Human tachykinin NK2 receptor: a comparative study of the colon and urinary bladder.

Abstract:

:1. The present study compared the binding and functional characteristics of tachykinin NK2 receptors in human detrusor muscle with those in human colon circular muscle. 2. In radioligand binding studies, similar KD values were observed for tachykinin NK2 receptor radioligands [125I]-neurokinin (NK) A, [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10,]NKA(4-10) and [3H]-SR48968 in both human colon circular muscle (0.28-1.1 nmol/L) and human bladder detrusor (0.49-0.91 nmol/L), suggesting binding was primarily to tachykinin NK2 receptors. Receptor capacity (Bmax) was greater in colon compared with detrusor muscle. 3. In functional studies of isolated smooth muscle contraction, there was an excellent positive correlation between human bladder detrusor and colon circular muscle with respect to in vitro contractile potency (r = 0.97) and maximum responses (r = 0.98) to tachykinins, selective tachykinin receptor ligands and l-Ala-substituted NKA(4-10) analogues. 4. Species differences between the human and rat tachykinin NK2 receptors were apparent as observed by a low correlation for potency (r = 0.77) and efficacy (r = 0.32) of l-Ala-substituted analogues in isolated smooth muscle contractile studies. 5. Minor differences observed in the affinity and potency of NK2 receptor agonists between colon and bladder are dependent on the tissue of interest, the receptor-effector coupling and the presence of other tachykinin receptors. Overall, the NK2 receptors of human colon and urinary bladder smooth muscle appear pharmacologically identical.

authors

Warner FJ,Miller RC,Burcher E

doi

10.1046/j.1440-1681.2003.03887.x

keywords:

subject

Has Abstract

pub_date

2003-09-01 00:00:00

pages

632-9

issue

9

eissn

0305-1870

issn

1440-1681

pii

3887

journal_volume

30

pub_type

杂志文章
  • Visfatin is associated with lipid metabolic abnormalities in Lyon hypertensive rats.

    abstract::1. Visfatin (also known as nicotinamide phosphoribosyltransferase or Nampt) is a novel adipokine associated with metabolic abnormalities in obesity and diabetes. The aim of the present study was to determine whether visfatin levels in the circulation and visfatin expression in fat tissues are altered in Lyon hypertens...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2010.05402.x

    authors: Wang P,Bai C,Xu QY,Xu TY,Su DF,Sassard J,Miao CY

    更新日期:2010-09-01 00:00:00

  • Cimetidine and ranitidine: a study of competitive and ion-channel blockade in the toad isolated rectus abdominis muscle.

    abstract::Responses of the toad isolated rectus abdominis muscle to cumulative doses of carbachol were recorded in the absence or presence of varying concentrations of cimetidine or ranitidine. The corresponding cumulative log concentration-response curves for carbachol were then plotted for each antagonist studied. Cimetidine ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1986.tb00946.x

    authors: Gwee MC,Cheah LS,Shoon ML

    更新日期:1986-08-01 00:00:00

  • Effects of dietary fibre on dimethylhydrazine-induced changes in prostanoid concentrations in rat colonic mucosa.

    abstract::1. This study was designed to elucidate the effects of guar gum, a dietary fibre, on changes in prostanoid contents induced by 1,2-dimethylhydrazine, a carcinogenic agent, in rat colonic mucosa. 2. Prostanoid contents were determined using high performance liquid chromatography; five prostanoids, namely 6-keto-prostag...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1995.tb01928.x

    authors: Kanamori S,Sugiyama S,Goto H,Hayakawa T,Shimomura Y,Ozawa T

    更新日期:1995-10-01 00:00:00

  • Effects of taurine and homocysteine on calcium homeostasis and hydrogen peroxide and superoxide anions in rat myocardial mitochondria.

    abstract::1. Taurine and homocysteine are metabolites of methionine. Hyperhomocysteinaemia is one of the risk factors for cardiovascular disease. Although taurine may be a cardiovascular cytoprotective substance, we hypothesized that it may antagonize the effects of homocysteine on myocardial mitochondrial function. 2. We studi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2004.03983.x

    authors: Chang L,Zhao J,Xu J,Jiang W,Tang CS,Qi YF

    更新日期:2004-04-01 00:00:00

  • Inhibition of cytokine release by and cardiac effects of type IV phosphodiesterase inhibition in early, profound endotoxaemia in vivo.

