In vitro autoradiographic endothelin-1 binding sites and sarafotoxin S6B binding sites in rat tissues.

Abstract:

:1. The distribution of binding sites for [125I]-labelled endothelin-1 ([125I]-ET-1) and [125I]-labelled sarafotoxin S6B ([125I]-SRT) was visualized in rat tissues using in vitro autoradiography. 2. A high density of endothelin-1 (ET-1) binding was found in the heart. In the kidney, ET-1 binding occurred in association with glomeruli, proximal tubules, the inner stripe and inner medulla. In the adrenal, a high density of ET-1 binding occurred in the medulla as well as the zona glomerulosa. 3. The binding affinity constant (KA) for ET-1 binding in these sites ranged from 1 to 10 x 10(9)/mol per litre. 4. Although sarafotoxin S6B (SRT) was 10-100-fold weaker than ET-1 in displacing [125I]-ET-1 from these sites, 1 mumol/L unlabelled SRT completely abolished [125I]-ET-1 binding in all sites. Other venom peptides did not affect [125I]-ET-1 binding. 5. The pattern of [125I]-SRT receptor binding in rat tissues by in vitro autoradiography was identical to that for ET-1 receptor binding, and both unlabelled SRT and unlabelled ET-1 fully competed with [125I]-SRT for binding. 6. These results provide evidence that SRT binds to the ET receptor in a range of rat tissues. The results suggest that there may be subclasses of ET receptors which can be distinguished by the relative potencies of ET-1 and SRT at various tissues.

authors

Kohzuki M,Johnston CI,Abe K,Chai SY,Casley DJ,Yasujima M,Yoshinaga K,Mendelsohn FA

doi

10.1111/j.1440-1681.1991.tb01485.x

keywords:

subject

Has Abstract

pub_date

1991-07-01 00:00:00

pages

509-15

issue

7

eissn

0305-1870

issn

1440-1681

journal_volume

18

pub_type

杂志文章
  • 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

    doi:10.1111/1440-1681.12584

    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

  • Characterization of single heart cell contractility by rapid imaging.

    abstract::1. A rapid imaging technique with temporal resolution of about 1 ms was employed to describe cell-length changes during the isotonic contraction cycle of adult rat ventricular myocytes at 22 degrees C. 2. Parameters of cell contraction and relaxation were defined and values obtained under control conditions and after ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1989.tb01542.x

    authors: Delbridge LM,Harris PJ,Morgan TO

    更新日期:1989-03-01 00:00:00

  • Nitric oxide as a metabolic regulator during exercise: effects of training in health and disease.

    abstract::1. Accumulating animal and human data suggest that nitric oxide (NO) is important for both coronary and peripheral haemodynamic control and metabolic regulation during performance of exercise. 2. While still controversial, NO of endothelial origin is thought to potentiate exercise-induced hyperaemia, both in the perip...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1440-1681.2000.03232.x

    authors: Kingwell BA

    更新日期:2000-04-01 00:00:00

  • MicroRNA-645 promotes metastasis of osteosarcoma via targeting tumor suppressor NM23 nucleoside diphosphate kinase 2.

    abstract::Osteosarcoma is the most common non-hematological primary bony malignancy in children and young adults with tumor metastasis being a common event at diagnosis. Understanding the pathogenesis of metastatic osteosarcoma may help identify potential therapeutic targets. In this study, we found that the level of microRNA-6...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/1440-1681.13006

    authors: Jiao GJ,Zhang SJ,Li Y,Wu WL,Liu HC

    更新日期:2018-12-01 00:00:00

  • From 'captive' agonism to insurmountable antagonism: demonstrating the power of analytical pharmacology.

    abstract::1. Mathematical modelling is useful in pharmacology, allowing the investigator to obtain insights into the biological processes under study that may not always be intuitively obvious. Examples are presented in this review using the pharmacology of the muscarinic acetylcholine receptor (mAChR) agonist xanomeline. 2. Xa...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1440-1681.2001.03376.x

    authors: Christopoulos A

    更新日期:2001-03-01 00:00:00

  • In Vitro electrophysiological activity of nerispirdine, a novel 4-aminopyridine derivative.

