Elevation of cytosolic calcium by imidazolines in mouse islets of Langerhans: implications for stimulus-response coupling of insulin release.

abstract：BACKGROUND AND PURPOSE:Red wine polyphenols (RWPs) inhibit the expression of vascular endothelial growth factor (VEGF), a major pro-angiogenic and pro-atherosclerotic factor, in vascular smooth muscle cells (VSMCs). The aim of this study was to identify which red wine polyphenols were inhibitory and to determine the me...

journal_title：British journal of pharmacology

authors： Oak MH,Bedoui JE,Madeira SV,Chalupsky K,Schini-Kerth VB

更新日期：2006-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:AZ11645373 and N-{2-methyl-5-[(1R, 5S)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-ylcarbonyl]phenyl}-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide hydrochloride (compound-22) are recently described P2X(7) receptor antagonists. In this study we have further characterized these compounds to determine their mecha...

journal_title：British journal of pharmacology

authors： Michel AD,Ng SW,Roman S,Clay WC,Dean DK,Walter DS

更新日期：2009-04-01 00:00:00

abstract：:Effects of isoprenaline (Isop) on the contractile properties of the smooth muscle cells of cat trachea were investigated using intact and chemically skinned muscle preparations and an isometric tension recording method. In the intact muscle preparations, Isop 3 X 10(-10) or 3 X 10(-9) M significantly suppressed the am...

journal_title：British journal of pharmacology

authors： Ito Y,Itoh T

更新日期：1984-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Palmitoylethanolamide (PEA) is an endogenous congener of anandamide and potentiates its actions at cannabinoid CB1 and CB2 receptors, and at transient receptor potential vanilloid type-1 (TRPV1) channels. The other endocannabinoid, 2-arachidonoylglycerol (2-AG), was recently suggested to act as a...

journal_title：British journal of pharmacology

authors： Petrosino S,Schiano Moriello A,Cerrato S,Fusco M,Puigdemont A,De Petrocellis L,Di Marzo V

更新日期：2016-04-01 00:00:00

abstract：:1. The effects of (-)-baclofen, muscimol and phaclofen on endogenous gamma-aminobutyric acid (GABA) release from rat cortical slices, spinal cord slices and entire retinas were studied. 2. The spontaneous resting release of GABA from the three tissues was 3 to 6 pmol mg-1 wet wt 10 min-1. Depolarization of cortical sl...

journal_title：British journal of pharmacology

authors： Neal MJ,Shah MA

更新日期：1989-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Kinins are pro-inflammatory peptides that are released during tissue injury, including that caused by inflammatory bowel disease. Herein, we assessed the role and underlying mechanisms through which the absence of kinin B(1) receptors exacerbates the development of dextran sulfate sodium (DSS)-i...

journal_title：British journal of pharmacology

authors： Marcon R,Claudino RF,Dutra RC,Bento AF,Schmidt EC,Bouzon ZL,Sordi R,Morais RL,Pesquero JB,Calixto JB

更新日期：2013-01-01 00:00:00

abstract：:1. We investigated how microsomal cytochrome P450 mono-oxygenase (Cyp450 MO) is regulated in cultured porcine aortic endothelial cells. The hypothesis that a Cyp450 MO-derived metabolite links Ca2+ store depletion and Ca2+ entry was studied further. 2. Microsomal Cyp450 MO was monitored fluorometrically by dealkylatio...

journal_title：British journal of pharmacology

authors： Hoebel BG,Kostner GM,Graier WF

更新日期：1997-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Anxiety disorder is a common mental health disorder. However, there are few safe and fast-acting anxiolytic drugs available that can treat anxiety disorder. We previously demonstrated that the interaction of neuronal NOS (nNOS) with its carboxy-terminal PDZ ligand (CAPON) is involved in regulatin...

journal_title：British journal of pharmacology

authors： Zhu LJ,Shi HJ,Chang L,Zhang CC,Si M,Li N,Zhu DY

更新日期：2020-08-01 00:00:00

abstract：:Cannabinoid (CB1) receptor activation acts neuronally, reducing GI motility, diarrhoea, pain, transient lower oesophageal sphincter relaxations (TLESRs) and emesis, and promoting eating. CB2 receptor activation acts mostly via immune cells to reduce inflammation. What are the key questions which now need answering to ...

