Autoradiographic analysis of (-)-[125I]-CYP binding in mouse kidney.


: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.


Lew R,Summers RJ




Has Abstract


1986-03-01 00:00:00












  • Extracellular fluid distribution in rats with chronic one- and two-kidney Goldblatt hypertension.

    abstract::1. The influence of the intact kidney on blood pressure, extracellular fluid volume (ECF, ferrocyanide space) and ECF volume distribution was studied in rats 60 days after constriction of the contralateral renal artery. 2. Renal artery constriction increased both blood pressure and ECF levels. The rise of both variabl...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Kunes J,Jelínek J

    更新日期:1979-09-01 00:00:00

  • An investigation of the influence of patient-related factors and comedications on lamotrigine clearance in patients with epilepsy.

    abstract::Lamotrigine (LTG) is one of the most widely used antiepileptic drugs. Confusion still exists in the literature as to the relative influence of age, body weight, and concomitant drug therapy on LTG pharmacokinetics. So, the objective of this study is to evaluate the influence of patient-related factors and comedication...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Baldoni AO,Freitas-Lima P,de Santi Ferreira FI,Martinez EZ,Queiroz RH,Sakamoto AC,Alexandre V,Perucca E,Pereira LR

    更新日期:2016-07-01 00:00:00

  • Effect of plasma cholesterol on red blood cell oxygen transport.

    abstract::1. Oxygen (O2) transfer from the blood to tissues is a function of the red blood cell (RBC) O2 saturation (SO2), the plasma O2 content being negligible. Under conditions of increased tissue O2 demand, the SO2 of arterial blood does not change appreciably (97%); however, the SO2 of mixed venous blood, equal to that of ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Buchwald H,O'Dea TJ,Menchaca HJ,Michalek VN,Rohde TD

    更新日期:2000-12-01 00:00:00

  • The hepatic transport of taurocholic acid in the rat: development of a mathematical model.

    abstract::1. The transport of taurocholic acid from portal blood to bile was studied in the anaesthetized rat by injecting a radiolabelled pulse of bile acid. 2. The transport process was very rapid, 50% of the dose being secreted within 5 min, and the total dose within 15 min. 3. The transport process had a large capacity. The...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Iser JH,Packer JS,Smallwood RA,Hoffman NE

    更新日期:1976-01-01 00:00:00

  • Therapeutic effect of green tea extract on advanced glycation and cross-linking of collagen in the aorta of streptozotocin diabetic rats.

    abstract::1. The therapeutic effect of green tea extract (GTE) on the aortic collagen content and its characteristics were investigated in streptozotocin diabetic rats. 2. Diabetes was induced in rats by a single intra peritoneal injection of streptozotocin (60 mg/kg bodyweight). Six weeks after diabetes induction, GTE was admi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Babu PV,Sabitha KE,Shyamaladevi CS

    更新日期:2006-04-01 00:00:00

  • Amelioration of L-thyroxine-induced hyperthyroidism by coumarin (1,2-benzopyrone) in female rats.

    abstract::1. The efficacy of coumarin (1,2-benzopyrone) was examined for the regulation of hyperthyroidism in female rats. 2. Coumarin was administered (10 mg/kg per day for 15 days) to l-thyroxine (L-T(4))-induced hyperthyroid as well as to euthyroid rats and changes in serum concentrations of thyroid hormones and in associate...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Panda S,Kar A

    更新日期:2007-11-01 00:00:00

  • Asymmetric dimethylarginine does not inhibit arginase activity and is pro-proliferative in pulmonary endothelial cells.

    abstract::Asymmetric dimethylarginine (ADMA) is an endogenously produced nitric oxide synthase (NOS) inhibitor. L-Arginine can be metabolised by NOS and arginase, and arginase is the first step in polyamine production necessary for cellular proliferation. We tested the hypothesis that ADMA would inhibit NOS but not arginase act...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Chen B,Strauch K,Jin Y,Cui H,Nelin LD,Chicoine LG

    更新日期:2014-07-01 00:00:00

  • Influence of somatostatin analogue (SMS 201-995, octreotide) on blood pressure in adrenocorticotrophin (ACTH) treated rats: role of hyperinsulinaemia in ACTH hypertension.

