Further evaluation of the selectivity of a novel antihypertensive agent, SGB-1534, for peripheral alpha 1-adrenoceptors in the spinally anesthetized dog.


:Experiments were designed to examine some characteristics of an orally active antihypertensive agent, SGB-1534 on alpha-adrenoceptors in spinally anesthetized dogs. In the saphenous arterial bed perfused by a constant pump volume, saphenous nerve stimulation and bolus applications of norepinephrine and phenylephrine into the artery-evoked frequency- or dose-dependent increases (i.e. vasoconstriction) in perfusion pressure. SGB-1534 and prazosin infused i.v. significantly reduced the vasoconstriction in response to saphenous nerve stimulation and the two agonists. In the saphenous arterial bed, alpha 1-adrenoceptor antagonist potency of SGB-1534 on a weight basis was approximately 30 times greater than that of prazosin. Unlike SGB-1534 and prazosin, yohimbine failed to inhibit the vasoconstriction induced by phenylephrine, but instead potentiated the vasoconstrictor response to saphenous nerve stimulation. The equieffective doses of methoxamine and B-HT 920 given i.v. produced sustained pressor responses. SGB-1534 and prazosin applied i.v. in a cumulative way reduced dose dependently the pressor response to methoxamine but not that to B-HT 920. When the doses that blunted the sustained pressor response to methoxamine by 50% were compared, the alpha 1-adrenoceptor antagonistic activity of SGB-1534 was nine times greater than that of prazosin.


Eur J Pharmacol


Imagawa J,Sakai K




Has Abstract


1986-11-19 00:00:00














  • Pharmacological properties of two analogues of angiotensin II containing carboranylalanine (Car).

    abstract::The pharmacological properties of two angiotensin II analogues containing carboranylalanine (Car) are reported. Sar-Arg-Val-Tyr-Val-His-Pro-Car is a weak partial agonist showing 15% intrinsic activity and a very long lasting action, specific for the angiotensin II receptor of the rabbit aorta. Sar-Arg-Val-Car-Val-His-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Escher E,Guillemette G,Leukart O,Regoli D

    更新日期:1980-09-05 00:00:00

  • Diazepam as a discriminative cue: its antagonism by bemegride.

    abstract::Gerbils trained to respond differentially to the presence or absence of diazepam (8.0 mg/kg) in a T-maze showed a dose-related antagonism when challenged with bemegride (5.0-40.0 mg/kg). Gerbils trained with a mixture of diazepam (8.0 mg/kg) and bemegride (20.0 mg/kg) evidenced response control more slowly than the gr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Johansson JO,Järbe TU

    更新日期:1975-02-01 00:00:00

  • Hydrophobic statins induce autophagy and cell death in human rhabdomyosarcoma cells by depleting geranylgeranyl diphosphate.

    abstract::Statins are the most common type of medicine used to treat hypercholesterolemia; however, they are associated with a low incidence of myotoxicity such as myopathy and rhabdomyolysis. The mechanisms for the adverse effects remain to be fully elucidated for safer chronic use and drug development. The results of our earl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Araki M,Maeda M,Motojima K

    更新日期:2012-01-15 00:00:00

  • Effects of sotalol, (-)-propranolol and prazosin on reperfusion-induced arrhythmias and increased cardiac norepinephrine release.

    abstract::The pharmacological actions of sotalol, (-)-propranolol and prazosin on norepinephrine (NE) concentration and creatine kinase (CK) activity in the coronary sinus blood of the ischemic heart were studied in open-chest dogs. A 60 min occlusion of the left anterior descending coronary artery was followed by a reperfusion...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Lamontagne D,Yamaguchi N,Nadeau R,De Champlain J,Godin D,Campeau N

    更新日期:1986-04-09 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


    authors: Kmecova J,Klimas J

    更新日期:2010-09-01 00:00:00

  • Effects of chlorogenic acid and its metabolites on the sleep-wakefulness cycle in rats.

    abstract::The effect of chlorogenic acid on the sleep-wakefulness cycle in rats was investigated in comparison with those of caffeic acid (the metabolite of chlorogenic acid) and dihydrocaffeic acid (the metabolite of caffeic acid). A significant prolongation of sleep latency was observed with chlorogenic acid and caffeic acid ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Shinomiya K,Omichi J,Ohnishi R,Ito H,Yoshida T,Kamei C

