Effects of the kinase inhibitor sorafenib on heart, muscle, liver and plasma metabolism in vivo using non-targeted metabolomics analysis.

abstract：:1 Neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) differentially activate three Y receptors (Y(1), Y(2) and Y(4)) in mouse and human isolated colon. 2 The aim of this study was to characterise Y(2) receptor-mediated responses in colon mucosa and longitudinal smooth muscle preparations from wild ...

journal_title：British journal of pharmacology

authors： Hyland NP,Sjöberg F,Tough IR,Herzog H,Cox HM

更新日期：2003-06-01 00:00:00

abstract：:1 The butyrophenone tranquilizer, azaperone, was administered intramuscularly, at dose levels of 0.4 and 0.8 mg/kg, to ponies and its effects on cardiovascular and respiratory functions assessed. 2 Arterial blood pH, CO2 tension (PaCO2) and O2 tension (PaO2) remained relatively constant throughout the course of action...

journal_title：British journal of pharmacology

authors： Lees P,Serrano L

更新日期：1976-03-01 00:00:00

abstract：:1. The effect of mastoparan on phosphatidylcholine hydrolysis was examined in 1321N1 human astrocytoma cells. Mastoparan (3-30 microM) caused an accumulation of diacylglycerol (DG) and phosphatidic acd (PA) accompanied by choline release in a concentration- and time-dependent manner. 2. In the presence of 2% n-butanol...

journal_title：British journal of pharmacology

authors： Mizuno K,Nakahata N,Ohizumi Y

更新日期：1995-10-01 00:00:00

abstract：:Rat vas deferens preparations became desensitized to the alpha 1-adrenoceptor antagonist thymoxamine: after 6 h in vitro, the t 1/2 value (time to attain half the occupancy of receptors occupied at equilibrium) of the response to this drug was 1.50 fold greater in control strips (strips exposed to thymoxamine at 6 h) ...

journal_title：British journal of pharmacology

authors： Onnen I

更新日期：1984-09-01 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：:Spontaneous inhibitory postsynaptic currents (i.p.s.cs) were recorded in voltage-clamped CA1 neurones in rat hippocampal slices. The exponential decay of i.p.s.cs was prolonged by concentrations of sodium pentobarbitone as low as 50 microM. With concentrations up to 100 microM, there was no change in the amplitude or ...

journal_title：British journal of pharmacology

authors： Gage PW,Robertson B

更新日期：1985-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic hepatic fatty liver disease (NAFLD) is a manifestation of the metabolic syndrome in the liver and non-alcoholic steatohepatitis (NASH) represents its advanced stage. R17 derived from bouchardatine, shows benefits in the metabolic syndrome, but has not been tested in the liver. The p...

journal_title：British journal of pharmacology

authors： Rao Y,Lu YT,Li C,Song QQ,Xu YH,Xu Z,Hu YT,Yu H,Gao L,Gu LQ,Ye JM,Huang ZS

更新日期：2019-08-01 00:00:00

abstract：:1. We have investigated the inhibitory effects of RP 73401 (piclamilast) and rolipram against human monocyte cyclic AMP-specific phosphodiesterase (PDE4) in relation to their effects on prostaglandin (PG)E2-induced cyclic AMP accumulation and lipopolysaccharide (LPS)-induced TNF alpha production and TNF alpha mRNA exp...

journal_title：British journal of pharmacology

authors： Souness JE,Griffin M,Maslen C,Ebsworth K,Scott LC,Pollock K,Palfreyman MN,Karlsson JA

更新日期：1996-06-01 00:00:00

abstract：:Liver X receptors (LXRs) are members of the nuclear receptor superfamily that are canonically activated by oxidized derivatives of cholesterol. Since the mid-90s, numerous groups have identified LXRs as endocrine receptors that are involved in the regulation of various physiological functions. As a result, when their ...

journal_title：British journal of pharmacology

authors： Buñay J,Fouache A,Trousson A,de Joussineau C,Bouchareb E,Zhu Z,Kocer A,Morel L,Baron S,Lobaccaro JA

