Mechanism of anti-inflammatory action of glucocorticoids: re-evaluation of vascular constriction hypothesis.

abstract：:The effects of the opioid receptor agonist RX783006 and of the opioid receptor partial agonist (+)-meptazinol have been examined on electrically induced twitch responses of the guinea-pig isolated ileum and of the mouse isolated vas deferens. Log10 concentration-tissue state curves were determined for (+)-meptazinol a...

journal_title：British journal of pharmacology

authors： Goodall J,Hughes IE,Mackay D

更新日期：1986-07-01 00:00:00

abstract：:1. Sodium nitroprusside, S-nitroso-N-acetyl-D,L-penicillamine, Spermine NONOate and DEA NONOate raised cyclic GMP levels in bovine chromaffin cells in a time and concentration dependent manner with different potencies, the most potent being DEA/NO with an EC50 value of 0.38 +/- 0.02 microM. 2. Measurements of NO relea...

journal_title：British journal of pharmacology

authors： Ferrero R,Rodríguez-Pascual F,Miras-Portugal MT,Torres M

更新日期：1999-06-01 00:00:00

abstract：:1. An investigation was carried out to determine if the sympathoinhibition caused by urapidil is due to activation of 5-HT1A receptors by investigating whether it could be reversed by the non-selective 5-HT1A receptor antagonist spiperone. To control for the possibility of functional antagonism by spiperone, the abili...

journal_title：British journal of pharmacology

authors： Ramage AG

更新日期：1991-04-01 00:00:00

abstract：:1 We investigated the neuritogenic action of nitric oxide (NO)-generating agents and their mechanisms of action in a subclone of rat pheochromocytoma, PC12h cells. 2 NO donors such as sodium nitroprusside (SNP, 0.05-1 microM), NOR1 (5-100 microM), NOR2 (5-20 microM), NOR3 (5-20 microM), NOR4 (5-100 microM), or S-nitro...

journal_title：British journal of pharmacology

authors： Yamazaki M,Chiba K,Mohri T

更新日期：2005-11-01 00:00:00

abstract：:Since protease-activated receptors (PARs) are distributed throughout the gastrointestinal tract, we investigated the role of PARs in modulation of the motility of the rat oesophageal muscularis mucosae. Thrombin produced contraction of segments of the upper and lower part of the smooth muscle. Trypsin contracted both ...

journal_title：British journal of pharmacology

authors： Kawabata A,Kuroda R,Kuroki N,Nishikawa H,Kawai K

更新日期：2000-10-01 00:00:00

abstract：:1. In this study, we investigated the effects of different drugs (a kappa-opioid receptor agonist U-50,488, a vasopressin receptor antagonist dPTyr(Me)AVP or an N-methyl-D-aspartate (NMDA) receptor antagonist MK-801) on the development of morphine tolerance in rat hippocampal slices. 2. Hippocampal slices (450 microm)...

journal_title：British journal of pharmacology

authors： Su MT,Lin WB,Lue WM,Cheng CY,Tao PL

更新日期：1998-02-01 00:00:00

abstract：:Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. In this study, the effects of TAK-147 at 2 mg kg(-1) p.o. for 21 days, compared t...

journal_title：British journal of pharmacology

authors： Hatip-Al-Khatib I,Iwasaki K,Yoshimitsu Y,Arai T,Egashira N,Mishima K,Ikeda T,Fujiwara M

更新日期：2005-08-01 00:00:00

abstract：:1. Cumulative concentration-response curves (CRC) to prostaglandin E1 (PGE1), PGE2, PGD2 and PGF2alpha (0.01-30 microM) and to the thromboxane A2 (TXA2) receptor agonist U-46619 (0.01-30 microM) were constructed in human isolated detrusor muscle strips both in basal conditions and during electrical field stimulation. ...

journal_title：British journal of pharmacology

authors： Palea S,Toson G,Pietra C,Trist DG,Artibani W,Romano O,Corsi M

更新日期：1998-07-01 00:00:00

abstract：:The electrically-evoked contractions of the rat vas deferens were selectively inhibited by beta-endorphin, the preparation being much less sensitive to enkephalins and narcotic analgesic drugs. However, introduction of D-Ala in position 2 of [Leu]-enkephalin enhanced the activity of the opioid peptide to the order of ...

journal_title：British journal of pharmacology

authors： Lemaire S,Magnan J,Regoli D

更新日期：1978-11-01 00:00:00

abstract：:1. Treatment of rat mesangial cells with interleukin 1 beta (IL-1 beta) or tumour necrosis factor alpha (TNF alpha) has been shown to induce a macrophage-type of nitric oxide (NO) synthase. Here we report that adenosine 3':5'-cyclic monophosphate (cyclic AMP) is another mediator that triggers induction of NO synthase ...