    abstract::Summary 1. The non-selective K(+) channel blocker 4-aminopyridine (4-AP) has shown clinical efficacy in the treatment of neurological disorders such as multiple sclerosis. The clinical usefulness of 4-AP is hampered by its ability to produce seizures. Nerispirdine, an analogue of 4-AP, is currently under clinical inve...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2009.05200.x

    authors: Smith C,Kongsamut S,Wang H,Ji J,Kang J,Rampe D

    更新日期:2009-11-01 00:00:00

  • Endothelin stimulates inositol phosphate accumulation in rat right and left atria: a comparison with noradrenaline.

    abstract::1. The effect of endothelin on phosphatidylinositol turnover in rat atria was investigated by measuring the generation of inositol phosphates following [3H]-inositol labelling. 2. In the presence of 10 mmol/L LiCl, endothelin caused dose-dependent increases in the accumulation of inositol mono, bis and trisphosphates ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1990.tb01320.x

    authors: Kuraja IJ,Woodcock EA

    更新日期:1990-04-01 00:00:00

  • Expression and functional activity of breast cancer resistance protein (BCRP, ABCG2) transporter in the human choriocarcinoma cell line BeWo.

    abstract::1. Breast cancer resistance protein (BCRP, ABCG2) is a drug efflux transporter that is believed to affect the drug disposition of several drugs and xenobiotics. In the present study, we evaluated the localization and functional expression of BCRP in the human choriocarcinoma cell line BeWo, an in vitro model of the hu...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2006.04324.x

    authors: Ceckova M,Libra A,Pavek P,Nachtigal P,Brabec M,Fuchs R,Staud F

    更新日期:2006-01-01 00:00:00

  • Nitric oxide inhibits renal cytochrome P450-dependent epoxygenases in the rat.

    abstract::1. Nitric oxide (NO), or peroxynitrite, is known to inhibit haemoproteins, including cytochrome P450 mono-oxygenases. The present study explores the functional correlates of the inhibition by NO of renal epoxygenase on the vascular responses to arachidonic acid (AA) in the perfused kidney. 2. Control kidneys produce m...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1046/j.1440-1681.2002.03762.x

    authors: Oyekan A

    更新日期:2002-11-01 00:00:00

  • Progesterone antagonizes development but not maintenance of ACTH-induced hypertension in sheep.

    abstract::1. This study investigated the effect of progesterone, which, under certain circumstances, can antagonize both the mineralocorticoid and glucocorticoid activities of steroid hormones, on the development and maintenance of adrenocorticotrophic hormone (ACTH)-induced hypertension in conscious sheep. 2. Progesterone (500...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1989.tb01618.x

    authors: Spence CD,Reid AF,Coghlan JP,Mills EH,Whitworth JA,Scoggins BA

    更新日期:1989-08-01 00:00:00

  • Inhibition of NO synthesis has an additive effect on hypertension induced by ACTH in conscious rats.

    abstract::1. The haemodynamic and metabolic effects of oral intake of approximately 30 mg/kg per day N-nitro-L-arginine (NOLA) were examined in sham and adrenocorticotrophin (ACTH, 0.5 mg/kg per day) treated conscious Sprague-Dawley rats (n = 33). 2. NOLA administration produced an increase in systolic blood pressure of 24 +/- ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1992.tb00403.x

    authors: Li M,Dusting GJ,Whitworth JA

    更新日期:1992-10-01 00:00:00

  • Pharmacological activities of the antihypertensive drug urapidil in the rat.

    abstract::Urapidil had blocking activity on alpha 1-adrenoceptors in the rat isolated caudal artery (pA2 congruent to 7) and in the anaesthetized rat. Urapidil had no clonidine like agonistic activity on alpha 2-adrenoceptors in preparations of the guinea-pig ileum (prejunctional) or dog saphenous vein (post-junctional). Urapid...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1984.tb00289.x

    authors: Verberne AJ,Rand MJ

    更新日期:1984-07-01 00:00:00

  • Anorexic response to rapamycin does not appear to involve a central mechanism.

    abstract::The authors have previously demonstrated that a low and intermittent peripheral dose of rapamycin (1 mg/kg three times/week) to rats inhibited mTORC1 signalling, but avoided the hyperlipidemia and diabetes-like syndrome associated with higher doses of rapamycin. The dosing regimen reduced food intake, body weight, adi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/1440-1681.12601

    authors: Toklu HZ,Bruce EB,Sakarya Y,Carter CS,Morgan D,Matheny MK,Kirichenko N,Scarpace PJ,Tümer N

    更新日期:2016-09-01 00:00:00

  • Tetanic fade during partial transmission failure produced by non-depolarizing neuromuscular blocking drugs in the cat.

