Relative inhibitory potency and plasma drug levels of angiotensin converting enzyme inhibitors in the rat.


:1. 125I-351A, a tyrosyl derivative of the angiotensin converting enzyme (ACE) inhibitor lisinopril, was used as a radioligand, and radioinhibitor binding and displacement assays have been established. 2. The in vitro potency of a range of ACE inhibitors against rat ACE was determined using the radioinhibitor binding displacement assay. 3. The concentration of an ACE inhibitor needed to displace 50% of 125I-351A bound to rat ACE (ID50) was closely correlated with the concentration needed to inhibit 50% of ACE enzymatic activity (IC50). 4. Radioinhibitor binding displacement assay was used to measure the plasma concentrations of lisinopril, cilazapril and perindopril in rat plasma. 5. Plasma concentrations of lisinopril measured by radioimmunoassay were identical with that measured by radioinhibitor binding assays.


Johnston CI,Cubela R,Jackson B




Has Abstract


1988-02-01 00:00:00












  • The effects of indomethacin in treated hypertensive patients.

    abstract::1. Twelve treated hypertensive patients (ages 58-71 years) who had also been treated for joint disease participated in a randomized double-blind crossover placebo-controlled study to investigate the effects of indomethacin (25 mg three times daily) on blood pressure and biochemical parameters over a 6-week period. 2. ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Wing LM,Bune AJ,Chalmers JP,Graham JR,West MJ

    更新日期:1981-09-01 00:00:00

  • Reduced [125I]-Bolton Hunter substance P binding (NK1 receptors) in the basal forebrain nuclei of aged rats.

    abstract::1. Quantitative autoradiography and homogenate radioligand binding of [125I]-Bolton Hunter substance P ([125I]-BHSP) were used to compare brain NK1 receptors in young (2 months) and aged (18-20 months) rats. 2. The autoradiographic distribution and density of [125I]-BHSP binding sites was similar in all cortical regio...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Geraghty DP,Maguire CM

    更新日期:2002-12-01 00:00:00

  • Role of non-selective adenosine receptor blockade and phosphodiesterase inhibition in cisplatin-induced nephrogonadal toxicity in rats.

    abstract::1. It is well documented that cisplatin (CDDP) treatment increases the expression of adenosine A(1) receptors in both kidney and testes. However, the effect of adenosine at these receptors is controversial. Adenosine A(1) receptors have been documented to be involved in either cytoprotection or aggravation of nephroto...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Saad SY,Najjar TA,Alashari M

    更新日期:2004-12-01 00:00:00

  • Antifibrotic effect of AT-1 blocker and statin in rats with hepatic fibrosis.

    abstract::Hepatic fibrosis is an outcome of chronic liver injury. Angiotensin II (ANG II) may play a role in the pathogenesis of hepatic fibrosis. Certain drugs such as ACE inhibitors, ANG II antagonists, and even statins could interfere with the renin angiotensin system and modulate its deleterious effects. This study was carr...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: El-Ashmawy NE,El-Bahrawy HA,Shamloula MM,Ibrahim AO

    更新日期:2015-09-01 00:00:00

  • Barriers to successful delivery of short interfering RNA after systemic administration.

    abstract::1. RNA interference in vivo has tremendous potential, both with respect to the elucidation of protein function in animals and as a therapeutic platform in humans. In vitro, short interfering RNA (siRNA) has been shown to completely silence gene expression in mammalian cells at low picomolar concentrations. 2. Although...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: White PJ

    更新日期:2008-11-01 00:00:00

  • Augmented exercise plasma noradrenaline with impaired chronotropic responsiveness in patients with hypertrophic cardiomyopathy.

    abstract::1. There is controversy regarding plasma catecholamine levels in patients with hypertrophic cardiomyopathy (HCM) and few data exist on serial plasma catecholamine measurements during exercise. The present study determined whether cardiovascular and plasma catecholamine responses to exercise were altered in patients wi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Omodani H,Kinugawa T,Ogino K,Furuse Y,Yamaguchi M,Mori M,Endo A,Kato M,Kato T,Osaki S,Miyakoda H,Igawa O,Hisatome I,Shigemasa C