journal_title：British journal of pharmacology

authors： Mühl H,Kunz D,Pfeilschifter J

更新日期：1994-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The type-5 PDE inhibitor vardenafil reduces myocardial infarct size in situ, following ischemia/reperfusion, when applied at reperfusion in animal models. Little is known about the underlying protective signaling. Here, we test whether vardenafil is protective in rat isolated hearts and in a cell...

journal_title：British journal of pharmacology

authors： Maas O,Donat U,Frenzel M,Rütz T,Kroemer HK,Felix SB,Krieg T

更新日期：2008-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Two of the most relevant unmet needs in epilepsy are represented by the development of disease-modifying drugs able to affect epileptogenesis and/or the study of related neuropsychiatric comorbidities. No systematic study has investigated the effects of chronic treatment with antipsychotics or an...

journal_title：British journal of pharmacology

authors： Citraro R,Leo A,De Fazio P,De Sarro G,Russo E

更新日期：2015-06-01 00:00:00

abstract：:The arterial endothelium critically contributes to blood pressure control by releasing vasodilating autacoids such as nitric oxide, prostacyclin and a third factor or pathway termed 'endothelium-derived hyperpolarizing factor' (EDHF). The nature of EDHF and EDHF-signalling pathways is not fully understood yet. However...

journal_title：British journal of pharmacology

authors： Grgic I,Kaistha BP,Hoyer J,Köhler R

更新日期：2009-06-01 00:00:00

abstract：:1. Conscious, Long Evans rats (n = 10), chronically instrumented for the measurement of regional haemodynamics, were studied on 3 consecutive experimental days to assess responses to angiotensin II (AII) (125 pmol kg-1, i.v.) and noradrenaline (1 nmol kg-1, i.v.) in the absence and presence of the AT2-receptor antagon...

journal_title：British journal of pharmacology

authors： Widdop RE,Gardiner SM,Kemp PA,Bennett T

更新日期：1992-11-01 00:00:00

abstract：:1. Protein phosphorylation is involved in the induction of nitric oxide synthase II (NOS II, iNOS) in several types of animal cells. Here we have investigated the possible involvement of major protein kinases in the induction of NOS II expression in human DLD-1 cells. 2. In DLD-1 cells, interferon--gamma alone induced...

journal_title：British journal of pharmacology

authors： Kleinert H,Euchenhofer C,Fritz G,Ihrig-Biedert I,Förstermann U

更新日期：1998-04-01 00:00:00

abstract：:1. The effects of ryanodine on changes in cytoplasmic Ca2+ level ([Ca2+]i) and muscle tension induced by maximum concentrations of phenylephrine (Phe; 1 microM), prostaglandin F2 alpha (PGF2 alpha, 10 microM), caffeine (Caf, 30 mM) and isoprenaline (Iso, 1 microM) were examined in rat aortic strips using fura-2. 2. In...

journal_title：British journal of pharmacology

authors： Hisayama T,Takayanagi I,Okamoto Y

更新日期：1990-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Glucocorticoids appear to control Na⁺ absorption in pulmonary epithelial cells via a mechanism dependent upon serum and glucocorticoid-inducible kinase 1 (SGK1), a kinase that allows control over the surface abundance of epithelial Na⁺ channel subunits (α-, β- and γ-ENaC). However, not all data s...

journal_title：British journal of pharmacology

authors： Watt GB,Ismail NA,Caballero AG,Land SC,Wilson SM

更新日期：2012-06-01 00:00:00

abstract：:The endogenous cannabinoid system is involved in numerous physiological and neuropsychological functions. Medications that target this system hold promise for the treatment of a wide variety of disorders. However, as reward is one of the most prominent of these functions, medications that activate this system must be ...

journal_title：British journal of pharmacology

authors： Panlilio LV,Justinova Z,Goldberg SR

更新日期：2010-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sepsis is a systemic inflammatory response accompanied by excessive production of inflammatory cytokines and cardiovascular dysfunction. Importantly, macrophage-derived pro-inflammatory agents play a key role in cardiovascular impairment in sepsis. Here we have investigated the effects of trimeta...

journal_title：British journal of pharmacology

authors： Chen J,Lai J,Yang L,Ruan G,Chaugai S,Ning Q,Chen C,Wang DW

更新日期：2016-02-01 00:00:00

abstract：:1. A series of GABAB receptor antagonists were tested against (+/-)-baclofen for activity on the presynaptic GABAB receptor in the rat vas deferens. 2. All the antagonists tested caused a rightward shift in the concentration-response curve to (+/-)-baclofen. 3. pA2 values calculated from full Schild analysis were as f...