    abstract::1. In rats, inhibition of type IV phosphodiesterase (PDE4) attenuates acute renal failure and early (hours) mortality induced by high-dose endotoxin. Because it is unlikely that protection of renal function accounts for improved early survivability, most likely PDE4 inhibition exerts multiple beneficial effects in end...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1046/j.1440-1681.2000.03332.x

    authors: Tofovic SP,Zacharia LC,Carcillo JA,Jackson EK

    更新日期:2000-10-01 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

  • Effects of atropine on the time and frequency domain estimates of blood pressure and heart rate variability in mice.

    abstract::1. Indices quantifying blood pressure (BP) and heart rate (HR) variability have been recently developed and may be used to assess the contribution of the autonomic nervous system to cardiovascular fluctuations. 2. Cardiovascular variables were measured in eight conscious mice equipped with a BP telemetric device. Each...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2008.04895.x

    authors: Laude D,Baudrie V,Elghozi JL

    更新日期:2008-04-01 00:00:00

  • Prostaglandins: antinociceptive effect of prostaglandin E1 in the rat.

    abstract::1. The antinociceptive effect of prostaglandins E1, E2 and F2alpha was studied in albino rats. Though all three prostaglandins produced similar degrees of sedation, only prostaglandin E1 (PGE1) produced a dose-related antinociceptive activity. 2. The antinociceptive activities of equi-analgesic doses of morphine (7.5....

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1977.tb02621.x

    authors: Sanyal AK,Bhattacharya SK,Keshary PR,Srivastava DN,Debnath PK

    更新日期:1977-05-01 00:00:00

  • Blunted renal vasoconstriction in patients with subclinical contrast-induced renal injury.

    abstract::Contrast media are considered to cause acute kidney injury by activating various factors that induce renal vasoconstriction. We analysed the renal microvascular haemodynamic response using the Doppler flow wire method. Then changes in urinary liver-type fatty acid-binding protein levels following contrast medium admin...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 信件

    doi:10.1111/1440-1681.12653

    authors: Kurihara O,Seino Y,Shibata Y,Matsushita M,Komiyama H,Kato K,Murakami D,Munakata R,Takano M,Miyauchi Y,Hata N,Shimizu W

    更新日期:2016-11-01 00:00:00

  • Hypertension mechanisms causing stroke.

    abstract::1. Although it is well established that hypertension is the main risk factor for stroke, the complexity of cerebrovascular problems related to hypertension is not generally appreciated. 2. Hypertension can cause stroke through many mechanisms. A high intraluminal pressure will lead to extensive alteration in endotheli...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1440-1681.1999.03081.x

    authors: Johansson BB

    更新日期:1999-07-01 00:00:00

  • Protective effects of magnesium against ischaemia-reperfusion injury through inhibition of P-selectin in rats.

    abstract::1. The leucocyte-mediated inflammatory response plays a pivotal role in ischaemia-reperfusion injury. P-Selectin and CD11b are important mediators for the recruitment of leucocytes into the endothelium. However, the time-course of changes in P-selectin and CD11b expression during reperfusion is not defined. Magnesium ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2007.04697.x

    authors: Ying SQ,Fang L,Xiang MX,Xu G,Shan J,Wang JA

    更新日期:2007-12-01 00:00:00

  • Metformin improves cardiac function in rats via activation of AMP-activated protein kinase.

    abstract::1. Metformin is one of the most commonly used drugs for the treatment of Type 2 diabetes. Accumulating evidence suggests that metformin also has cardioprotective effects. In the present study, we investigated the cardioprotective effects of metformin and the mechanisms involved. 2. A rat model of chronic heart failure...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2010.05470.x

    authors: Wang XF,Zhang JY,Li L,Zhao XY,Tao HL,Zhang L

    更新日期:2011-02-01 00:00:00

  • Activation of imidazoline-I3 receptors ameliorates pancreatic damage.

    abstract::Agmatine, an endogenous ligand of imidazoline receptors, is reported to exhibit anti-hyperglycaemic and many other effects. It has been established that the imidazoline I3 receptor is involved in insulin secretion. The current study characterizes the role of the imidazoline I3 receptor in the protection of pancreatic ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/1440-1681.12441

    authors: Li Y,Cheng KC,Asakawa A,Amitani H,Takimoto Y,Runtuwene J,Inui A

    更新日期:2015-09-01 00:00:00

  • Decreased oxidative stress in prehepatic portal hypertensive rat livers following the induction of diabetes.