    abstract::1. A comparison has been made of the effects of three acetylcholine antagonists--hexamethonium, tubocurarine and pancuronium--on maximal tetani of limb muscles of cats under chloralose anaesthesia. In most experiments, the indirectly stimulated soleus muscle was studied, but observations were also made on the tibialis...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1976.tb00636.x

    authors: Bowman WC,Webb SN

    更新日期:1976-11-01 00:00:00

  • Interaction between epidermal growth factor and arginine vasopressin in renal medullary membranes.

    abstract::1. Epidermal growth factor is a potent mitogen that causes natriuresis, diuresis and inhibition of arginine vasopressin-induced water reabsorption. 2. The aim of this study was to determine any interaction between epidermal growth factor and the V1 (vascular) and/or V2 (antidiuretic) arginine vasopressin receptor subt...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1994.tb02506.x

    authors: Grant SL,Phillips PA,Gow CB

    更新日期:1994-03-01 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

    doi:10.1111/j.1440-1681.1983.tb00172.x

    authors: May CN,Parsons BJ

    更新日期:1983-01-01 00:00:00

  • Possible participation of NMDA and glycine receptors but not GABAA receptors in enflurane-induced opisthotonus in mice.

    abstract::1. We previously reported that volatile anaesthetics produce incidences of a transient opisthotonus in mice, a sign of CNS stimulation. This study was performed to investigate mechanisms by which enflurane-induced opisthotonus (EIO) occurs. 2. The effects of pretreatment of N-methyl-D-aspartate (NMDA) antagonists dizo...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1994.tb02546.x

    authors: Komatsu H,Nogaya J,Ueki M,Yokono S,Ogli K

    更新日期:1994-06-01 00:00:00

  • Transient receptor potential (TRP) channels, vascular tone and autoregulation of cerebral blood flow.

    abstract::Members of the transient receptor potential (TRP) channel superfamily are present in vascular smooth muscle cells and play important roles in the regulation of vascular contractility. The TRPC3 and TRPC6 channels are activated by stimulation of several excitatory receptors in vascular smooth muscle cells. Activation o...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1440-1681.2007.04855.x

    authors: Brayden JE,Earley S,Nelson MT,Reading S

    更新日期:2008-09-01 00:00:00

  • Demonstration of alpha-adrenoceptor antagonism by the 5HT2 antagonist, ketanserin (R49945), in sheep.

    abstract::Serotonin causes a dose related (0.1-20 micrograms/kg i.v.) increase in mean arterial blood pressure (MAP) and heart rate in conscious sheep. Ketanserin (0.1 mg/kg per h i.v.) causes a decrease in blood pressure, and an increase in heart rate. In the presence of ketanserin, serotonin induced increases in MAP are atten...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1984.tb00872.x

    authors: Nelson MA,Coghlan JP,Denton DA,Mills EH,Spence CD,Whitworth JA,Scoggins BA

    更新日期:1984-11-01 00:00:00

  • P2X7 receptor in cardiovascular disease: The heart side.

    abstract::The P2X7 receptor is a ligand-gated purinergic receptor activated by extracellular ATP. The receptor is highly expressed in immune cells and in the brain, and, upon activation, the P2X7 receptor allows a cation flux, leading to the distinct activation of intracellular signalling pathways as the secretion of pro-inflam...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1111/1440-1681.13079

    authors: Guerra Martinez C

    更新日期:2019-06-01 00:00:00

  • Renal blood flow in obstructive jaundice: an experimental study in baboons.

    abstract::1. The distribution of intrarenal blood flow has been measured using the 133Xe-washout technique in thirteen baboons 2 weeks after ligation of the common bile duct. 2. In comparison with eight sham-operated baboons, there was a signifigant decrease in the percentage distribution of blood to the cortex, although the ra...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1976.tb00624.x

    authors: Bloom DS,Bomzon L,Rosendorff C,Kew MC

    更新日期:1976-09-01 00:00:00

  • Role of cAMP in the effects of K+ on the steroidogenesis of zona glomerulosa cells.

    abstract::1. Investigations of the role of cAMP in the stimulation of the steroidogenesis of zona glomerulosa (ZG) cells by increased extracellular K+ concentration are reviewed. 2. Possible reasons for discrepancies in the results of different investigators on whether K+ increases the cAMP content or output of ZG tissue or dis...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1440-1681.1999.03173.x

    authors: Tait JF,Tait SA

    更新日期:1999-12-01 00:00:00

  • High plasma concentrations of prorenin in a transgenic animal model of nephropathy with overexpression of transforming growth factor-beta1 in the kidneys.

