当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > [3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype.

[3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype.

Abstract：

:The mode of binding of [3H]BQ-123 (cyclo(-D-Trp-D-Asp-[prolyl-3,4 (n)-[3H]]Pro-D-Val-Leu)), an endothelin receptor antagonist radioligand, was evaluated in the human neuroblastoma cell line SK-N-MC at 37 degrees C. Scatchard analysis indicated the presence of a single class of [3H]BQ-123 binding sites with a high affinity of 3.2 nM. [3H]BQ-123 binding achieved steady state within 7 min and dissociated with a half-time of 1.4 min, while [125I] endothelin-1 binding barely reached a steady state even after 6 h and showed little dissociation. [3H]BQ-123 binding was sensitive to endothelin-1 and endothelin-2 (Ki values = 0.058 and 0.10 nM, respectively) and the endothelin ETA receptor-selective antagonist BQ-123 (Ki = 3.3 nM), while showing low affinity for endothelin-3 (Ki = 50 nM), the endothelin ETB receptor-selective agonist BQ-3020 (Ki = 970 nM) and other bioactive peptides. Thus, [3H]BQ-123 is a specific and reversible radioligand for endothelin ETA receptors. The rapid reversibility of [3H]BQ-123 binding should provide a tool for estimating the equilibrium inhibition constants (Ki values) of various compounds for endothelin ETA receptors.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Ihara M,Yamanaka R,Ohwaki K,Ozaki S,Fukami T,Ishikawa K,Towers P,Yano M

doi

10.1016/0014-2999(94)00670-3

subject

Has Abstract

pub_date

1995-02-14 00:00:00

pages

1-6

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)00670-3

journal_volume

274

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • Apomorphine prevents LPS-induced IL-23 p19 mRNA expression via inhibition of JNK and ATF4 in HAPI cells.

    abstract：:Inflammation has been reported to be closely related to exaggeration of cerebral ischemia and neurodegenerative diseases. Microglia, resident immune cells in the central nervous system, can be activated in response to neuronal injury and produce proinflammatory cytokines, resulting in further aggravation of neuronal i...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.12.014

    authors： Hara H,Kimoto D,Kajita M,Takada C,Kamiya T,Adachi T

    更新日期：2017-01-15 00:00:00

  • Converting enzyme inhibition and vascular prostacyclin synthesis: effect of kinin receptor antagonism.

    abstract：:The effects of angiotensin I-converting enzyme (ACE) inhibitors and bradykinin (BK) on prostacyclin (PGI2) production in isolated arterial tissue were investigated. Rings of rat abdominal aorta were incubated in Krebs-Ringer bicarbonate buffer and PGI2 generation was assessed by the determination of its stable hydroly...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(90)94795-y

    authors： Hoffmann G,Pietsch R,Göbel BO,Weisser B,Bönner G,Vetter H,Düsing R

    更新日期：1990-03-13 00:00:00

  • Evaluation of receptor mechanism mediating fentanyl analgesia and toxicity.

    abstract：:In the present study the antagonism of fentanyl pharmacodynamics was studied in the mouse and the receptor populations mediating the analgesic and lethal effects of fentanyl were examined. Both 1 and 8 days following implantation (s.c.) of a 15 mg naltrexone pellet there was a significant shift to the right of the fen...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(91)90512-o

    authors： Jang Y,Yoburn BC

    更新日期：1991-05-17 00:00:00

  • Synergistic effect of calcitonin gene-related peptide on adenosine-induced vasodepression in rats.

    abstract：:The action of calcitonin gene-related peptide (CGRP) on the vasodepressor response to adenosine was investigated in anesthetized rats. I.v. bolus injections of adenosine (1-100 microg/kg), acetylcholine (0.05-0.4 microg/kg), isoproterenol (1-30 ng/kg), nitroglycerin (0.3-10 microg/kg) and diltiazem (10-300 microg/kg) ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)01566-5

    authors： Sakai K,Saito K,Akima M

    更新日期：1998-03-05 00:00:00

  • Facilitation of noradrenaline release by adenosine A(2A) receptors in the epididymal portion and adenosine A(2B) receptors in the prostatic portion of the rat vas deferens.

    abstract：:The adenosine-receptor modulation of noradrenaline release was compared in prostatic and epididymal portions of rat vas deferens. In both portions, tritium overflow elicited by electrical stimulation (100 pulses/8 Hz) was reduced by the adenosine A(1) receptor agonist, N(6)-cyclopentyladenosine, and enhanced by the no...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)01906-4

    authors： Queiroz G,Diniz C,Gonçalves J

    更新日期：2002-07-12 00:00:00

  • Emetic, central nervous system, and pulmonary activities of rolipram in the dog.