    更新日期:1998-12-01 00:00:00

  • Long non-coding RNA myocardial infarction associated transcript promotes the proliferation of cholangiocarcinoma cells by targeting miR-551b-3p/CCND1 axis.

    abstract::Accumulating reports have demonstrated that long non-coding RNAs (lncRNAs) play critical roles in the occurrence and metastasis of cholangiocarcinoma (CCA). LncRNA myocardial infarction associated transcript (MIAT) has been widely reported in hepatocellular carcinoma, pancreatic cancer and colorectal cancer, but the r...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Chang W,Wang Y,Li W,Geng Z

    更新日期:2020-06-01 00:00:00

  • Renomedullary interstitial cells: a target for endocrine and paracrine actions of vasoactive peptides in the renal medulla.

    abstract::1. The renal medulla plays an important role in regulating body sodium and fluid balance and blood pressure homeostasis through its unique structural relationships and interactions between renomedullary interstitial cells (RMIC), renal tubules and medullary vasculature. 2. Several endocrine and/or paracrine factors, i...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Zhuo JL

    更新日期:2000-07-01 00:00:00

  • MicroRNA-217 suppresses homocysteine-induced proliferation and migration of vascular smooth muscle cells via N-methyl-D-aspartic acid receptor inhibition.

    abstract::Hyperhomocysteine has become a critical risk for atherosclerosis and can stimulate proliferation and migration of vascular smooth muscle cells (VSMCs). N-methyl-D-aspartic acid receptor (NMDAR) is a receptor of homocysteine and mediates the effects of homocysteine on VSMCs. Bioinformatics analysis has shown NMDAR is a...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Duan H,Li Y,Yan L,Yang H,Wu J,Qian P,Li B,Wang S

    更新日期:2016-10-01 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


    authors: Verberne AJ,Rand MJ

    更新日期:1984-07-01 00:00:00

  • 7,8-dihydroxyflavone enhanced cholinergic contraction of rat gastric smooth muscle via augmenting muscarinic M3 receptor expression.

    abstract::Although 7,8-dihydroxyflavone (7,8-DHF), a synthetic agonist specific for tyrosine kinase receptor B (TrkB), has been reported to promote intestinal dynamics, its effect on gastric dynamics has not been studied as yet. In this study, we explored how 7,8-DHF affected the carbachol (CCh)-induced contraction of rat gastr...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: He B,Qu Z,Tian Z,Zhao K,Wei L,Ma L

    更新日期:2018-11-01 00:00:00

  • Engineering imaging: using particle image velocimetry to see physiology in a new light.

    abstract::1. Despite the array of sophisticated imaging techniques available for biological applications, none of the standard biomedical techniques adequately provides the capability to measure motion and flow. Those techniques currently in use are particularly lacking in spatial and temporal resolution. 2. Herein, we introduc...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Fouras A,Dusting J,Sheridan J,Kawahashi M,Hirahara H,Hourigan K

    更新日期:2009-02-01 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


    authors: Grant SL,Phillips PA,Gow CB

    更新日期:1994-03-01 00:00:00

  • Urinary NO3- excretion as an indicator of nitric oxide formation in vivo during oral administration of L-arginine or L-name in rats.

    abstract::1. Endothelium-derived nitric oxide (NO), a major modulator of vascular tone, is synthesized from the terminal guanidino nitrogen of L-arginine. This reaction is inhibited by analogues of L-arginine, such as N-nitro-L-arginine methyl ester (L-NAME). Many of the biological effects of NO are mediated by the second messe...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Boger RH,Bode-Boger SM,Gerecke U,Gutzki FM,Tsikas D,Frolich JC

    更新日期:1996-01-01 00:00:00

  • Effect of alcohol on cytochrome p450 arachidonic acid metabolism and blood pressure in rats and its modulation by red wine polyphenolics.

    abstract::Alcohol-induced hypertension is well recognized with clear evidence for a direct pressor effect of chronic alcohol consumption provided by a number of intervention studies in humans. In experimental animals, the effect of alcohol on blood pressure is less consistent; however, in Sprague-Dawley rats, alcohol feeding co...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Cowpland C,Su GM,Murray M,Puddey IB,Croft KD