    更新日期:2004-11-19 00:00:00

  • Effects of intravenous baclofen on dorsal horn neurons of spinal cats.

    abstract::Intravenous baclofen (1 mg/kg) abolished or severely attenuated the high threshold late component (but not the low threshold early component of long duration (greater than 150 msec) discharges evoked in cat dorsal horn neurons by intense transcutaneous electrical stimulation. Baclofen similarly reduced the spontaneous...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Piercey MF,Hollister RP

    更新日期:1979-02-01 00:00:00

  • Evidence for a role of human organic anion transporters in the muscular side effects of HMG-CoA reductase inhibitors.

    abstract::The purpose of this study was to elucidate the role of human organic anion transporters (human OATs) in the induction of drug-induced skeletal muscle abnormalities. 3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors have been clinically used for lowering plasma cholesterol levels, and are known to in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Takeda M,Noshiro R,Onozato ML,Tojo A,Hasannejad H,Huang XL,Narikawa S,Endou H

    更新日期:2004-01-12 00:00:00

  • Argatroban, specific thrombin inhibitor, induced phenotype change of cultured rabbit vascular smooth muscle cells.

    abstract::To investigate whether argatroban ((2R,4R)-4-methyl-1-[N(2)-((RS)-3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid hydrate, a selective thrombin inhibitor, exerts a direct action on phenotype conversion of vascular smooth muscle cells, cultured rabbit aortic vascular smooth muscl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Yoshinaga M,Sunagawa M,Shimada S,Nakamura M,Murayama S,Kosugi T

    更新日期:2003-02-07 00:00:00

  • Vasorelaxant effect of taurine is diminished by tetraethylammonium in rat isolated arteries.

    abstract::Although the vasorelaxant effects of taurine have been studied in rabbit ear artery, rat isolated aorta and mesenteric artery, its pharmacological properties in other vascular beds and underlying mechanism(s) are still not well clarified. The present study was designed to observe the effects of taurine on the contract...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Niu LG,Zhang MS,Liu Y,Xue WX,Liu DB,Zhang J,Liang YQ

    更新日期:2008-02-02 00:00:00

  • Endothelial P2Y receptors induce hyperpolarisation of vascular smooth muscle by release of endothelium-derived hyperpolarising factor.

    abstract::The effects of P2Y receptor agonists on smooth muscle membrane potential in isolated ring segments of rat mesenteric artery were examined by intracellular microelectrodes. In the presence of inhibitors of nitric oxide-synthase and cyclo-oxygenase, the selective P2Y1 receptor agonist adenosine 5'-O-thiodiphosphate (ADP...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Malmsjö M,Erlinge D,Högestätt ED,Zygmunt PM

    更新日期:1999-01-08 00:00:00

  • Molecular pharmacology of LR-B/081, a new non-peptide angiotensin AT1 receptor antagonist.

    abstract::This report describes the molecular pharmacological properties of LR-B/081 (methyl 2-[[4-butyl-2-methyl-6-oxo-5-[[2'-(1H-tetrazol-5- yl) [1,1'-biphenyl]-4-yl]methyl]-1 (6H)-pyrimidinyl]methyl]- 3-thiophenecarboxilate), a novel non-peptide angiotensin II receptor antagonist. This compound potently displaced [3H]angiote...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Renzetti AR,Criscuoli M,Salimbeni A,Subissi A

    更新日期:1995-07-18 00:00:00

  • Effect of chronic moderate ethanol consumption on heart brain natriuretic peptide.

    abstract::There is experimental evidence indicating that chronic moderate ethanol consumption delays the age-dependent increase in blood pressure. Since the brain natriuretic peptide (BNP) is a potent hypotensive hormone, the effect of chronic ethanol treatment on the heart BNP system was investigated, using spontaneously hyper...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Guillaume P,Jankowski M,Gutkowska J,Gianoulakis C

    更新日期:1996-11-28 00:00:00

  • The open field as a paradigm to measure the effects of drugs on anxiety-like behaviors: a review.

