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

abstract：:We report positron emission tomography studies of beta-adrenoceptors in the human thorax with (S)-[(11)C]CGP12388 (4-(3-(2'-[(11)C]-isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one). Beta-adrenoceptors have previously been quantified using (S)-[(11)C]CGP12177 (4-(3-tert-butylamino-2-hydroxypropoxy)-2H-benzimida...

journal_title：European journal of pharmacology

authors： Elsinga PH,Doze P,van Waarde A,Pieterman RM,Blanksma PK,Willemsen AT,Vaalburg W

更新日期：2001-12-21 00:00:00

abstract：:Previous work has demonstrated that neuropeptide tyrosine (NPY), Y(1) receptor and Y(2) receptor are critical in modulation of pain after nerve injury. We hypothesized that NPY was important for nociception after surgical incision. As a model of postoperative pain, rats underwent a plantar incision in one hindpaw. Wes...

journal_title：European journal of pharmacology

authors： Yalamuri SM,Brennan TJ,Spofford CM

更新日期：2013-01-05 00:00:00

abstract：:Vascular smooth muscle cells in culture are capable of secreting endothelin which is a vasoconstrictor and mitogenic peptide. The effect of glucocorticoids on endothelin release from vascular smooth muscle cells of the rat and rabbit aortas was investigated. Micromolar concentrations of dexamethasone and cortisol caus...

journal_title：European journal of pharmacology

authors： Kanse SM,Takahashi K,Warren JB,Ghatei M,Bloom SR

更新日期：1991-06-18 00:00:00

abstract：:The interaction of phencyclidine, dexoxadrol, their analogs and stereoisomers with phencyclidine receptors was compared to their ability to induce stereotyped behavior and ataxia after i.c.v. administration to rats. The order of potency for binding to phencyclidine receptors revealed that among the stereoisomers of ph...

journal_title：European journal of pharmacology

authors： Contreras PC,Rice KC,Jacobson AE,O'Donohue TL

更新日期：1986-02-11 00:00:00

abstract：:The action of antidepressants on cell proliferation (bromodeoxyuridine (BrdU) or [3H]thymidine incorporation) was studied in the adult rat hippocampus in vivo and in neural precursors (immature rat cerebellar granule cells) in vitro. In vivo, prolonged (21 days) but not acute (single) intraperitoneal treatment with fl...

journal_title：European journal of pharmacology

authors： Manev H,Uz T,Smalheiser NR,Manev R

更新日期：2001-01-05 00:00:00

abstract：:We are interested in the rat as an animal model for infant-mother attachment. In the first experiment we tried to distinguish between a preference for familiar animals (attachment theory) and a preference for genetically related animals (kin selection theory) with the use of an early cross-fostering procedure. Genetic...

journal_title：European journal of pharmacology

authors： Sigling HO,Wolterink-Donselaar IG,Spruijt BM

更新日期：2009-06-10 00:00:00

abstract：:The site of action of the kappa opioid receptor agonist, U-50,488H in suppressing the development of tolerance to morphine antinociception was examined by local application, either intrathecal (i.t., spinal) or intracerebroventricular (i.c.v., supraspinal) in mice. Mice given morphine s.c., i.c.v. or i.t. daily develo...

journal_title：European journal of pharmacology

authors： Takahashi M,Senda T,Kaneto H

更新日期：1991-08-06 00:00:00

abstract：:Studies were done to assess the effects of 4-aminopyridine (4AP) and streptomycin (SM) on transmitter release parameters and extracellularly recorded presynaptic action potential. The application of 5 micrometer 4AP resulted in a marked increase in the mean quantal content (m1) associated with an increase in the total...

journal_title：European journal of pharmacology

authors： Enomoto K,Maeno T

更新日期：1981-11-19 00:00:00

abstract：:Zolpidem has abuse potential, particularly among individuals with histories of drug abuse. This double-blind, placebo-controlled, cross over pilot study investigated the subjective effects of zolpidem (10 mg) in drug-naïve females. Over the course of a 5-h period vital signs were monitored and a series of computerized...

journal_title：European journal of pharmacology

authors： Licata SC,Penetar DM,Dunlap S,Lukas SE

更新日期：2008-11-19 00:00:00

abstract：:Thoracic preganglionic sympathetic nerve activity, blood pressure, heart rate and femoral arterial conductance were recorded in anaesthetised, paralysed cats. Cumulative dose-response curves were constructed for 8-OH-DPAT, ipsapirone and clonidine. All three drugs caused dose-related falls in blood pressure which were...

journal_title：European journal of pharmacology

authors： Ramage AG,Fozard JR

更新日期：1987-06-19 00:00:00

abstract：:The effect of lithium ion (Li+) on receptor-mediated synthesis of cyclic GMP, a putative second messenger, was examined using intact murine neuroblastoma cells (clone N1E-115). Lithium chloride potently inhibited cyclic GMP formation stimulated by the neuropeptides, neurotensin, angiotensin II and bradykinin in an ide...