    abstract::1. The hypothesis that adrenocorticotrophin (ACTH)-induced hypertension is a consequence of steroid-induced hyperinsulinaemia was tested using the somatostatin analogue (sandostatin, octreotide) to inhibit insulin release in Sprague-Dawley (SD) rats (n = 41). 2. Octreotide (20 micrograms, twice daily) did not modify b...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Li M,Wong KS,Whitworth JA

    更新日期:1993-10-01 00:00:00

  • Significance of serine proteinase and matrix metalloproteinase systems in the destruction of human articular cartilage.

    abstract::1. During the destruction of articular cartilage, fibrinolytic enzymes and matrix metalloproteinases (MMP) may contribute to the related pathology. The activities, antigens and messenger RNA (mRNA) levels of urokinase-type plasminogen activator (uPA) and plasminogen activator inhibitor-1 (PAI-1) in articular cartilage...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Kikuchi H,Shimada W,Nonaka T,Ueshima S,Tanaka S

    更新日期:1996-10-01 00:00:00

  • Nitric oxide induced sinusoidal relaxation after a propranolol priming dose in the perfused rat liver reduces propranolol availability on subsequent dosing.

    abstract::1. The present study sought to explain the mechanism leading to reduced availability of propranolol when given after a priming dose in the single-pass perfused rat liver. 2. Extracellular sucrose space (as a measure of sinusoidal relaxation) in perfused rat liver before and after propranolol or propranolol and N(G)-ni...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Liu X,Zou Y,Khlentzos AM,Yang Y,Nikolovski J,Weiss M,Roberts MS

    更新日期:2010-10-01 00:00:00

  • Inhibition of nuclear translocation of transcription factor nuclear factor-kappa B induces FAS- as well as tumour necrosis factor-alpha-mediated apoptosis through downregulation of a conserved family of inhibitor of apoptosis 1.

    abstract::1. In the present study, we examined whether the nuclear transcription factor (NF)-kappaB activity plays a role in the determination of sensitivity to tumour necrosis factor (TNF)-alpha or agonistic Fas antibody (Ab) in human vascular smooth muscle cells (hVSMC). 2. To inhibit agonist-induced NF-kappaB activation in h...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Imanishi T,Hano T,Takarada S,Nishio I

    更新日期:2003-03-01 00:00:00

  • Effect of mineralocorticoids and salt loading on renin release, renal renin content and renal renin mRNA in mice.

    abstract::1. DOCA and 9 alpha-fludrocortisone were given to mice on a high-sodium diet for periods of up to 20 weeks, resulting in decreases in plasma renin concentration, renal renin concentration and renal renin mRNA with both treatments. 2. Plasma renin concentration was suppressed prior to suppression of renin mRNA and rena...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Barrett G,Morgan T,Smith M,Aldred P

    更新日期:1989-08-01 00:00:00

  • Effects of reserpine pretreatment on neuroeffector transmission in the vas deferens.

    abstract::1. The effects of reserpine pretreatment on neurotransmission in the guinea-pig vas deferens have been re-examined with a view to study the role of noradrenaline (NA) in mediating postjunctional electrical responses and, in particular, excitatory junction potentials (EJP). 2. Reserpine (5 mg/kg, i.p.) caused almost to...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Cunnane TC,Manchanda R

    更新日期:1989-06-01 00:00:00

  • Characterization of the acute cardiovascular effects of intravenously administered insulin-like growth factor-I in conscious Sprague-Dawley rats.

    abstract::1. Insulin-like growth factor (IGF)-I has acute effects on cardiovascular function, including a well-characterized vasodilator response in isolated arteries. In addition to increasing the release of nitric oxide, IGF-I also has effects on a variety of other signalling pathways that affect vascular tone, in particular ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Cao N,Lau S,Nguyen TT,White PJ

    更新日期:2006-12-01 00:00:00

  • Effect of placental growth factor in models of experimental pre-eclampsia and trophoblast invasion.

