Effects of endothelin receptor antagonism with bosentan on peripheral nerve function in experimental diabetes.

abstract：:YM471, (Z)-4'-[4,4-difluoro-5-[2-(4-dimethylaminopiperidino)-2-oxoethylidene]-2,3,4,5-tetrahydro-1H-1-benzoazepine-1-carbonyl]-2-phenylbenzanilide monohydrochloride, is a newly synthesized potent vasopressin (AVP) receptor antagonist. Its effects on binding to and signal transduction by cloned human AVP receptors (V(1...

journal_title：British journal of pharmacology

authors： Tsukada J,Tahara A,Tomura Y,Wada Ki,Kusayama T,Ishii N,Yatsu T,Uchida W,Taniguchi N,Tanaka A

更新日期：2001-07-01 00:00:00

abstract：:1. A pentobarbitone-anaesthetized canine model of myocardial conduction was developed to evaluate drug effects on intra-atrial (I-A), intra-ventricular (I-V) and atrioventricular (A-V) conduction parameters, both at rest and during electrical pacing of the right atrium or ventricle. Drug effects on the ability of the ...

journal_title：British journal of pharmacology

authors： Allely MC,Alps BJ

更新日期：1988-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Airway remodelling is a consequence of long-term inflammation and MAPKs are key signalling molecules that drive pro-inflammatory pathways. The endogenous MAPK deactivator--MAPK phosphatase 1 (MKP-1)--is a critical negative regulator of the myriad pro-inflammatory pathways activated by MAPKs in th...

journal_title：British journal of pharmacology

authors： Manetsch M,Ramsay EE,King EM,Seidel P,Che W,Ge Q,Hibbs DE,Newton R,Ammit AJ

更新日期：2012-08-01 00:00:00

abstract：:1. The respiratory response to microinjection of tachykinins and analogues into the commissural nucleus of the solitary tract (cNTS) of urethane-anaesthetized rats was investigated in the presence and absence of selective tachykinin NK(1), NK(2) and NK(3) antagonists (RP 67580, SR 48968 and SR 142801, respectively). 2...

journal_title：British journal of pharmacology

authors： Mazzone SB,Geraghty DP

更新日期：2000-03-01 00:00:00

abstract：:Cyclic nucleotide phosphodiesterases (PDEs) that specifically inactivate the intracellular messengers cAMP and cGMP in a compartmentalized manner represent an important enzyme class constituted by 11 gene-related families of isozymes (PDE1 to PDE11). Downstream receptors, PDEs play a major role in controlling the sign...

journal_title：British journal of pharmacology

authors： Keravis T,Lugnier C

更新日期：2012-03-01 00:00:00

abstract：:Rabbits treated with 2-deoxy-D-glucose (2DG) (300 mg/kg) show an increased intake of food and water. Pretreatment with haloperidol (1 mg/kg) abolishes the increase in water intake but does not prevent the increase in food intake. ...

journal_title：British journal of pharmacology

authors： Anderson J,Sharman DF,Stephens DB

更新日期：1979-05-01 00:00:00

abstract：:1. Noradrenaline sensitivity and acetylcholine-induced relaxation were investigated in mesenteric resistance arteries from female Wistar rats (220-250 g) following exposure to isotonic supraphysiological glucose solutions (20 and 45 mM, in physiological buffer, 2 h incubation). 2. Arteries incubated in 20 mM glucose d...

journal_title：British journal of pharmacology

authors： Taylor PD,Poston L

更新日期：1994-11-01 00:00:00

abstract：:1. Antidepressant drugs are known to inhibit some changes evoked by glucocorticoids, as well as a hyperactivity of hypothalamic-pituitary-adrenal (HPA) axis, often observed in depression. 2. The aim of present study was to investigate effects of various antidepressant drugs on the glucocorticoid-mediated gene transcri...

journal_title：British journal of pharmacology

authors： Budziszewska B,Jaworska-Feil L,Kajta M,Lasoń W

更新日期：2000-07-01 00:00:00

abstract：:1. Besides its antimuscarinic effects, propiverine may possess an additional mode of action. We compared the effects of propiverine, three of its metabolites (M-5, M-6, M-14) and atropine in human, pig and mouse urinary bladder preparations in order to elucidate the nature of a possible additional mode of action. 2. L...

journal_title：British journal of pharmacology

authors： Wuest M,Hecht J,Christ T,Braeter M,Schoeberl C,Hakenberg OW,Wirth MP,Ravens U

更新日期：2005-07-01 00:00:00

abstract：:1 The effects of the prostaglandin synthetase inhibitor, indomethacin and the prostaglandin antagonist SC-19220 (1-acetyl-2-[8-chloro-10,11-dihydrodibenz (b,f) (1,4)oxazepine-10-carbonyl] hydrazine), were examined on the tone of the guinea-pig isolated tracheal preparation and on the responses of the preparation to pr...