journal_title：British journal of pharmacology

authors： Sanger GJ

更新日期：2007-11-01 00:00:00

abstract：UNLABELLED:Reorganization of the actin cytoskeleton is essential for cell motility and chemotaxis. Actin-binding proteins (ABPs) and membrane lipids, especially phosphoinositides PI(4,5)P2 and PI(3,4,5)P3 are involved in the regulation of this reorganization. At least 15 ABPs have been reported to interact with, or reg...

journal_title：British journal of pharmacology

authors： Wu CY,Lin MW,Wu DC,Huang YB,Huang HT,Chen CL

更新日期：2014-12-01 00:00:00

abstract：:1. The measurement of changes in spike generation and membrane resistance in the guinea-pig taenia coli, using the sucrose gap extracellular recording method, has been shown to be a useful way to demonstrate the intrinsic sympathomimetic activity of the beta adrenoceptor blocking agents.2. Pronethalol, INPEA, MJ 1999,...

journal_title：British journal of pharmacology

authors： Davis WG

更新日期：1970-01-01 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 aim of this study was to assess the role of endothelial cells in the modulation of vasocontractile responses to endothelin-1 (ET-1) of human placental vasculature. 2. Isolated stem villi small arteries (diameter = 170-250 microns) were obtained from healthy parturients who underwent caesarean surgery during the...

journal_title：British journal of pharmacology

authors： Sabry S,Mondon F,Levy M,Ferré F,Dinh-Xuan AT

更新日期：1995-07-01 00:00:00

abstract：:1. 5-Hydroxytryptamine (5-HT) is known to produce a number of different effects in the gastrointestinal tract of various species, and has been proposed to play a key role in a number of intestinal disorders in man, including irritable bowel syndrome (IBS), although the receptors involved have yet to be established. Th...

journal_title：British journal of pharmacology

authors： Borman RA,Tilford NS,Harmer DW,Day N,Ellis ES,Sheldrick RL,Carey J,Coleman RA,Baxter GS

更新日期：2002-03-01 00:00:00

abstract：:1. The purpose of this study was to determine the in vivo inhibitory efficacy of azapropazone on neutrophil migration. The effects of azapropazone given at a dose of 100 mg kg-1 i.v. every 2 h on the neutrophil migration into skin inflammation sites (blister fluid) as well as into an autologous serum (+/- chemoattract...

journal_title：British journal of pharmacology

authors： Mousa SA,Brown R,Chan Y,Hsieh J,Smith RD

更新日期：1990-02-01 00:00:00

abstract：:1. Ca currents in rat and mouse sensory dorsal root ganglion (DRG) neurones were inhibited by concentrations of (-)-baclofen as low as 1 micron. The proportion of neurones responding to baclofen was low (less than 20%), except in young cultures of neonate rat DRG neurones (3 days in culture), where 86% of the neurones...

journal_title：British journal of pharmacology

authors： Green KA,Cottrell GA

更新日期：1988-05-01 00:00:00

abstract：:Pulmonary hypertension (PH) is defined by elevated mean pulmonary artery pressure following the pathological remodelling of small pulmonary arteries. An increase in right ventricular (RV) afterload results in RV hypertrophy and RV failure. The pathophysiology of PH, and RV remodelling in particular, is not well unders...

journal_title：British journal of pharmacology

authors： Maarman GJ,Schulz R,Sliwa K,Schermuly RT,Lecour S

更新日期：2017-04-01 00:00:00

abstract：:1. Muscularis mucosae of the distal oesophagus of the opossum contracts in response to substance P and to a variety of tachykinins. To delineate the nature of the receptors present in this tissue, we evaluated contractile responses to substance P, neurokinin A, neurokinin B, eledoisin and analogues believed to be high...

journal_title：British journal of pharmacology

authors： Daniel EE,Cipris S,Manaka Y,Bowker P,Regoli D

更新日期：1989-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The endocannabinoid, anandamide, has anti-arrhythmic effects. The aim of the present study was to explore the electrophysiological effects of anandamide on rat myocardium. EXPERIMENTAL APPROACH:Evoked action potentials (APs) were recorded using intracellular recording technique in rat cardiac pa...

journal_title：British journal of pharmacology

authors： Li Q,Ma HJ,Zhang H,Qi Z,Guan Y,Zhang Y

更新日期：2009-12-01 00:00:00

abstract：:The effects of the alpha- and beta-isomers of flupenthixol on 5-hydroxytryptamine (5-HT)-induced platelet aggregation and on 5-HT and dopamine uptake were investigated. Alpha-Flupenthixol was 185 times more potent than the beta-isomer as an inhibitor of platelet aggregation. In contrast both isomers were equipotent a...