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Chau K,Bobek G,Xu B,Stait-Gardner T,Price W,Hennessy A,Makris A

    更新日期:2020-01-01 00:00:00

  • Demonstration of hereditarily accelerated proliferation in astrocytes derived from spontaneously hypertensive rats.

    abstract::1. We examined the proliferative rates of cultured astrocytes isolated from stroke-prone spontaneously hypertensive rats (SHRSP) and stroke-resistant spontaneously hypertensive rats (SHRSR). Wistar-Kyoto rats (WKY) were used as a control for SHRSP and SHRSR. 2. In the presence of 10% fetal bovine serum (FBS), the doub...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Yamagata K,Nara Y,Tagami M,Yamori Y

    更新日期:1995-09-01 00:00:00

  • Growth inhibitory effect of β-eudesmol on cholangiocarcinoma cells and its potential suppressive effect on heme oxygenase-1 production, STAT1/3 activation, and NF-κB downregulation.

    abstract::Cholangiocarcinoma (CCA) is a progressively fatal form of cancer originating from the malignant transformation of hepatic biliary cholangiocytes. The present study reports for the first time in vitro growth inhibitory activities of β-eudesmol, the bioactive sesquiterpenoid present in the rhizome of Atractylodes lancea...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Mathema VB,Chaijaroenkul W,Karbwang J,Na-Bangchang K

    更新日期:2017-11-01 00:00:00

  • Increased expression of calcium-sensing receptors induced by ox-LDL amplifies apoptosis of cardiomyocytes during simulated ischaemia-reperfusion.

    abstract::1. Acute myocardial infarction (AMI) is strongly associated with atherosclerosis, and is responsible for significant morbidity and mortality worldwide. The pathogenic mechanisms that underlie atherosclerosis and AMI are undefined at present. The calcium-sensing receptor (CaSR) is a member of the superfamily of G-prote...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Guo J,Li HZ,Zhang WH,Wang LC,Wang LN,Zhang L,Li GW,Li HX,Yang BF,Wu L,Wang R,Xu CQ

    更新日期:2010-03-01 00:00:00

  • Serum dopamine beta-hydroxylase (D beta H) levels during tilting in patients with spinal cord injuries.

    abstract::The activity of dopamine-beta-hydroxylase (D beta H) in the serum was measured in patients with quadriplegia and in healthy subjects. We assume that the plasma D beta H levels reflect sympathetic tone. Quadriplegics had significantly lower D beta H levels at rest. After head-up tilting a significant decrease in D beta...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Ohry A,Rabinowitz R,Korczyn AD

    更新日期:1980-07-01 00:00:00

  • Differential expression of GAS5 in rapamycin-induced reversion of glucocorticoid resistance.

    abstract::This study evaluates the association between the long noncoding RNA GAS5 levels and the anti-proliferative effect of the glucocorticoid (GC) methylprednisolone (MP) alone and in combination with rapamycin in peripheral blood mononuclear cells (PBMCs) obtained from healthy donors. The effect of MP, rapamycin, and MP pl...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Lucafò M,Bravin V,Tommasini A,Martelossi S,Rabach I,Ventura A,Decorti G,De Iudicibus S

    更新日期:2016-06-01 00:00:00

  • Pharmacology of a unique adenosine binding site in rat brain using a selective ligand.

    abstract::1. In order to further characterize the adenosine binding sites that we previously purified and termed P3 purinergic receptor-like protein (P3LP), a reliable binding assay method was developed using [3H]-5'-N-ethylcarboxamidoadenosine (NECA) as a radioligand and the newly developed high-affinity selective ligand 9-(6,...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Yoshioka K,Matsuda A,Nakata H

    更新日期:2001-04-01 00:00:00

  • Enhanced antitumour activity of doxorubicin and simvastatin combination loaded nanoemulsion treatment against a Swiss albino mouse model of Ehrlich ascites carcinoma.

    abstract::Doxorubicin (DOX) is the most commonly used anticancer drug; however, it has limited use because prolonged administration may result in severe cardiotoxicity. Simvastatin (SIM), generally prescribed for hypercholesterolaemia, has also shown salubrious results in the monotherapy or combinational drug therapy of differe...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Alkreathy HM,Alkhatib MH,Al Musaddi SA,Balamash KSA,Osman NN,Ahmad A

    更新日期:2019-05-01 00:00:00

  • Differential trafficking of saccharidic probes following aspirin in clinical tests of intestinal permeability in young healthy women.