journal_title：British journal of pharmacology

authors： Farmer JB,Farrar DG,Wilson J

更新日期：1974-12-01 00:00:00

abstract：:1. The binding of 2-[125I]-iodomelatonin to chicken brain membranes, and the inhibition of binding by melatonin, N-acetyltryptamine and luzindole, were examined at temperatures between 4 degrees C and 37 degrees C. 2. At all temperatures studied, the binding affinity (Kd or Ki) for 2-[125I]-iodomelatonin, melatonin (b...

journal_title：British journal of pharmacology

authors： Chong NW,Sugden D

更新日期：1994-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Aminoguanidine (AG), an inhibitor of advanced glycation endproducts, has been shown to prevent arterial stiffening and cardiac hypertrophy in streptozotocin (STZ) and nicotinamide (NA)-induced type 2 diabetes in rats. Our aims were to examine whether AG produced benefits on cardiac pumping mechan...

journal_title：British journal of pharmacology

authors： Wu MS,Liang JT,Lin YD,Wu ET,Tseng YZ,Chang KC

更新日期：2008-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Peptides from venomous animals have long been important for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide from the venom of the armed spider Phoneutria nigriventer, produces analgesia by blocking the TRPA1 channel. EXPERIMENTA...

journal_title：British journal of pharmacology

authors： Tonello R,Fusi C,Materazzi S,Marone IM,De Logu F,Benemei S,Gonçalves MC,Coppi E,Castro-Junior CJ,Gomez MV,Geppetti P,Ferreira J,Nassini R

更新日期：2017-01-01 00:00:00

abstract：:1. Comparison of the rank order of potency of the natural prostanoids prostaglandin E2 (PGE2), PGD2, PGF2 alpha and carbaprostacyclin in stimulating cyclic AMP in Jurkat cells is consistent with the presence of an EP receptor. 2. Lack of responsiveness to the EP1/EP3 selective agonist, sulprostone, and the EP2 agonist...

journal_title：British journal of pharmacology

authors： De Vries GW,Guarino P,McLaughlin A,Chen J,Andrews S,Woodward DF

更新日期：1995-08-01 00:00:00

abstract：:1 N-2-Chlorethyl-N-ethyl-2-bromobenzylamine hydrochloride (DSP 4) 50 mg/kg intraperitoneally, produced a long-term decrease in the capacity of brain homogenates to accumulate noradrenaline with significant effect 8 months after the injection. It had no effect on the noradrenaline uptake in homogenates from the striatu...

journal_title：British journal of pharmacology

authors： Ross SB

更新日期：1976-12-01 00:00:00

abstract：:1. Recombinant human ETA receptors were expressed in a mouse fibroblast cell line (Ltk- cell) and functional coupling of the receptors with Ca2+ permeable channels at low concentrations of endothelin-1 (ET-1) was investigated using whole-cell recordings and monitoring the changes in intracellular free Ca2+ concentrati...

journal_title：British journal of pharmacology

authors： Enoki T,Miwa S,Sakamoto A,Minowa T,Komuro T,Kobayashi S,Ninomiya H,Masaki T

更新日期：1995-06-01 00:00:00

abstract：:1. Glycine responses were studied under voltage clamp in Xenopus oocytes injected with cDNA encoding mammalian glycine receptor subunits and in rat medullary neurones. Bath application of glycine gave strychnine-sensitive currents which reversed close to the expected equilibrium potentials for chloride ions. The peak ...

journal_title：British journal of pharmacology

authors： Downie DL,Hall AC,Lieb WR,Franks NP

更新日期：1996-06-01 00:00:00

abstract：:1 Because normal human blood platelets contain higher concentrations of taurine than any other amino acid, and have a platelet: plasma concentration gradient exceeding 400: 1, we isolated the cells in vitro and incubated them with radioactively labelled taurine in order to investigate the existence of a metabolically-...

journal_title：British journal of pharmacology

authors： Ahtee L,Boullin DJ,Paasonen MK

更新日期：1974-10-01 00:00:00

abstract：:1 The effects of indomethacin and eicosa-5,8,11,14-tetraynoic acid (ETYA) on the contractile response of the transmurally stimulated rabbit portal vein were studied in vitro.2 When the veins were stimulated for 240 pulses at 1 and 2 Hz, the responses were potentiated by indomethacin and ETYA. However, responses to 4 a...

journal_title：British journal of pharmacology

authors： Greenberg R

更新日期：1974-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) plays a role in thermogenesis. The exogenous compound capsaicin increased SERCA-mediated ATP hydrolysis not coupled to Ca²⁺ transport. Here, we have sought to identify endogenous compounds that may function as SERCA uncoupling agents. EXPERIMENTAL A...