更新日期：2020-10-20 00:00:00

abstract：BACKGROUND AND PURPOSE:Chemokines and their receptors form an intricate interaction and signalling network that plays critical roles in various physiological and pathological cellular processes. The high promiscuity and apparent redundancy of this network makes probing individual chemokine/receptor interactions and fun...

journal_title：British journal of pharmacology

authors： Szpakowska M,Nevins AM,Meyrath M,Rhainds D,D'huys T,Guité-Vinet F,Dupuis N,Gauthier PA,Counson M,Kleist A,St-Onge G,Hanson J,Schols D,Volkman BF,Heveker N,Chevigné A

更新日期：2018-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gut microbiota plays an important role in type 2 diabetes mellitus (T2DM) progression. From our previous work N-(4-Hydroxyphenethyl)-3-mercapto-2-methylpropanamide (HMPA) is a potential T2DM drug. We evaluated the effect of HMPA on gut microbiota and studied the molecular mechanism underlying HMP...

journal_title：British journal of pharmacology

authors： Liu H,Qin Y,Li K,Li M,Yang J,Tao H,Tang Y,Yang L,Chen S,Liu Y,Yang C,Gao W,Sun T

更新日期：2020-12-07 00:00:00

abstract：:1. Adenosine has been shown to be responsible for the hyperaemic response of the hepatic artery to portal vein occlusion (the hepatic arterial 'buffer response'). 2. The effect of adenosine receptor blockade and of adenosine uptake inhibition on the hepatic arterial response to portal vein occlusion was investigated i...

journal_title：British journal of pharmacology

authors： Mathie RT,Alexander B

更新日期：1990-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Allosteric modulators of ionotropic receptors and GPCRs might constitute valuable therapeutic tools for intervention in several diseases, including Parkinson's disease (PD). However, the possibility that some of these compounds could alter neurotransmission in health and disease has not been thor...

journal_title：British journal of pharmacology

authors： Zhang X,Feng ZJ,Chergui K

更新日期：2014-08-01 00:00:00

abstract：:1. The systemic and regional haemodynamic effects of the potassium channel activator EMD 52692 or its solvent were investigated after intravenous and after intracoronary administration in anaesthetized pigs. 2. Consecutive intravenous 10 min infusions of EMD 52692 (0.15, 0.30, 0.60, 1.20 micrograms kg-1 min-1; n = 7) ...

journal_title：British journal of pharmacology

authors： Sassen LM,Duncker DJ,Gho BC,Diekmann HW,Verdouw PD

更新日期：1990-11-01 00:00:00

abstract：:1. In human epithelial-like DLD-I cells, nitric oxide synthase (NOS) II expression was induced by interferon-gamma (100 u ml(-1)) alone and, to a larger extent, by a cytokine mixture (CM) consisting of interferon-gamma, interleukin-1beta (50 u ml(-1)) and tumor necrosis factor-alpha (10 ng ml(-1)). 2. CM-induced NOS I...

journal_title：British journal of pharmacology

authors： Kleinert H,Wallerath T,Fritz G,Ihrig-Biedert I,Rodriguez-Pascual F,Geller DA,Förstermann U

更新日期：1998-09-01 00:00:00

abstract：:1. The ratio of the content of vasopressin to that of oxytocin (V/O ratio) was estimated in the supraoptic nucleus (SON), paraventricular nucleus (PVN) and posterior pituitary gland (PIT) of guinea-pigs.2. Extracts were assayed for antidiuretic activity to estimate vasopressin and for milk-ejecting activity to estimat...

journal_title：British journal of pharmacology

authors： Bisset GW,Errington ML,Richards CD

更新日期：1973-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An influx drug/proton antiporter of unknown structure has been functionally demonstrated at the blood-brain barrier. This transporter, which handles some psychoactive drugs like diphenhydramine, clonidine, oxycodone, nicotine and cocaine, could represent a new pharmacological target in drug addic...

journal_title：British journal of pharmacology

authors： Chapy H,Goracci L,Vayer P,Parmentier Y,Carrupt PA,Declèves X,Scherrmann JM,Cisternino S,Cruciani G