    abstract::The effects of inflammatory changes on the absorption of different-sized probes and their permeability ratios are poorly understood. The aim of the present study was to determine the effects of a pharmacological agent on the permeability of the gut mucosa to saccharidic probes of larger and smaller molecular weight. P...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,随机对照试验


    authors: Sequeira IR,Lentle RG,Kruger MC,Hurst RD

    更新日期:2014-02-01 00:00:00

  • Role of calcium-activated potassium channels in the relaxation of tracheal smooth muscles by forskolin.

    abstract::1. The role of calcium-activated potassium (KCa) channels in bronchodilation produced by a direct adenylyl cyclase activator, forskolin, was investigated. The involvement of intracellular cyclic AMP (cAMP) in the process was also examined. 2. The isometric tension records from guinea-pig tracheal smooth muscles indica...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Hiramatsu T,Kume H,Kotlikoff MI,Takagi K

    更新日期:1994-05-01 00:00:00

  • Original and generic latanoprost for the treatment of glaucoma and ocular hypertension: are they really the same?

    abstract::We compared the intraocular pressure (IOP)-lowering effect and safety profile of latanoprost (Xalatan) with its generic variant, Glautan (Unipharm, Tel Aviv, Israel). After 1 and 4 weeks of treatment, a randomized, prospective, cross-over comparison was carried out that included patients with open-angle glaucoma or oc...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,随机对照试验


    authors: Golan S,Rosenfeld E,Shemesh G,Kurtz S

    更新日期:2015-02-01 00:00:00

  • Ascites fluid of nephrotic rats: sodium dodecyl sulphate-polyacrylamide gel electrophoresis protein pattern and the renin-angiotensin system.

    abstract::1. The concentration of renin and angiotensinogen (Ao) and the activity of angiotensin I-converting enzyme (ACE) was measured in the ascites fluid of nephrotic rats obtained 8 days after puromycin aminonucleoside (PAN) injection. 2. Ascites fluid, serum and urine proteins of these rats were analysed by sodium dodecyl ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Cruz C,Correa-Rotter R,Mézquita C,Medina-Campos ON,Pedraza-Chaverrí J

    更新日期:1998-07-01 00:00:00

  • Carotid body potentiation induced by intermittent hypoxia: implications for cardiorespiratory changes induced by sleep apnoea.

    abstract::1. The most usual form of chronic hypoxia in humans is the intermittent hypoxia resulting from obstructive sleep apnoea (OSA). The OSA syndrome is a highly prevalent sleep breathing disorder that is considered an independent risk factor for hypertension and cardiovascular diseases. Endothelial dysfunction, oxidative s...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Iturriaga R,Moya EA,Del Rio R

    更新日期:2009-12-01 00:00:00

  • Autacoid interactions in the regulation of blood flow in the human placenta.

    abstract::1. Interactions between autacoids may play important roles in the regulation of blood flow in the foetal placenta. In order to investigate this aspect of placental haemodynamics, human normal-term placentae were perfused in vitro and the responses of the foetal vessels to various combinations of vasoactive agents were...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Gude NM,King RG,Brennecke SP

    更新日期:1998-09-01 00:00:00

  • Salt and water intake and sodium and potassium excretion in spontaneously hypertensive rats.

    abstract::1. Total fluid and saline intakes were greater in spontaneously hypertensive rats (SHR) than in normotensive rats (NTR). 2. Total fluid and saline intake were significantly elevated in prehypertensive SHR, 5 weeks old, compared with age-matched NTR, and the intakes fell with age in both strains but remained considerab...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: May CN,Parsons BJ

    更新日期:1983-01-01 00:00:00

  • Effect of Anoectochilus formosanus on fibrosis and regeneration of the liver in rats.

    abstract::1. The present study examined the effects of an aqueous extract of Anoectochilus formosanus (AFE) on both hepatic fibrosis and regeneration in rats. 2. Fibrosis was induced by intraperitoneal injection of dimethylnitrosamine (DMN) for 3 consecutive days per week for 4 weeks. 3. In DMN-treated rats, liver cirrhosis-ass...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Shih CC,Wu YW,Hsieh CC,Lin WC

    更新日期:2004-09-01 00:00:00