journal_title：European journal of pharmacology

authors： Kanba S,Pfenning M,Kanba KS,Richelson E

更新日期：1986-07-15 00:00:00

abstract：:The chick has a practical advantage in the screening process in that chicks require only small quantities of drugs. The chick separation stress paradigm has traditionally been recognized as a valid form of anxiolytic screening. Further, chick behavior involving standing motionless with eyes closed or sitting motionles...

journal_title：European journal of pharmacology

authors： Furuse M

更新日期：2015-09-05 00:00:00

abstract：:Cancer cell lines derived from hepatocytes have an altered phenotype and they lack hepatocyte-specific functions. It is at least partly due to the under-expression of transcription factors such as hepatocyte nuclear factor 4α (HNF4α), steroid receptor co-activator 1 (SRC1) etc. Recently, a strategy of transient transf...

journal_title：European journal of pharmacology

authors： Novotna A,Doricakova A,Vrzal R,Pavek P,Dvorak Z

更新日期：2011-11-01 00:00:00

abstract：:Serotonin(1A) (5-HT(1A)) receptors are involved in anxiety. This study focuses on the role of genetic factors on the anxiety-related effects of 5-HT(1A) receptor stimulation using both a within subject design. The effects of 5-HT(1A) receptor activation were studied in high- and low-anxiety mice (129S6/SvEvTac (S6) an...

journal_title：European journal of pharmacology

authors： Bouwknecht JA,van der Gugten J,Groenink L,Olivier B,Paylor RE

更新日期：2004-06-21 00:00:00

abstract：:The leukotrienes are potent inflammatory mediators, which may have a role in inflammatory diseases such as allergic rhinitis, inflammatory bowl disease and asthma. Zafirlukast, a cysteinyl leukotriene receptor antagonist, is claimed to be effective in asthma. However, it is not known whether these leukotrienes are inv...

journal_title：European journal of pharmacology

authors： Jain NK,Kulkarni SK,Singh A

更新日期：2001-06-29 00:00:00

abstract：:The calcium currents (ICa) of isolated smooth muscle cells (urinary bladder of the guinea-pig) were analyzed at 35 degrees C and 3.6 mM [Ca]0. The whole cells were voltage-clamped with a single patch electrode which was filled with 150 mM CsCl in order to block potassium outward currents. Tiapamil reduced ICa at conce...

journal_title：European journal of pharmacology

authors： Klöckner U,Isenberg G

更新日期：1986-08-15 00:00:00

abstract：:The Kd values of the multiple agonist binding sites in cardiac muscarinic receptors (mAChR) and pD2 values for negative inotropic actions were determined independently and their relation was examined. The guinea-pig cardiac mAChR is known to have three agonist binding sites (super-high (SH), high (H) and low (L) affin...

journal_title：European journal of pharmacology

authors： Mizushima A,Uchida S,Matsumoto K,Osugi T,Kagiya T,Zhou XM,Higuchi H,Yoshida H

更新日期：1985-12-17 00:00:00

abstract：:The ability of calcium entry blockers to inhibit allergic histamine release from rabbit leukocytes was studied. Bepridil, verapamil, nifedipine, diltiazem and TMB-8 produced concentration-dependent inhibition of allergic histamine release from rabbit leukocytes. The calculated IC50s (microM) were as follows: verapamil...

journal_title：European journal of pharmacology

authors： Chand N,Pillar J,Diamantis W,Sofia RD

更新日期：1985-01-08 00:00:00

abstract：:We studied the effects of inhaled formoterol (0.75 mg/ml, 60 breaths = 26 micrograms), a long-acting beta 2-adrenoceptor agonist, or of the more short-acting drug, salbutamol (25 mg/ml, 60 breaths = 875 micrograms), on acute airflow obstruction and airway microvascular leakage (MVL) induced by inhaled histamine in ane...

journal_title：European journal of pharmacology

authors： Tokuyama K,Lötvall JO,Löfdahl CG,Barnes PJ,Chung KF

更新日期：1991-01-25 00:00:00

abstract：:NO plays a key role in the pathological mechanisms of articular diseases. As cytoskeletal proteins are responsible for the polymerization, stabilization, and dynamics of the cytoskeleton network, we investigated whether cytoskeletal proteins are the intracellular pathological targets of NO. We aimed at clarifying whet...