journal_title：British journal of pharmacology

authors： Mahmmoud YA,Gaster M

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Benzofurans are newly used psychoactive substances, but their pharmacology is unknown. The aim of the present study was to pharmacologically characterize benzofurans in vitro. EXPERIMENTAL APPROACH:We assessed the effects of the benzofurans 5-APB, 5-APDB, 6-APB, 6-APDB, 4-APB, 7-APB, 5-EAPB and ...

journal_title：British journal of pharmacology

authors： Rickli A,Kopf S,Hoener MC,Liechti ME

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Melanocortins reverse circulatory shock and improve survival by counteracting the systemic inflammatory response, and through the activation of the vagus nerve-mediated cholinergic anti-inflammatory pathway. To gain insight into the potential therapeutic value of melanocortins against multiple or...

journal_title：British journal of pharmacology

authors： Bitto A,Polito F,Altavilla D,Irrera N,Giuliani D,Ottani A,Minutoli L,Spaccapelo L,Galantucci M,Lodi R,Guzzo G,Guarini S,Squadrito F

更新日期：2011-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:mTOR inhibitors are currently used as immunosuppressants in transplanted patients and as promising anti-cancer agents. However, new-onset diabetes is a frequent complication occurring in patients treated with mTOR inhibitors such as rapamycin (Sirolimus). Here, we investigated the mechanisms asso...

journal_title：British journal of pharmacology

authors： Deblon N,Bourgoin L,Veyrat-Durebex C,Peyrou M,Vinciguerra M,Caillon A,Maeder C,Fournier M,Montet X,Rohner-Jeanrenaud F,Foti M

更新日期：2012-04-01 00:00:00

abstract：:1. The effects of the putative gap junction uncoupler, 1-heptanol, on the neurogenic and myogenic contractile responses of guinea-pig vas deferens were studied in vitro. 2. Superfusion of 2.0 mM heptanol for 20-30 min produced the following reversible changes in the biphasic neurogenic contractile response (8 trials):...

journal_title：British journal of pharmacology

authors： Venkateswarlu K,Dange SY,Manchanda R

更新日期：1999-01-01 00:00:00

abstract：:Biological nitrogen oxide signalling and stress is an area of extreme clinical, pharmacological, toxicological, biochemical and chemical research interest. The utility of nitric oxide and derived species as signalling agents is due to their novel and vast chemical interactions with a variety of biological targets. Her...

journal_title：British journal of pharmacology

authors： Heinrich TA,da Silva RS,Miranda KM,Switzer CH,Wink DA,Fukuto JM

更新日期：2013-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Positive allosteric modulation of α4β2 nicotinic acetylcholine (nACh) receptors could add a new dimension to the pharmacology and therapeutic approach to these receptors. The novel modulator NS9283 was therefore tested extensively. EXPERIMENTAL APPROACH:Effects of NS9283 were evaluated in vitro ...

journal_title：British journal of pharmacology

authors： Timmermann DB,Sandager-Nielsen K,Dyhring T,Smith M,Jacobsen AM,Nielsen EØ,Grunnet M,Christensen JK,Peters D,Kohlhaas K,Olsen GM,Ahring PK

更新日期：2012-09-01 00:00:00

abstract：:1 The effects of gamma-aminobutyric acid (GABA) and related substances were examined in guinea-pig ileum longitudinal muscle.2 GABA at doses ranging from 10(-7) M to 3 x 10(-6) M elicited a relaxation while at higher doses (3 x 10(-6) M - 10(-4) M), as previously described, it caused a contraction followed by relaxati...

journal_title：British journal of pharmacology

authors： Giotti A,Luzzi S,Spagnesi S,Zilletti L

更新日期：1983-03-01 00:00:00

abstract：:The past two decades have seen an immense increase in our appreciation of the vast range of signalling processes and supporting machinery that occur in cells. Pivotal to this is the notion of signal compartmentalization (compartmentation). Targeting by protein domains is critical in allowing signalling complexes to be...

journal_title：British journal of pharmacology

authors： Houslay MD

更新日期：2009-09-01 00:00:00

abstract：:1. The effects of chronic oral administration of desmethylimipramine (DMI) or zimelidine (1.25 and 5 mg kg-1 twice daily for 21 days) were studied on rat whole cortical gamma-aminobutyric acidB (GABAB) binding sites. No changes in receptor affinity or number were found with either drug. 2. A subsequent study of GABAB ...

journal_title：British journal of pharmacology

authors： Cross JA,Horton RW

更新日期：1988-02-01 00:00:00

abstract：:A new canine model of endotoxin shock has been developed in which spontaneous recovery of cardiovascular function is largely prevented, the haemodynamic effects of anaesthesia are minimized and intravascular volume replacement is given. This model has been evaluated using two groups of five adult mongrel dogs anaesthe...

journal_title：British journal of pharmacology

authors： Evans SF,Hinds CJ,Varley JG

更新日期：1984-10-01 00:00:00