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


: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-(6,7-dideoxy-beta-D-allo-hept-5-ynofuranosyl) adenine (HAK2701) as a selective displacer. 2. Using this assay method, it was found that rat brain membranes possess high- and low-affinity [3H]-NECA binding sites. The high-affinity binding site showed KD and Bmax values of 19.7+/-2.5 nmol/L and 0.192+/-0.05 pmol/mg protein, respectively, and the KD value for the low-affinity binding site was 4260+/-330 nmol/L. The KD value for the high-affinity site agreed well with that of the [3H]-NECA binding site determined with the partially purified P3LP preparation described previously. 3. The distribution of P3LP in rat tissues was determined using the [3H]-NECA binding method described above. The highest level of P3LP was in the cerebellum followed by the olfactory bulb and the spinal cord. 4. The order of the affinity for various purinergic or related compounds to P3LP in rat brain preparations was also determined by the [3H]-NECA binding method to be HAK2701 > NECA = adenosine 5'-O-(2-thiodiphosphate) > cAMP = beta,gamma-methyleneadenosine 5'-triphosphate > diadenosine tetraphosphate > alpha,beta-methyleneadenosine 5'-triphosphate > 5'-deoxy-5'-methylthioadenosine > N6-cyclopentyladenosine. 5. These studies reveal that the [3H]-NECA binding assay in combination with HAK2701 is successful in the characterization of P3LP, especially the membrane-bound form.


Yoshioka K,Matsuda A,Nakata H





Has Abstract


2001-04-01 00:00:00














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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Ribeiro S,Garrido P,Fernandes J,Vala H,Rocha-Pereira P,Costa E,Belo L,Reis F,Santos-Silva A

    更新日期:2016-03-01 00:00:00

  • Central choline suppresses plasma renin response to graded haemorrhage in rats.

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Isbil-Buyukcoskun N,Ilcol YO,Cansev M,Hamurtekin E,Ozluk K,Ulus IH

    更新日期:2008-09-01 00:00:00

  • Effects of locally administered argatroban on restenosis after balloon angioplasty: experimental and clinical study.

    abstract::1. This study was undertaken to evaluate the preventive effects of locally administered argatroban, a competitive inhibitor of thrombin-induced platelet activation, on restenosis after balloon angioplasty. 2. A hydrogel-coated balloon catheter was immersed three times in argatroban/saline solution (1 mg/mL) for 60 s, ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Imanishi T,Arita M,Tomobuchi Y,Hamada M,Hano T,Nishio I

    更新日期:1997-11-01 00:00:00

  • Quantitative tissue velocity imaging evaluation of ventricular function in obstructive sleep apnoea-hypopnoea syndrome in children.

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Mu H,Liu J,Gong K,Li D,Zhang J

    更新日期:2015-06-01 00:00:00

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    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

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    authors: Song HP,Zhang L,Dang YM,Yan H,Chu ZG,Huang YS

    更新日期:2010-05-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Collins SP,White MD,Denborough MA

    更新日期:1988-06-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Rechtman MP,King RG,Boura AL

    更新日期:1988-12-01 00:00:00

  • Renal prostaglandin efflux induced by vasopressin, dDAVP and arachidonic acid: contrasting profile and sites of release.

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    pub_type: 杂志文章


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    更新日期:1986-08-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


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    更新日期:1996-01-01 00:00:00

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    pub_type: 杂志文章


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    更新日期:2018-08-01 00:00:00

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    pub_type: 杂志文章


    authors: Raghavendran HB,Sathivel A,Yogeeta RS,Devaki T

    更新日期:2007-03-01 00:00:00

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    abstract::1. Plasma concentration and atrial content of atrial natriuretic factor (ANF) were measured in rats with chronic renal failure induced by subtotal nephrectomy. 2. Plasma ANF was higher, and atrial ANF content lower in rats with renal failure when compared with sham-operated controls. 3. Plasma renin activity (PRA) and...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Hodsman GP,Jackson B,Debrevi LM,Ogawa K,Johnston CI

    更新日期:1987-03-01 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

  • Deleterious effects of salt intake other than effects on blood pressure.

    abstract::1. Salt intake is not only known to play an important role in determining blood pressure (BP) but has been shown to have other deleterious effects independent of BP. 2. Epidemiological and animal studies have provided evidence that salt intake may have an adverse effect on stroke mortality independent of BP. 3. Signif...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Antonios TF,MacGregor GA

    更新日期:1995-03-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Wang S,Han HM,Jiang YN,Wang C,Song HX,Pan ZY,Fan K,Du J,Fan YH,Du ZM,Liu Y

    更新日期:2012-04-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Terpstra GK,Raaijmakers JA,Kreukniet J

    更新日期:1979-03-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 信件


    authors: Zaniqueli D,Alvim RO,Baldo MP,Luiz SG,Cunha RS,Mill JG

    更新日期:2018-05-01 00:00:00

  • Protecting murine hearts from ischaemia-reperfusion using selective inhibitors of adenosine metabolism.

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Willems L,Headrick JP

    更新日期:2005-03-01 00:00:00

  • Effects of glutamate transport substrates and glutamate receptor ligands on the activity of Na-/K(+)-ATPase in brain tissue in vitro.

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    authors: Nanitsos EK,Acosta GB,Saihara Y,Stanton D,Liao LP,Shin JW,Rae C,Balcar VJ

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  • Anti-oxidant effects of atorvastatin in dexamethasone-induced hypertension in the rat.

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    journal_title:Clinical and experimental pharmacology & physiology

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    authors: Mondo CK,Yang WS,Zhang N,Huang TG

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  • Increase in serum total angiotensin-converting enzyme activity with enalapril therapy in humans: a controlled trial.

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    pub_type: 临床试验,杂志文章,随机对照试验


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    更新日期:1992-05-01 00:00:00

  • Opioid receptors mediate inotropic and depressor effects of apelin in rats with 2K1C-induced chronic renovascular hypertension.

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Rostamzadeh F,Najafipour H,Yeganeh-Hajahmadi M,Joukar S

    更新日期:2018-02-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Hishinuma S,Matsumoto Y,Sato R,Saito M

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

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    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

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    abstract::1. There is mounting evidence that a wide range of antidepressants share the common feature of increasing hippocampal neurogenesis. The specificity of this association has suggested that an ability to increase neurogenesis might be a useful paradigm to screen for compounds with antidepressant activity. 2. The hope of ...

    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Nandam LS,Jhaveri D,Bartlett P

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  • Both extracellular ATP and shear stress regulate the release of nitric oxide in rat caudal artery.

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    pub_type: 杂志文章


    authors: Kwon YM,Shinozuka K,Kagota S,Yamaguchi Y,Nakamura K,Kunitomo M

    更新日期:1999-05-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章,评审


    authors: Grounds MD,Radley HG,Gebski BL,Bogoyevitch MA,Shavlakadze T

    更新日期:2008-07-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Barbier J,Mouas C,Rannou-Bekono F,Carré F

    更新日期:2007-08-01 00:00:00

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    journal_title:Clinical and experimental pharmacology & physiology

    pub_type: 杂志文章


    authors: Miura I,Nasa Y,Ichihara K,Abiko Y

    更新日期:1991-04-01 00:00:00

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

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    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