    更新日期:2006-03-01 00:00:00

  • Renal kallikrein in chronic hypoxic rats.

    abstract::1. We have studied the role of kallikrein (KK) in the maintenance of renal function in chronic hypoxic rats (high altitude; HA), compared with control rats kept at sea level (SL). Hypoxia was induced by placing female Wistar rats (198-290 g) in an altitude chamber (5500 m) 15 h/day for 4 weeks. Experiments were also c...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Chen CF,Chen LW,Chien CT,Wu MS,Tsai TJ

    更新日期:1996-09-01 00:00:00

  • A study of the relationship between cardiac beta-adrenoceptor blockade and intrinsic sympathomimetic activity in rats depleted of catecholamines.

    abstract::1. The intrinsic sympathomimetic activity of a range of beta-adrenoceptor antagonists and its relationship to beta-adrenoceptor blockade was studied in pentobarbitone-anaesthetized, vagotomized rats which had been depleted of catecholamines by pretreatment with syrosingopine. Dichlorisoprenaline, practolol, oxprenolol...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Bilski A,Robertson HH,Wale JL

    更新日期:1979-01-01 00:00:00

  • Isolation of opiate receptor ligands in coffee.

    abstract::1. We have reported previously that instant coffee contains ligands for opiate receptors with characteristics similar to those of opiate antagonists. 2. A concentrate of receptor-active ligands from instant coffee was prepared by serial treatments involving Amberlite XAD-2, flash chromatography and gel permeation chro...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Wynne KN,Familari M,Boublik JH,Drummer OH,Rae ID,Funder JW

    更新日期:1987-10-01 00:00:00

  • Histone modifications and skeletal muscle metabolic gene expression.

    abstract::1. Skeletal muscle oxidative function and metabolic gene expression are co-ordinately downregulated in metabolic diseases such as insulin resistance, obesity and Type 2 diabetes. Altering skeletal muscle metabolic gene expression to favour enhanced energy expenditure is considered a potential therapy to combat these d...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: McGee SL,Hargreaves M

    更新日期:2010-03-01 00:00:00

  • Beneficial effect of T-1095, a selective inhibitor of renal Na+-glucose cotransporters, on metabolic index and insulin secretion in spontaneously diabetic GK rats.

    abstract::1. To investigate the pharmacological effects of T-1095, this novel derivative of phlorizin was administered to GK rats for 8 weeks. T-1095 treatment significantly lowered plasma glucose and glycosylated haemoglobin (HbA1c) levels, but did not significantly affect bodyweight. 2. T-1095 treatment did not affect 3.3 mmo...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Nunoi K,Yasuda K,Adachi T,Okamoto Y,Shihara N,Uno M,Tamon A,Suzuki N,Oku A,Tsuda K

    更新日期:2002-05-01 00:00:00

  • Nephropreventing effect of hypoxia-inducible factor 1α in a rat model of ischaemic/reperfusion acute kidney injury.

    abstract::Acute kidney injury (AKI) occurs in 5% of hospitalized patients and in 50% of sepsis patients with acute renal dysfunction. However, there have been no safe and effective therapeutic strategies. The hypoxia condition is closely related to renal injury and function under AKI. As hypoxia-inducible factor 1α (HIF-1α) is ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Wang H,Liu N,Li R,Tian J,Hu W,Zhang J

    更新日期:2018-10-01 00:00:00

  • Low KISS1 expression predicts poor prognosis for patients with colorectal cancer: A meta-analysis.

    abstract::KISS1 and KISS1R, a novel pair of metastasis suppressors, are likely to be associated with the prognosis of colorectal cancer (CRC). Here, a meta-analysis was performed to study the role of KISS1 and KISS1R in CRC. Heterogeneity, stability and publication bias were all estimated. Six publications describing a total of...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,meta分析


    authors: Wang XQ,Fang PF,Zhang C,Xu YY,Song XB,Liang J,Xia QR

    更新日期:2019-07-01 00:00:00

  • Irinotecan (CPT-11): a brief overview.