    abstract：:Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity. At doses > or = 0.1 mg/kg i.v., rolipram induced emesis, anxiety, and stepping behaviors in conscious dogs, and increased heart rate and...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00457-2

    authors： Heaslip RJ,Evans DY

    更新日期：1995-11-24 00:00:00

  • The thyrotropin-releasing hormone-like peptides pGlu-Phe-Pro amide and pGlu-Glu-Pro amide increase plasma triiodothyronine levels in the mouse; the activity is sensitive to testosterone.

    abstract：:Three naturally occurring peptides, pGlu-Glu-Pro amide, pGlu-Phe-Pro amide and pGlu-Gln-Pro amide, with similar structures to thyrotropin releasing hormone (TRH) have recently been identified but no studies of their in vivo activities have been reported previously. We describe here the ability of pGlu-Phe-Pro amide an...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00593-7

    authors： Cremades A,Peñafiel R,Rausell V,Del Rio-Garcia J,Smyth DG

    更新日期：1998-09-25 00:00:00

  • Effects of derivatives of cyclic amp and cyclic gmp on contraction force of cat papillary muscles.

    abstract：:Right ventricular kitten papillary muscles were incubated with dibutyryl adenosine 3',5'-monophosphate (dbcAMP) at varying concentrations as low as 1 X 10(-4)M. A positive inotropic effect was observed with all concentrations of dbcAMP. Concomitant administration of 5 X 10(-4)M monobutyryl guanosine 3',5'-monophosphat...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(76)90280-6

    authors： Wilkerson RD,Paddock RJ,George WJ

    更新日期：1976-03-01 00:00:00

  • Pulmonary and systemic vascular effects of exogenous prostaglandin I2 in fetal lambs.

    abstract：:Effects of PGI2 upon pulmonary vascular resistance and systemic arterial pressure of near term fetuses were evaluated in anesthetized, exteriorized, unventilated fetal lambs by means of an open-chest, pump-perfused lung preparation. These effects were compared to those of PGE1 and PGE2 in the same animals. Intrapulmon...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(79)90405-9

    authors： Leffler CW,Hessler JR

    更新日期：1979-02-15 00:00:00

  • Release and aggregation of cytochrome c and alpha-synuclein are inhibited by the antiparkinsonian drugs, talipexole and pramipexole.

    abstract：:Recently, it has been shown that release of cytochrome c from the mitochondria to the cytosol is required for activation of the caspase-3-dependent cascade in apoptosis, and also for alpha-synuclein aggregation. In the present study, we examined the effects of talipexole and pramipexole on the release of cytochrome c ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(01)00902-5

    authors： Kakimura J,Kitamura Y,Takata K,Kohno Y,Nomura Y,Taniguchi T

    更新日期：2001-04-06 00:00:00

  • The impact of α-Lipoic acid on cell viability and expression of nephrin and ZNF580 in normal human podocytes.

    abstract：:Human podocytes (hPC) are essential for maintaining normal kidney function and dysfunction or loss of hPC play a pivotal role in the manifestation and progression of chronic kidney diseases including diabetic nephropathy. Previously, α-Lipoic acid (α-LA), a licensed drug for treatment of diabetic neuropathy, was shown...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2017.06.013

    authors： Leppert U,Gillespie A,Orphal M,Böhme K,Plum C,Nagorsen K,Berkholz J,Kreutz R,Eisenreich A

    更新日期：2017-09-05 00:00:00

  • Tricyclic antidepressants activate the pituitary-adrenal axis in the rat. Tolerance to repeated drug administration.

    abstract：:The effects of acute chronic administration of tricyclic antidepressants on the pituitary-adrenal axis were studied in adult male rats. Acute administration of desipramine, imipramine and chlorimipramine activated the pituitary-adrenal axis. The effect of imipramine was found to be of short duration with a significant...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(87)90812-0

    authors： Armario A,García-Marquez C

    更新日期：1987-08-11 00:00:00

  • Participation of cholinergic system in memory deficits induced by blockade of hippocampal mGlu(1) receptors.

    abstract：:We investigated the role of hippocampal group I metabotropic glutamate receptors (mGlu(1) receptors) in the retrieval process of spatial memory using 8-arm radial maze performance with 4 arms baited. In addition, the participation of the cholinergic system in memory deficits induced by mGlu(1) receptors antagonist was...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.07.010

    authors： Mikami A,Masuoka T,Yasuda M,Yamamoto Y,Kamei C

    更新日期：2007-12-01 00:00:00

  • Ca2+ release-activated channels in rat stomach smooth muscle cells.

    abstract：:In rat stomach fundus, contractions induced by Ca2+ (1.8 mM) were strikingly potentiated by thapsigargin. This potentiation was partially inhibited by the blockers of Ca2+ release activated channels (CRACs), miconazole and SK&F96365 ([1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole, HCL]) and sli...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)01537-9

    authors： Smaili SS,Cavalcanti PM,Oshiro ME,Ferreira AT,Jurkiewicz A

    更新日期：1998-01-19 00:00:00

  • Differential effect of HERG blocking agents on cardiac electrical alternans in the guinea pig.