    abstract::The open field is a very popular animal model of anxiety-like behavior. An overview of the literature on the action elicited by effective or putative anxiolytics in animal subjected to this procedure indicates that classical treatments such as benzodiazepine receptor full agonists or 5-HT(1A) receptor full or partial ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Prut L,Belzung C

    更新日期:2003-02-28 00:00:00

  • Time course of phorbol ester-induced contraction and protein kinase C activation in rat aorta.

    abstract::This study investigates the relationship between the rate of phorbol ester-induced contraction of intact rat aorta and protein kinase C activation, as assessed by the translocation of protein kinase C from the cytosolic to the particulate fraction. Aorta was exposed to Ca(2+)-free physiologic salt solution prior to ph...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bazan E,Campbell AK,Rapoport RM

    更新日期:1995-08-15 00:00:00

  • Prevention of aortic calcification by etidronate in the renal failure rat model.

    abstract::Our recent clinical study indicated that etidronate may inhibit the progression of aortic calcification in hemodialysis patients. To determine whether etidronate inhibits aortic calcification in renal failure rats, renal failure was induced by subtotal nephrectomy, in which 5/6 of the kidneys were removed. Significant...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Tamura K,Suzuki Y,Matsushita M,Fujii H,Miyaura C,Aizawa S,Kogo H

    更新日期:2007-03-08 00:00:00

  • Neuroprotective activity of chemokines against N-methyl-D-aspartate or beta-amyloid-induced toxicity in culture.

    abstract::We have examined the effect of various chemokines on neuronal toxicity in culture. In mixed cortical cultures, challenged with a brief pulse of N-methyl-D-aspartate (NMDA, 60 microM, 10 min), chemokines were either present for 2 h preceding the pulse or they were co-applied with NMDA and then kept in the medium for th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bruno V,Copani A,Besong G,Scoto G,Nicoletti F

    更新日期:2000-07-07 00:00:00

  • Comparison between dopamine transporter affinity and self-administration potency of local anesthetics in rhesus monkeys.

    abstract::Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wilcox KM,Paul IA,Woolverton WL

    更新日期:1999-02-19 00:00:00

  • Effect of acute treatment with YM992 on extracellular norepinephrine levels in the rat frontal cortex.

    abstract::The effects of acute treatment with (S)-2-[[(7-fluoroindan-4-yl)oxy]methyl]morpholine monohydrochloride (YM992), venlafaxine, fluoxetine and citalopram on extracellular norepinephrine levels were examined in the rat frontal cortex by in vivo microdialysis. YM992 (3, 10, 30 mg/kg, i.p.) dose-dependently increased extra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Hatanaka K,Yatsugi S,Yamaguchi T

    更新日期:2000-04-21 00:00:00

  • The effects of lidoflazine and flunarizine on cerebral reactive hyperemia.

    abstract::Cerebral blood flow in the rat was monitored by a venous outflow technique with an extracorporeal circulation, which allows for the continuous recording of flow over periods of several hours. The bi-fluorophenyl-piperazine derivatives, lidoflazine and flunarizine, enhanced the reactive hyperemia elicited by a brief (3...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Phillis JW,DeLong RE,Towner JK

    更新日期:1985-06-19 00:00:00

  • The mu opiate receptor is responsible for descending pain inhibition originating in the periaqueductal gray region of the rat brain.

    abstract::Opiate agonists exhibiting selectivity for mu, kappa, sigma, and delta opiate receptors were microinjected into the periaqueductal gray region (PAG) of the brain of rats to determine the receptor subtype(s) associated with the initiation of descending pain inhibition. The spinally organized, heat nociceptive tail-flic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Smith DJ,Perrotti JM,Crisp T,Cabral ME,Long JT,Scalzitti JM

    更新日期:1988-10-26 00:00:00

  • Effect of cyclosporin A on morphine-induced place conditioning in mice: involvement of nitric oxide.

    abstract::Cyclosporin A is shown to attenuate antinociceptive effects of morphine, development and expression of morphine-induced tolerance and dependency via nitric oxide (NO) pathway. In the present study, the effect of systemic cyclosporin A on morphine-induced conditioned place preference (CPP) and the probable involvement ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Motiei Langroudi R,Khoshnoodi MA,Abadi NY,Tahsili Fahadan P,Ghahremani MH,Dehpour AR