    abstract::1. Irinotecan (also known as CPT-11) is a water soluble, semi-synthetic analogue of 20(S)camptothecin (CPT) with promising activity against a range of tumour types. 2. As with all other active analogues of CPT, irinotecan causes cell toxicity by stabilizing a ternary complex between the nuclear enzyme topoisomerase I ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Rivory LP

    更新日期:1996-10-01 00:00:00

  • The difference in nifedipine sensitivity between hypertensive and normotensive rat aortae is dependent on age.

    abstract::1. In order to investigate further whether the increased sensitivity to inhibition by nifedipine of the responses to noradrenaline of aortae from spontaneously hypertensive stroke-prone (SHRSP) rats is related to the development of the hypertension, we have compared the sensitivity to noradrenaline, potassium chloride...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Jiang GC,Iwanov V,Moulds RF

    更新日期:1995-01-01 00:00:00

  • Effect of pregnancy in the rabbit on the pressor response to angiotensin and noradrenaline.

    abstract::The pressor responses to angiotensin II injections of 29, 117 and 468 pmol/kg and infusion at 54 pmol/kg per min were compared in near-term pregnant and matched non-pregnant rabbits. The responses to noradrenaline injections of 652, 2608 and 10 432 pmol/kg and infusion at 1185 pmol/kg per min were similarly compared. ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Joels N,Humphreys PW

    更新日期:1985-11-01 00:00:00

  • Renin and the (pro)renin receptor in the renal collecting duct: Role in the pathogenesis of hypertension.

    abstract::The intrarenal renin-angiotensin system (RAS) plays a critical role in the pathogenesis and progression of hypertension and kidney disease. In angiotensin (Ang) II-dependent hypertension, collecting duct renin synthesis and secretion are stimulated despite suppression of juxtaglomerular (JG) renin. This effect is medi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Gonzalez AA,Prieto MC

    更新日期:2015-01-01 00:00:00

  • Elevation of blood pressure in hypertensive rats after lesioning serotonin nerves in the dorsomedial medulla oblongata.

    abstract::The possibility that serotonin (5HT) nerve endings in the dorsomedial medulla oblongata participate in the control of blood pressure was investigated in stroke-prone hypertensive rats and in normotensive rats. 5HT nerves were destroyed by injecting 5,7-dihydroxytryptamine bilaterally into the solitary tract nucleus. I...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Howe PR,Rogers PF,King RA,Smith RM

    更新日期:1983-05-01 00:00:00

  • N-methyl d-aspartate receptors are involved in the induction, but not expression stage of amphetamine sensitization in schedule-induced polydipsia in rats.

    abstract::1. The aim of the present study was to examine the role of dopaminergic and glutamatergic receptors on different stages of the amphetamine (AMPH) sensitized effect in schedule-induced polydipsia (SIP) in rats. 2. Three experiments were designed to evaluate the roles of DAD2 receptor antagonist haloperidol (HAL) and gl...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Liu YP,Tung CS,Lin PJ,Wan FJ

    更新日期:2010-09-01 00:00:00

  • Acute systemic complications in the preterm fetus after asphyxia: role of cardiovascular and blood flow responses.

    abstract::1. Poor perfusion of the kidneys and gut, and associated functional impairment, are major problems in the first days of life in very preterm infants. These complications can be associated with a substantial mortality and further problems such as reduced kidney growth and chronic renal problems in later childhood. 2. T...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Bennet L,Booth L,Malpas SC,Quaedackers JS,Jensen E,Dean J,Gunn AJ

    更新日期:2006-04-01 00:00:00

  • Endothelin and post-ganglionic sympathetic neurons.

    abstract::1. The present report documents evidence suggesting that endothelin (ET) is a mediator and modulator of post-ganglionic sympathetic neuronal development. 2. Endothelin is produced by post-ganglionic neurons and by cells adjacent to these neurons. 3. Post-ganglionic sympathetic neurons express functional receptors for ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Damon DH

    更新日期:1999-12-01 00:00:00