    abstract：:Beat-to-beat alternations of the cardiac monophasic action potential, known as electrical alternans, were studied at drug concentrations that have known arrhythmogenic outcomes. Electrical alternans were elicited from the heart of anesthetized guinea pigs, both in the absence and presence of drugs that inhibit the del...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2003.12.028

    authors： Fossa AA,Wisialowski T,Wolfgang E,Wang E,Avery M,Raunig DL,Fermini B

    更新日期：2004-02-20 00:00:00

  • Validation of a pharmacological model for mitochondrial dysfunction in healthy subjects using simvastatin: A randomized placebo-controlled proof-of-pharmacology study.

    abstract：:Proof-of-pharmacology models to study compounds in healthy subjects offer multiple advantages. Simvastatin is known to induce mitochondrial dysfunction at least partly by depletion of co-enzyme Q10. The goal of this study was to evaluate a model of simvastatin-induced mitochondrial dysfunction in healthy subjects and ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,随机对照试验

    doi：10.1016/j.ejphar.2017.09.031

    authors： van Diemen MPJ,Berends CL,Akram N,Wezel J,Teeuwisse WM,Mik BG,Kan HE,Webb A,Beenakker JWM,Groeneveld GJ

    更新日期：2017-11-15 00:00:00

  • Heart rate correction of the QT duration in rats.

    abstract：:Duration of heart rate corrected QT interval (QTc) is a crucial and critical factor in the assessment of repolarization changes considering safety of drugs and cardiac disorders. In rats, a validated approach to QT correction is lacking. In this study, we tested the normalization of QTc using normalization factor acco...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2010.05.038

    authors： Kmecova J,Klimas J

    更新日期：2010-09-01 00:00:00

  • Compared effects of indapamide, hydrochlorothiazide and chlorthalidone on electrical and mechanical activities in vascular smooth muscle.

    abstract：:The effects of indapamide, hydrochlorothiazide and chlorthalidone were studied on isometric contractions, calcium contractures (in depolarized preparations) and membrane potentials in isolated longitudinal strips from rat portal veins. Indapamide inhibited all three responses more potently than did current diuretics. ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(81)90068-6

    authors： Mironneau J,Savineau JP,Mironneau C

    更新日期：1981-10-22 00:00:00

  • Novel neuroprotective effects with O-benzyl derivative of pralidoxime in soman-intoxicated rodents.

    abstract：:Pharmacological properties of oxime reactivators, not related to its ability to regenerate or reactivate nerve agent-inhibited acetylcholinesterase located at nerve synapses, have been reported to be important in protecting against poisoning by the nerve agent soman. Such non-reactivation effects have thus far been as...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2005.07.033

    authors： Loke WK,Sim MK,Go ML

    更新日期：2005-10-03 00:00:00

  • NG-nitro-L-arginine methyl ester protects against lipid peroxidation in the gerbil following cerebral ischaemia.

    abstract：:The aim of this study was to assess the role of nitric oxide (NO) in lipid peroxidation following 5 min of bilateral carotid occlusion in the Mongolian gerbil. The study consisted of 4 experimental groups (n = 10). Animals were either sham operated, subjected to bilateral carotid occlusion or administered the NO synth...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00502-c

    authors： Caldwell M,O'Neill M,Earley B,Kelly JP,Leonard BE

    更新日期：1995-10-16 00:00:00

  • Interaction between intrathecal morphine and glutamate receptor antagonists in formalin test.

    abstract：:The analgesic interaction between intrathecally administered morphine and the NMDA receptor antagonist, ((+/-)-2-amino-5-phosphonopentanoic acid; AP-5), the NMDA receptor glycine site antagonist, (5-nitro-6,7-dichloro-2,3-quinoxaline dion; ACEA 1021), or the AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic ac...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(00)00268-5

    authors： Nishiyama T

    更新日期：2000-05-03 00:00:00

  • Increase of myocardial pH by 1- and d-propranolol during ischemia of the heart in dogs.

    abstract：:Myocardial pH was measured continuously with a micro pH electrode inserted into the left ventricular wall in dogs. Anterior descending coronary flow was reduced to about 1/3 of the original flow by partial occlusion of the coronary artery. Myocardial pH decreased from 7.50--7.60 to 7.06--7.24 after partial occlusion. ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(80)90231-9

    authors： Abiko Y,Sakai K

    更新日期：1980-06-27 00:00:00

  • Effect of dantrolene sodium on the transmembrane potentials and contractility of guinea pig atrial myocardium.