    abstract::1. Oxidative stress (OS) is a biological entity indicated as being responsible for several pathologies, including diabetes. Diabetes can also be associated with human cirrhosis. Portal hypertension (PH), a major syndrome in cirrhosis, produces hyperdynamic splanchnic circulation and hyperaemia. The present study was d...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2004.03963.x

    authors: Evelson P,Llesuy S,Filinger E,Rodriguez RR,Lemberg A,Scorticati C,Susemihl M,Villareal I,Polo JM,Peredo H,Perazzo JC

    更新日期:2004-03-01 00:00:00

  • Dopamine D1 receptors induce apoptosis of osteosarcoma cells via changes of MAPK pathway.

    abstract::This study explored the effects and mechanisms of dopamine D1 receptors (DR1) activation on the apoptosis of osteosarcoma cells (OS732).The DR1 agonist SKF-38393 decreased the viability of OS732 cells and increased their rate of apoptosis, whereas the DR1 antagonist SCH-23390 abolished the effects of SKF-38393. In OS7...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 信件

    doi:10.1111/1440-1681.12814

    authors: Gao J,Gao F

    更新日期:2017-11-01 00:00:00

  • Influence of low and normal appendicular lean mass on central blood pressure and wave reflection responses to muscle metaboreflex activation in postmenopausal women.

    abstract::Sarcopenia, defined by reduced appendicular skeletal muscle mass (ASM)/height2 (ASMI), is associated with increased arterial stiffness (brachial-ankle pulse wave velocity, baPWV) and wave reflection (augmentation index, AIx). Blood pressure (BP) responses to metaboreflex activation (post-exercise muscle ischemia, PEMI...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 信件

    doi:10.1111/1440-1681.12655

    authors: Figueroa A,Alvarez-Alvarado S,Jaime SJ,Johnson SA,Campbell JC,Feresin RG,Elam ML,Navaei N,Pourafshar S,Arjmandi BH

    更新日期:2016-12-01 00:00:00

  • Effect of labetalol on human platelet function.

    abstract::1. The effects of the alpha-beta-adrenergic antagonist labetalol on the activation of human platelets by adrenaline and other aggregating stimuli have been investigated. 2. Labetalol inhibited platelet aggregation and secretion induced by collagen and the second phase of aggregation caused by ADP, platelet activating ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1988.tb01099.x

    authors: Anfossi G,Trovati M,Lanzio M,Mularoni E,Massucco P,Emanuelli G

    更新日期:1988-06-01 00:00:00

  • L-type calcium channels and CRH-mediated ACTH and cortisol release in humans.

    abstract::1. The effect of pretreatment with nifedipine on naloxone-stimulated corticotrophin-releasing hormone (CRH)-induced adrenocorticotrophin (ACTH) release in humans was investigated. The mean peak plasma ACTH and cortisol levels and the mean peak change in cortisol levels from basal were significantly lower in the nifedi...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1991.tb01451.x

    authors: Hockings GI,Grice JE,Walters MM,Jackson RV

    更新日期:1991-05-01 00:00:00

  • The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors.

    abstract::The pharmacological actions of 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP), a putative presynaptic GABA(B) receptor modulator, were examined in electrically stimulated rat neocortical brain slices preloaded with [3H]-GABA or [3H]-glutamic acid. At 10 mmol/L, BSPP inhibited the release of [3H]-GAB...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2008.04948.x

    authors: Parker DA,Marino V,Ong J,Puspawati NM,Prager RH

    更新日期:2008-09-01 00:00:00

  • Hypoxia-activated prodrugs as antitumour agents: strategies for maximizing tumour cell killing.

    abstract::1. Hypoxia arises in solid tumour because of inefficient blood supply. While hypoxic cells are resistant to radiotherapy and probably to many chemotherapeutic drugs they can, in principle, be turned to advantage through the development of hypoxia-activated cytotoxic drugs (bioreductive drugs). 2. Three general approac...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1995.tb01956.x

    authors: Wilson WR,Pruijn FB

    更新日期:1995-11-01 00:00:00

  • Characterization of two polyclonal peptide antibodies that recognize the carboxy terminus of angiotensin II AT1A and AT1B receptors.

    abstract::1. The differential identification of the angiotensin AT1A and AT1B receptor subtypes is impaired by the existing>96% homology of both receptors. In the present study, we characterized two polyclonal rabbit peptide antibodies, namely alpha-AT1A and alpha-AT1B, that recognize the C-terminal region of mouse AT1A and AT1...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2005.04288.x

    authors: Hoffmann A,Cool DR

    更新日期:2005-11-01 00:00:00

  • Renal tubulointerstitial hypoxia: cause and consequence of kidney dysfunction.