journal_title：British journal of pharmacology

authors： Hills JM,Larkin MM,Howson W

更新日期：1991-03-01 00:00:00

abstract：:1. We investigated the mechanism of action of two novel nonsulphonylurea ATP-sensitive potassium channel (K(ATP)) inhibitors, PNU-99963 and PNU-37883A, on four types of cloned K(ATP) channels. 2. Whole-cell currents were recorded in a symmetrical potassium (140 mM) gradient in HEK-293 cells stably expressing Kir6.2/SU...

journal_title：British journal of pharmacology

authors： Cui Y,Tinker A,Clapp LH

更新日期：2003-05-01 00:00:00

abstract：:1 Thermic oedema induced by heating rat paws at 46.5 degrees C was potentiated by local injection of adrenaline, noradrenaline or high doses of isoprenaline. The pro-inflammatory effect of sympathomimetic amines was antagonized by phenoxybenzamine or phentolamine but not by propranolol.2 The subcutaneous space of heat...

journal_title：British journal of pharmacology

authors： Green KL

更新日期：1974-02-01 00:00:00

abstract：:1. Imidazoline binding sites have been reported to be present in the locus coeruleus (LC). To investigate the role of these sites in the control of LC neuron activity, we studied the effect of imidazolines using in vivo and in vitro single-unit extracellular recording techniques. 2. In anaesthetized rats, local (27 pm...

journal_title：British journal of pharmacology

authors： Ugedo L,Pineda J,Ruiz-Ortega JA,Martín-Ruiz R

更新日期：1998-12-01 00:00:00

abstract：:1. We examined the effect of the sulphonylurea glimepiride on three types of recombinant ATP-sensitive potassium (K(ATP)) channels. 2. K(ATP) channels share a common pore-forming subunit, Kir6.2, which associates with different sulphonylurea receptor isoforms (SUR1 in beta-cells, SUR2A in heart and SUR2B in smooth mus...

journal_title：British journal of pharmacology

authors： Song DK,Ashcroft FM

更新日期：2001-05-01 00:00:00

abstract：:1. The regional binding of [3H]-(+)-5-methyl-10,11-dihydro-5H-dibenzo (a,d)cyclohepten-5,10-imine maleate ([3H]-(+)-MK 801) to sections of rat brain was measured by an in vitro quantitative autoradiographic technique. A heterogeneous distribution of binding sites was observed. 2. High values of binding were detected i...

journal_title：British journal of pharmacology

authors： Tacconi S,Ratti E,Marien MR,Gaviraghi G,Bowery NG

更新日期：1993-03-01 00:00:00

abstract：:1 Salbutamol and disodium cromoglycate were compared for anti-anaphylactic activity against passive anaphylaxis in rat skin and peritoneum in vivo and in rat mast cells and human lung fragments in vitro.2 Salbutamol administered intravenously to rats inhibited cutaneous anaphylaxis, but also inhibited cutaneous respon...

journal_title：British journal of pharmacology

authors： Butchers PR,Fullarton JR,Skidmore IF,Thompson LE,Vardey CJ,Wheeldon A

更新日期：1979-09-01 00:00:00

abstract：:The binding of [3H]-iloprost (ZK36374) to NCB-20 membranes revealed a single population of high affinity receptors (KD = 9.55 nM, Bmax = 431 fmol mg-1 protein) and a low affinity, non-saturable binding component. Desensitization of prostacyclin-responsiveness of NCB-20 cells is induced by culture in the presence of th...

journal_title：British journal of pharmacology

authors： Leigh PJ,MacDermot J

更新日期：1985-05-01 00:00:00

abstract：:Fresh human erythrocytes were washed and incubated at 37 degrees C in physiological saline buffered with Tris, containing calcium and either neuraminidase or trypsin or both enzymes together. Each enzyme alone, as well as both together, released similar amounts of sialic acids without haemolysis, apparently therefore ...

journal_title：British journal of pharmacology

authors： Born GV,Housley GM

更新日期：1983-06-01 00:00:00

abstract：:Cyclic adenosine monophosphate (cAMP) is one of the second messengers critically involved in the molecular mechanisms underlying memory formation. In the CNS, the availability of cAMP is tightly controlled by phosphodiesterase 4 (PDE4), a family of enzymes that degrades the cyclic nucleotide to inactive AMP. Among the...

journal_title：British journal of pharmacology

authors： Ricciarelli R,Fedele E

更新日期：2015-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Normal pregnancy is associated with decreased vascular resistance and increased release of vasodilators. Endothelin-1 (ET-1) causes vasoconstriction via endothelin receptor type A (ET(A)R), but could activate ET(B)R in the endothelium and release vasodilator substances. However, the roles of ET(B...

journal_title：British journal of pharmacology

authors： Mazzuca MQ,Dang Y,Khalil RA

更新日期：2013-07-01 00:00:00