    abstract：:Dantrolene sodium (3 X 10(-4) M) exerted a biphasic effect on the mechanical and electrical activity of the isolated guinea pig left atrium. In the first phase, the drug increased the contractile force by about 200%, and prolonged the action potential duration. This transient positive inotropic effect was antagonized ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(81)90529-x

    authors： Mészáros J,Kecskeméti V,Szegi J

    更新日期：1981-09-11 00:00:00

  • Potent antioxidant role of pirfenidone in experimental cirrhosis.

    abstract：:Three important features must be considered when proposing therapeutic strategies in liver cirrhosis: inflammation, oxidative stress and fibrogenesis. Pirfenidone is a synthetic molecule which oxidative action has not been tested in cirrhosis. Cirrhosis was induced in rats by ligation of the common bile duct or carbon...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2008.06.110

    authors： Salazar-Montes A,Ruiz-Corro L,López-Reyes A,Castrejón-Gómez E,Armendáriz-Borunda J

    更新日期：2008-10-24 00:00:00

  • The hypotensive agent dodoneine inhibits L-type Ca2+ current with negative inotropic effect on rat heart.

    abstract：:Agelanthus dodoneifolius is one of the medicinal plants used in African pharmacopeia and traditional medicine for the treatment of cardiovascular diseases. A chemical analysis has identified one of the active principles: Dodoneine (Ddn). It is a new dihydropyranone which exerts hypotensive and vasorelaxant effects on ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2014.01.059

    authors： Carré G,Carreyre H,Ouedraogo M,Becq F,Bois P,Thibaudeau S,Vandebrouck C,Bescond J

    更新日期：2014-04-05 00:00:00

  • The role of the mu 2-opioid receptor in the antitussive effect of morphine in mu 1-opioid receptor-deficient CXBK mice.

    abstract：:The effect of morphine on the capsaicin-induced cough reflex was studied in mu 1-opioid receptor-deficient CXBK mice. There was no significant difference between the morphine-induced antitussive effect in CXBK mice and C57BL/6 mice, a progenitor strain. Furthermore, the antitussive effects of morphine in both the CXBK...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90553-t

    authors： Kamei J,Iwamoto Y,Suzuki T,Misawa M,Nagase H,Kasuya Y

    更新日期：1993-08-10 00:00:00

  • Epidermal growth factor accelerates pancreatic recovery after caerulein-induced pancreatitis.

    abstract：:We examined the influence of endogenous and exogenous epidermal growth factor (EGF) on pancreatic repair after acute pancreatitis. Caerulein-induced pancreatitis was evoked in rats with intact or removed salivary glands and EGF (10 microg/kg) was administered starting 24 h after cessation of caerulein infusion. The do...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(00)00301-0

    authors： Dembiński A,Warzecha Z,Konturek PC,Ceranowicz P,Stachura J,Tomaszewska R,Konturek SJ

    更新日期：2000-06-09 00:00:00

  • Inhibition of cytochrome P450 2J2 by tanshinone IIA induces apoptotic cell death in hepatocellular carcinoma HepG2 cells.

    abstract：:Cytochrome P450 2J2 (CYP2J2) is highly expressed in human tumors and carcinoma cell lines, and has been implicated in the pathogenesis of human cancers. The aim of this study was to identify a compound that could inhibit the activity of CYP2J2, and to examine its anticancer activity. To identify CYP2J2 inhibitors, 10 ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.07.047

    authors： Jeon YJ,Kim JS,Hwang GH,Wu Z,Han HJ,Park SH,Chang W,Kim LK,Lee YM,Liu KH,Lee MY

    更新日期：2015-10-05 00:00:00

  • Endothelin and 5-hydroxytryptamine on rat pulmonary artery in pulmonary hypertension.

    abstract：:Contractile responses to endothelin, 5-hydroxytryptamine (5-HT), noradrenaline and potassium were obtained on isolated preparations of pulmonary artery from rats made pulmonary hypertensive by an injection of monocrotaline (105 mg/kg s.c.) 4 weeks previously. When compared with data obtained in control rats, the poten...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(90)90524-a

    authors： Wanstall JC,O'Donnell SR

    更新日期：1990-02-06 00:00:00

  • Negative inotropic effects of diadenosine tetraphosphate are mediated by protein kinase C and phosphodiesterases stimulation in the rat heart.

    abstract：:Extracellular diadenosine polyphosphates (ApnA) are recently considered as an endogenous signaling compounds with transmitter-like activity which present in numerous tissues, including heart. It has been demonstrated previously that extracellular ApnA cause alteration of the heart functioning via purine receptors in d...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2017.12.024

    authors： Pakhomov N,Pustovit K,Potekhina V,Filatova T,Kuzmin V,Abramochkin D

    更新日期：2018-02-05 00:00:00