journal_title：British journal of pharmacology

authors： Boullin DJ,Grimes RP,Orr MW

更新日期：1975-12-01 00:00:00

abstract：:1. The alpha 1-adrenoceptor subtypes mediating contractions of the smooth muscle in human prostatic urethra and branches of internal iliac artery were characterized in isometric contraction experiments. 2. Phenylephrine produced concentration-dependent contractions in both the urethra and artery. These responses were ...

journal_title：British journal of pharmacology

authors： Hatano A,Takahashi H,Tamaki M,Komeyama T,Koizumi T,Takeda M

更新日期：1994-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Down's syndrome is a common genetic cause of intellectual disability, for which there are no drug therapies. Mechanistic studies in a model of Down's syndrome [Ts65Dn (TS) mice] demonstrated that impaired cognitive function was due to excessive neuronal inhibitory tone. These deficits were normal...

journal_title：British journal of pharmacology

authors： Colas D,Chuluun B,Warrier D,Blank M,Wetmore DZ,Buckmaster P,Garner CC,Heller HC

更新日期：2013-07-01 00:00:00

abstract：:1. The regulation of adenosine 3':5'-cyclic monophosphate (cyclic AMP) levels by cholinoceptors has been studied in cultured bovine adrenal medullary cells. 2. Acetylcholine (100 microM), nicotine (10 microM) and dimethylphenylpiperazinium (20 microM) each increased cellular cyclic AMP levels 2 to 4 fold over 5 min in...

journal_title：British journal of pharmacology

authors： Anderson K,Robinson PJ,Marley PD

更新日期：1992-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cytochrome P450 (CYP, P450) 3A4 is involved in the metabolism of 50% of drugs and its catalytic activity in vivo is not explained only by hepatic expression levels. We previously demonstrated that UDP-glucuronosyltransferase (UGT) 2B7 suppressed CYP3A4 activity through an interaction. In the pres...

journal_title：British journal of pharmacology

authors： Miyauchi Y,Tanaka Y,Nagata K,Yamazoe Y,Mackenzie PI,Yamada H,Ishii Y

更新日期：2020-03-01 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:Inhibitory neurotransmission plays an important role in controlling excitability within nociceptive circuits of the spinal cord dorsal horn. Loss of inhibitory signalling is thought to contribute to the development of pathological pain. Preclinical studies suggest that increasing inhibitory glyci...

journal_title：British journal of pharmacology

authors： Winters BL,Rawling T,Vandenberg RJ,Christie MJ,Bhola RF,Imlach WL

更新日期：2018-06-01 00:00:00

abstract：:1. Adenosine A(1), A(2A), and A(3) receptors (ARs) and extracellular signal-regulated kinase 1/2 (ERK1/2) play a major role in myocardium protection from ischaemic injury. In this study, we have characterized the adenosine receptor subtypes involved in ERK1/2 activation in newborn rat cardiomyocytes. 2. Adenosine (non...

journal_title：British journal of pharmacology

authors： Germack R,Dickenson JM

更新日期：2004-01-01 00:00:00

abstract：:1 The appearance of pancreatic muscarinic receptors during development has been measured by use of the specific ligand [3H]-quinuclidinyl benzilate ([3H]-QNB). 2 QNB binding sites are present in foetal pancreas; their maximal concentration is attained at the age of 30 days and a significant decrease is observed in one...

journal_title：British journal of pharmacology

authors： Dumont Y,Larose L,Morisset J,Poirier GG

更新日期：1981-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The non-nucleoside analogue reverse transcriptase inhibitor efavirenz is associated with hepatic toxicity and metabolic disturbances. Although the mechanisms involved are not clear, recent evidence has pinpointed a specific mitochondrial action of efavirenz accompanied by the induction of an endo...

journal_title：British journal of pharmacology

authors： Polo M,Alegre F,Funes HA,Blas-Garcia A,Victor VM,Esplugues JV,Apostolova N

更新日期：2015-04-01 00:00:00

abstract：:1 Dose-related increases in airways resistance (Raw) and decreases in dynamic lung compliance (Cdyn) were recorded in guinea-pigs and rats following intravenous injection of propranolol and of the cardioselective beta-adrenoceptor blocking drugs, atenolol and practolol. 2 The bronchoconstriction reached a peak in 2 to...

journal_title：British journal of pharmacology

authors： Maclagan J,Ney UM

更新日期：1979-07-01 00:00:00