    abstract::1. Plasma concentrations of prorenin were determined in a transgenic animal model of nephropathy induced by overexpression of transforming growth factor (TGF)-beta1 in the juxtaglomerular apparatus. 2. In both female and male mice, plasma concentrations of prorenin were higher in transgenic than in non-transgenic anim...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1046/j.1440-1681.2000.03330.x

    authors: Krag S,Nielsen AH,Wogensen L

    更新日期:2000-09-01 00:00:00

  • Exercise is good for your blood pressure: effects of endurance training and resistance training.

    abstract::1. Although several epidemiological studies have not observed significant independent relationships between physical activity or fitness and blood pressure, others have concluded that blood pressure is lower in individuals who are more fit or active. However, longitudinal intervention studies are more appropriate for ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,meta分析

    doi:10.1111/j.1440-1681.2006.04453.x

    authors: Fagard RH

    更新日期:2006-09-01 00:00:00

  • Erlotinib activates mitochondrial death pathways related to the production of reactive oxygen species in the human non-small cell lung cancer cell line A549.

    abstract::1. Erlotinib, a small-molecule epidermal growth factor receptor-tyrosine kinase (EGFR-TK) inhibitor, has been approved for the management of advanced non-small cell lung cancer. The aim of the present study was to investigate whether erlotinib exerts potent antitumour activities through the reactive oxygen species (RO...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2008.05091.x

    authors: Qian X,Li J,Ding J,Wang Z,Zhang W,Hu G

    更新日期:2009-05-01 00:00:00

  • The emerging role of calmodulin regulation of RyR2 in controlling heart rhythm, the progression of heart failure and the antiarrhythmic action of dantrolene.

    abstract::Cardiac output and rhythm depend on the release and the take-up of calcium from the sarcoplasmic reticulum (SR). Excessive diastolic calcium leak from the SR due to dysfunctional calcium release channels (RyR2) contributes to the formation of delayed after-depolarizations, which underlie the fatal arrhythmias that occ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1111/1440-1681.12669

    authors: Walweel K,Oo YW,Laver DR

    更新日期:2017-01-01 00:00:00

  • Cholinergic prejunctional inhibition of nitrergic neurotransmission in the guinea-pig isolated basilar artery.

    abstract::1. The effects of endogenous and exogenous acetylcholine (ACh) on nitrergic relaxations elicited by electrical field stimulation (EFS) were studied in guinea-pig endothelium-denuded basilar artery preparations precontracted with 1 mumol/L prostaglandin F2 alpha and a possible role of K+ channels in mediating the effec...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:

    authors: Jiang F,Li CG,Rand MJ

    更新日期:1999-04-01 00:00:00

  • Effects of celery extract and 3-N-butylphthalide on lipid levels in genetically hypercholesterolaemic (RICO) rats.

    abstract::1. Aqueous celery extract was administered intraperitoneally to genetically hypercholesterolaemic (RICO) and normocholesterolaemic (RAIF) rats via Alzet osmotic pumps over a 13 day period. 2. The serum cholesterol concentration of the celery extract-treated RICO rats was found to be significantly lower (P < 0.05) than...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1996.tb02598.x

    authors: Tsi D,Tan BK

    更新日期:1996-03-01 00:00:00

  • Integrative role of the lamina terminalis in the regulation of cardiovascular and body fluid homeostasis.

    abstract::1. Cardiovascular and body fluid homeostasis depends upon the activation and co-ordination of reflexes and behavioural responses. In order to accomplish this, the brain receives and processes both neural and chemical input. Once in the brain, information from sources signalling the status of the cardiovascular system ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1996.tb02594.x

    authors: Johnson AK,Cunningham JT,Thunhorst RL

    更新日期:1996-02-01 00:00:00

  • Effects of endothelium-derived relaxing factor on the smooth muscle of the rat tail artery.

    abstract::Simultaneous measurements of smooth muscle membrane potential and tension were made from isolated pieces of rat tail artery. A single electrical stimulus to the perivascular nerves produced a transient contraction of the smooth muscle. The amplitude of the contraction was increased after removal of the endothelium. Th...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1986.tb00343.x

    authors: Kotecha N,Neild TO

    更新日期:1986-03-01 00:00:00