    更新日期:2005-01-10 00:00:00

  • Pharmacological characterization of the algesic response to the subplantar injection of serotonin in the rat.

    abstract::Subplantar injection of 0.10 micrograms of serotonin in the rat resulted in a brief period (0-20 min) of increased pain sensitivity to an applied force (hyperalgesia) which preceded a longer period (40-120 min) of decreased pain sensitivity (hypoalgesia). The magnitude of each of these changes and the duration of the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Vinegar R,Truax JF,Selph JL,Johnston PR

    更新日期:1989-05-30 00:00:00

  • Analysis of the effects of phosphodiesterase type 3 and 4 inhibitors in cerebral arteries.

    abstract::Inhibitors of phosphodiesterases 3 and 4, the main cyclic AMP (cAMP) degrading enzymes in arteries, may have therapeutic potential in cerebrovascular disorders. We analysed the effects of such phosphodiesterases in guinea pig cerebral arteries with organ bath technique and cyclic nucleotide assays. Guinea pig and huma...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Birk S,Edvinsson L,Olesen J,Kruuse C

    更新日期:2004-04-05 00:00:00

  • Antinociceptive effect of some carboxypeptidase A inhibitors in comparison with D-phenylalanine.

    abstract::It had previously been shown that D-phenylalanine and hydrocinnamic acid, two in vitro inhibitors of carboxypeptidase A, possess an analgesic action when injected i.p. in mice. We have studied the in vivo effects of indole-3-acetic acid, another carboxypeptidase A inhibitor, and of the following analogs of D-phenylala...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Giusti P,Carrara M,Cima L,Borin G

    更新日期:1985-10-22 00:00:00

  • The role of adenosine in rat coronary flow regulation during respiratory and metabolic acidosis.

    abstract::The role of adenosine in rat coronary flow regulation during acidosis was evaluated in isolated, perfused, Langendorff rat heart preparations exposed to brief periods of hypercapnic or metabolic acidosis. Acidosis resulted in increases in coronary flow rate, in conjunction with decreases in ventricular contractile ten...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Phillis JW,Song D,O'Regan MH

    更新日期:1998-09-04 00:00:00

  • Specific and potent interactions of carbamazepine with brain adenosine receptors.

    abstract::Carbamazepine, a drug effective in pain, seizure, and affective disorders, was screened for its ability to interact with a variety of neurotransmitter and neuromodulator binding sites on brain membranes. The most potent effect was observed on adenosine antagonist ( [3H]DPX) binding to the adenosine receptor (KI = 3.5 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Marangos PJ,Post RM,Patel J,Zander K,Parma A,Weiss S

    更新日期:1983-09-30 00:00:00

  • Novel arylaminopyridazine-GABA receptor antagonists examined electrophysiologically in Ascaris suum.

    abstract::The structure-activity relationships of 35 novel derivatives of 2-(carboxypropyl)-3-amino-4-methyl-6-phenyl pyridazine (SR 95103) were examined as gamma-aminobutyric acid (GABA) antagonists in the flap preparation of the parasitic nematode, Ascaris suum, using a two-microelectrode current-clamp technique. All but one ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Martin RJ,Sitamze JM,Duittoz AH,Wermuth CG

    更新日期:1995-03-24 00:00:00

  • Apolipoprotein B of low-density lipoprotein impairs nitric oxide-mediated endothelium-dependent relaxation in rat mesenteric arteries.

    abstract::Apolipoprotein B (ApoB) of low-density lipoprotein (LDL) causes endothelial dysfunction in the initial stage of atherogenesis. The present study was designed to explore the underlying molecular mechanisms involved. Rat mesenteric arteries were organ cultured in the presence of different concentrations of ApoB or LDL. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Zhang Y,Zhang W,Edvinsson L,Xu CB

    更新日期:2014-02-15 00:00:00

  • CNS site of antiarrhythmic action of diphenylhydantoin (DPH) in the cat.

    abstract::Diphenylhydantoin (DPH) is known to be a potent anticonvulsant agent, useful in treating and preventing grand mal seizures. More recently, DPH was reported also to be a potent antiarrhythmic agent acting by means of a depressant action on the heart. The present experiments demonstrated that DPH has also a potent antia...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Lisander B,Jaju B,Wang SC

    更新日期:1975-03-01 00:00:00