shown to promote HIF-1α tran...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/1440-1681.13162
更新日期:2019-12-01 00:00:00
abstract::1. Physical movement is accompanied by coordinated changes in respiratory and cardiovascular activity proportional to the metabolic demands of the locomotor task. Cardiorespiratory changes include increases in ventilation, blood pressure and heart rate, as well as altered regional sympathetic nerve activity and blood ...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1046/j.1440-1681.2002.03610.x
更新日期:2002-01-01 00:00:00
abstract::1. Stimulation of the mesolimbic dopamine system, by micro-injection of the substance P analogue [pGlu5,MePhe8,Sar9] substance P (DiMe-C7) into the ventral tegmental area induced a prolonged increase in blood pressure and circulating levels of vasopressin. 2. In the present study, this treatment produced a significant...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1998.tb02264.x
更新日期:1998-07-01 00:00:00
abstract::1. In the present study, we investigated aqueous extracts of Anoectochilus formosanus (AFE) for antihyperglycaemic and anti-oxidant effects in diabetic rats induced by streptozotocin (STZ). 2. Diabetic rats were randomly divided into groups and treated orally by gavage with vehicle (distilled water) or AFE (1 and 2 g/...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.2002.03717.x
更新日期:2002-08-01 00:00:00
abstract::1. In the [(13)C]-octanoic acid breath test, the time versus pulmonary [(13)CO(2)] excretion rate curve is analysed using mathematical curve-fitting techniques to calculate gastric emptying parameters. Thus, the goodness-of-fit highly influences the accuracy of the breath test. However, a double-peaked [(13)CO(2)] exc...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 临床试验,杂志文章
doi:10.1111/j.1440-1681.2005.04235.x
更新日期:2005-07-01 00:00:00
abstract::1. Two patients with angiotensin-responsive aldosterone-producing adenoma (APA) and one with adrenal cortical carcinoma demonstrated autonomous secretion of cortisol as well as of aldosterone. 2. The response of cortisol and of aldosterone to ACTH did not differentiate between the two APA which secreted cortisol and t...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1990.tb01300.x
更新日期:1990-03-01 00:00:00
abstract::1. After a severe burn, a marked decrease in myocardial blood flow results in ischaemic and hypoxic injury, which subsequently leads to apoptosis or necrosis. Phosphatidylinositol 3-kinase (PI3-K)/Akt is an important intracellular signal transduction molecule that regulates cell proliferation, differentiation, glucose...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2010.05355.x
更新日期:2010-05-01 00:00:00
abstract::1. The possibility that the anticonvulsant activity of the benzodiazepines, diazepam and clobazam, is related to changes in EEG parameters, particularly beta activity, was investigated in amygdaloid kindled rats. 2. The effects of diazepam (1, 2, 4, 8 and 16 mumols/kg), administered intraperitoneally (i.p.), clobazam ...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1988.tb01015.x
更新日期:1988-10-01 00:00:00
abstract::1. Although measuring the rate of firing of multi-unit muscle sympathetic nerve activity (MSNA) has provided important information in many aspects of cardiovascular medicine, measuring single-unit vasoconstrictor activity provides a better understanding of the possible mechanisms underlying disturbed sympathetic nervo...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1111/j.1440-1681.2008.04905.x
更新日期:2008-04-01 00:00:00
abstract::Non-alcoholic fatty liver disease (NAFLD) has been considered as a multi-factorial metabolic syndrome. MicroRNA-375 (MiR-375) was significantly up-regulated in serum of NAFLD patients and the role of miR-375 was addressed as a putative biomarker of NAFLD progression. However, the specific function of miR-375 in the pr...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/1440-1681.12940
更新日期:2018-08-01 00:00:00
abstract::1. The aim of the present study was to assess the bioequivalence of two cefadroxil products, namely Ultracef (a reference product) in the form of a 500 mg capsule (produced by Bristol-Myers Squibb Laboratories, Princeton, NJ, USA) and Roxil (a test product) in the form of a 500 mg capsule (produced by Tabuk Pharmaceut...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1111/j.1440-1681.2004.04012.x
更新日期:2004-07-01 00:00:00
abstract::1. In the present study, we attempted to clarify whether the antidiabetic drug miglitol, an alpha-glucosidase inhibitor, has a protective effect against anginal ischaemia. We had reported previously that miglitol reduces myocardial infarct size through inhibition of glycogenolysis during ischaemia in rabbits. However,...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2005.04269.x
更新日期:2005-10-01 00:00:00
abstract::1. Angiotensin (Ang)II is involved in responses to hypovolaemia, such as sodium appetite and increase in blood pressure. Target areas subserving these responses for AngII include the cardiovascular system in the periphery and the circumventricular organs in the brain. 2. Conflicting data have been reported for the rol...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1046/j.1440-1681.2000.03262.x
更新日期:2000-05-01 00:00:00
abstract::1. Intravenous endothelin-1 releases endothelium-derived relaxing factor (EDRF) and prostacyclin from the lungs, and substantial pulmonary clearance is claimed. Since these vaso-active substances could alter the haemodynamic effects of endothelin-1, the effects of boluses of endothelin-1 injected intravenously and int...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1994.tb02521.x
更新日期:1994-04-01 00:00:00
abstract::1. In an isolated right atrial preparation, an increase in right atrial pressure (RAP) produces an increase in atrial rate. This rate response is larger and occurs faster when there is background vagal or muscarinic stimulation. 2. We hypothesized that in the latter situation, an increase in RAP antagonizes the effect...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2010.05408.x
更新日期:2010-09-01 00:00:00
abstract::1. It is a central thesis of this review that in clinical and experimental pharmacology and physiology the goal of statistical analysis should be to minimize the risk of making any false-positive inferences from the results of an experiment (experimentwise Type I error). 2. It is common in clinical and experimental ph...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 社论,评审
doi:10.1111/j.1440-1681.1991.tb01468.x
更新日期:1991-06-01 00:00:00
abstract::1. To understand the roles of a putative hypertension gene in the chromosome 1 quantitative trait locus (QTL) region, the response to restraint stress was studied in strains congenic for this QTL. 2. To establish congenic strains, the QTL region was introgressed from stroke-prone spontaneously hypertensive rats (SHRSP...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.2003.03860.x
更新日期:2003-07-01 00:00:00
abstract::1. We tested the effects of intravenous infusions of angiotensin II (AngII; 300 ng/kg per min) and the vasopressin V1 receptor agonist [Phe2,Ile3,Orn8]-vasopressin (30 ng/kg per min) on regional kidney perfusion in an extracorporeal circuit model in anaesthetized rabbits in which renal artery pressure (RAP) can be set...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.2000.03377.x
更新日期:2000-12-01 00:00:00
abstract::Apelin receptors (APJ) cross-talk with other G-protein-coupled receptors. However, the role of APJ interaction with opioid receptors (OPR) on the cardiovascular effects of apelin in hypertension is not clear. Renovascular hypertension was induced by placing a Plexiglas clip on the left kidney of rats. After 16 weeks, ...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/1440-1681.12860
更新日期:2018-02-01 00:00:00
abstract::1. The chronotropic and inotropic effects of the anti-anginal agent SG-75 (2-nicotinamidoethyl nitrate) and 1-verapamil were investigated in isolated blood-perfused canine atrial preparations. The compounds were administered via the cannulated sinus node artery. 2. SG-75 induced a selective negative inotropic as oppos...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1980.tb00062.x
更新日期:1980-03-01 00:00:00