    abstract::1. Intrarenal oxygen availability is the balance between supply, mainly dependent on renal blood flow, and demand, determined by the basal metabolic demand and the energy-requiring tubular electrolyte transport. Renal blood flow is maintained within close limits in order to sustain stable glomerular filtration, so inc...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1440-1681.2011.05532.x

    authors: Palm F,Nordquist L

    更新日期:2011-07-01 00:00:00

  • RNA interference-mediated silencing of UBCH10 gene inhibits colorectal cancer cell growth in vitro and in vivo.

    abstract::1. UbcH10 is the cancer-related E2 ubiquitin-conjugating enzyme, and its overexpression has been demonstrated in a variety of malignancies. The aim of the present study is to silence UbcH10 gene by RNA interference (RNAi) and to observe its inhibitory effect on the colorectal cancer cell growth in vitro and in vivo. 2...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2009.05348.x

    authors: Chen SM,Jiang CY,Wu JY,Liu B,Chen YJ,Hu CJ,Liu XX

    更新日期:2010-05-01 00:00:00

  • Ageing has no effect on the volume density of hepatocytes, reticulo-endothelial cells or the extracellular space in livers of female Sprague-Dawley rats.

    abstract::1. The hepatic reticulo-endothelial cell population is generally assumed to increase in size, along with the liver, during ageing in rats. However, this has not been rigorously established. 2. Using electron microscopy and stereological techniques, the present study has shown that the volume densities of hepatocytes a...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1992.tb00501.x

    authors: Martin G,Sewell RB,Yeomans ND,Smallwood RA

    更新日期:1992-07-01 00:00:00

  • Characterization and localization of (-)[125I]-cyanopindolol binding to non-beta-adrenoceptor sites in dog kidney.

    abstract::1. (-)[125I]-Cyanopindolol (CYP) binding to non-beta-adrenoceptor sites in dog kidney was characterized in homogenate preparations and their distribution in sections determined using autoradiography. 2. In homogenate studies, (-)[125I]-CYP bound to a single population of non-interacting sites (Bmax = 5.45, s.e.m. = 1....

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.1987.tb01896.x

    authors: Lew R,Summers RJ

    更新日期:1987-09-01 00:00:00

  • Similar renoprotection after renin-angiotensin-dependent and -independent antihypertensive therapy in 5/6-nephrectomized Ren-2 transgenic rats: are there blood pressure-independent effects?

    abstract::1. Hypertension plays a critical role in the progression of chronic kidney disease (CKD) to end-stage renal disease (ESRD), but it has also been postulated that antihypertensive drugs that block the renin-angiotensin system (RAS) show class-specific renoprotective actions beyond their blood pressure (BP)-lowering effe...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/j.1440-1681.2010.05453.x

    authors: Kujal P,Chábová VČ,Vernerová Z,Walkowska A,Kompanowska-Jezierska E,Sadowski J,Vaňourková Z,Husková Z,Opočenský M,Skaroupková P,Schejbalová S,Kramer HJ,Rakušan D,Malý J,Netuka I,Vaněčková I,Kopkan L,Cervenka L

    更新日期:2010-12-01 00:00:00

  • L-arginine and aminoguanidine reduce colonic damage of acetic acid-induced colitis in rats: potential modulation of nuclear factor-κB/p65.

    abstract::The transcription factor, nuclear factor-κB (NF-κB) is a key inducer of inducible nitric oxide synthase (iNOS) gene expression. The aim of the present study was to investigate the potential protective effect of l-arginine (Arg; nitric oxide precursor) and aminoguanidine (inducible nitric oxide synthase inhibitor) agai...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/1440-1681.12287

    authors: Farghaly HS,Thabit RH

    更新日期:2014-10-01 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

    doi:10.1111/1440-1681.13093

    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

  • Cathelicidin deficiency exacerbates cardiac dysfunction in lipopolysaccharide-induced endotoxaemic mice.

    abstract::The therapeutic potential of the antimicrobial peptide cathelicidin (Camp) administration in sepsis has been widely investigated. However, little is known about the pathophysiological roles of cathelicidin in septic cardiomyopathy. In a lipopolysaccharide (LPS)-induced endotoxaemic model, we found that the mRNA and pr...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章

    doi:10.1111/1440-1681.13234

    authors: Zhai T,Zhang J,Zhang Y,Wu Y

    更新日期:2020-04-01 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

    doi:10.1111/j.1440-1681.1981.tb00763.x

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

    更新日期:1981-09-01 00:00:00