journal_title：European journal of pharmacology

authors： Kao XB,Chen Q,Gao Y,Fan P,Chen JH,Wang ZL,Wang YQ,Chen YN,Yan YP

更新日期：2018-04-05 00:00:00

abstract：:The use of antipsychotic medication has consistently been associated with serious side effects including weight gain and metabolic abnormalities. Strategies for mitigating these side effects have been tested, yet effective interventions have not been identified. The current study tested whether two recently identified...

journal_title：European journal of pharmacology

authors： Belanoff JK,Blasey CM,Clark RD,Roe RL

更新日期：2011-03-25 00:00:00

abstract：:Citrus flavonoids are acknowledged for numerous pharmacological activities, including the myorelaxant effect on various smooth muscles. However, there is no data on their effect on jejunum contractility. Therefore, the aim of the study at hand was to evaluate the impact of hesperetin and diosmetin along with their gly...

journal_title：European journal of pharmacology

authors： Mendel M,Chłopecka M,Dziekan N,Karlik W

更新日期：2016-11-15 00:00:00

abstract：:The comparative dromotropic activity of timolol (TML) and propranolol (PPL) was studied by means of His bundle electrograms in two groups of pentobarbital-anesthetized dogs: group I, 7 non-atropinized dogs; group II, 8 atropinized dogs. beta-Blocking agents were injected in 4 cumulative doses in each dog at 3 days' in...

journal_title：European journal of pharmacology

authors： Jaillon P,Heckle J,Weissenburger J,Cheymol G

更新日期：1978-01-15 00:00:00

abstract：:In neutrophils and several other phagocytes, a pertussis and cholera toxin-sensitive guanine nucleotide-binding protein (G-protein) couples the receptors for formyl methionine-containing chemotactic peptides to stimulation of phospholipase C. We used membranes of myeloid-differentiated HL 60 cells to study the role of...

journal_title：European journal of pharmacology

authors： Gierschik P,Sidiropoulos D,Steisslinger M,Jakobs KH

更新日期：1989-12-05 00:00:00

abstract：:The effects of endothelin on coronary circulation were studied in isolated rat heart using a constant-flow system. Endothelin (10 fmol to 20 pmol/g heart weight) elevated the coronary perfusion pressure in a dose-dependent manner. Nifedipine (100 nM) inhibited the vasoconstriction and shifted the dose-response curve t...

journal_title：European journal of pharmacology

authors： Fukuda K,Hori S,Kusuhara M,Satoh T,Kyotani S,Handa S,Nakamura Y,Oono H,Yamaguchi K

更新日期：1989-06-20 00:00:00

abstract：:Administration of ovalbumin by aerosol to sensitised rats produced a rapid (15 min) protein exudation in different airway tissues, as determined by Evans blue staining. This was associated with marked mast cell degranulation determined by histological examination, with there being no difference between mucosal and con...

journal_title：European journal of pharmacology

authors： Damazo AS,Tavares de Lima W,Perretti M,Oliani SM

更新日期：2001-08-24 00:00:00

abstract：:Concanavalin A-induced hepatitis is often used as a model of liver injury. In this model, plasma tumor necrosis factor-alpha (TNF-alpha) level increased in concanavalin A-injected mice. Prophylactic treatment with Y-40138, N-[1-(4-[4-(pyrimidin-2-yl)piperazin-1-yl]methyl phenyl)cyclopropyl] acetamide.HCl, significantl...

journal_title：European journal of pharmacology

authors： Fukuda T,Mogami A,Hisadome M,Komatsu H

更新日期：2005-10-31 00:00:00

abstract：:Persistent hyperglycemia increases a systemic oxidative stress, causing the onset of vascular endothelial dysfunction and atherosclerosis. Diallyl trisulfide (DAT), a natural organosulfur compound in garlic, has been reported to have actions of dilating blood vessels and antibacteria, etc. In this study, models of obe...

journal_title：European journal of pharmacology

authors： Liu LL,Yan L,Chen YH,Zeng GH,Zhou Y,Chen HP,Peng WJ,He M,Huang QR

更新日期：2014-02-15 00:00:00

abstract：:Microglia initially undergo rapid activation in response to injury and stressful stimuli, such as hypoxia. Oxidative stress and the inflammatory response play critical roles in hypoxic-ischemic brain injury. Carvedilol is a β-blocker used to treat high blood pressure and heart failure. In this study, we investigated w...

journal_title：European journal of pharmacology

authors： Gao X,Wu B,Fu Z,Zhang Z,Xu G

更新日期：2017-11-05 00:00:00

abstract：:Ascorbate has both antioxidant and pro-oxidant activities. We have previously shown that plasma levels of ascorbate induce constriction and blockade of dilatation mediated by endothelium-derived hyperpolarizing factor (EDHF). In this study we sought to determine if these detrimental actions were mediated by a prooxida...

journal_title：European journal of pharmacology

authors： Nelli S,Craig J,Martin W

更新日期：2009-07-01 00:00:00