更新日期：2015-10-01 00:00:00

abstract：:In this study, the mechanism of nicotine-induced hippocampal acetylcholine (ACh) release in awake, freely moving rats was examined using in vivo microdialysis. Systemic administration of nicotine (0.4 mg kg(-1), s.c.) increased the levels of ACh in hippocampal dialysates. The nicotine-induced hippocampal ACh release w...

journal_title：British journal of pharmacology

authors： Reid RT,Lloyd GK,Rao TS

更新日期：1999-07-01 00:00:00

abstract：AIMS:The trace amine-associated receptor (Taar) family displays high species- and subtype-specific pharmacology. Several trace amines such as β-phenylethylamine (β-PEA), p-tyramine and tryptamine are agonists at TA(1) but poorly activate rat and mouse Taar4. PRINCIPAL RESULTS:Using rat TA(1) and Taar4 chimera, we id...

journal_title：British journal of pharmacology

authors： Stäubert C,Bohnekamp J,Schöneberg T

更新日期：2013-03-01 00:00:00

abstract：:1. The effects of seven agonist and three antagonist adenosine receptor ligands were compared on the guinea-pig sinoatrial (SA) node (isolated right atrium) and atrioventricular (AV) node (perfused whole heart). Single agonist concentration-effect curves were obtained to 5'-N-ethylcarboxamidoadenosine (NECA), R(-)-N6-...

journal_title：British journal of pharmacology

authors： Meester BJ,Shankley NP,Welsh NJ,Wood J,Meijler FL,Black JW

更新日期：1998-06-01 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：BACKGROUND AND PURPOSE:The cannabinoid receptor-mediated analgesic effects of 2-arachidonoylglycerol (2-AG) are limited by monoacylglycerol lipase (MAGL). 4-nitrophenyl 4-[bis (1,3-benzodioxol-5-yl) (hydroxy) methyl] piperidine-1-carboxylate (JZL184) is a potent inhibitor of MAGL in the mouse, though potency is reporte...

journal_title：British journal of pharmacology

authors： Woodhams SG,Wong A,Barrett DA,Bennett AJ,Chapman V,Alexander SP

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary arterial hypertension (PAH, type 1 pulmonary hypertension) has a 3-year survival of ~50% and is in need of new, effective therapies. In PAH, remodelling of the pulmonary artery (PA) increases pulmonary vascular resistance and can result in right heart dysfunction and failure. Genetic mu...

journal_title：British journal of pharmacology

authors： Gorr MW,Sriram K,Muthusamy A,Insel PA

更新日期：2020-08-01 00:00:00

abstract：:Chronic heart failure (HF) is characterized by left ventricular (LV) structural remodeling, impaired function, increased circulating noradrenaline (NA) levels and impaired responsiveness of the myocardial beta-adrenoceptor (betaAR)-adenylyl cyclase (AC) system. In failing hearts, inhibition of the sodium/proton-exchan...

journal_title：British journal of pharmacology

authors： Leineweber K,Aker S,Beilfuss A,Rekasi H,Konietzka I,Martin C,Heusch G,Schulz R

更新日期：2006-05-01 00:00:00

abstract：:C-C chemokine receptor-1 (CCR1) has been implicated in mediating a variety of inflammatory conditions including multiple sclerosis and organ rejection. Although originally referred to as the MIP-1alpha/RANTES receptor, CCR1 is quite promiscuous and can be activated by numerous chemokines. We used radioligand binding a...

journal_title：British journal of pharmacology

authors： Chou CC,Fine JS,Pugliese-Sivo C,Gonsiorek W,Davies L,Deno G,Petro M,Schwarz M,Zavodny PJ,Hipkin RW

更新日期：2002-11-01 00:00:00

abstract：:1. The role of smooth muscle-derived lipoprotein lipase (LPL) that translocates to the endothelium surface on vascular dysfunction during atherogenesis is unclear. Thus, the role of vascular LPL on blood vessel reactivity was assessed in transgenic mice that specifically express human LPL in the circulatory system. 2....

journal_title：British journal of pharmacology

authors： Esenabhalu VE,Cerimagic M,Malli R,Osibow K,Levak-Frank S,Frieden M,Sattler W,Kostner GM,Zechner R,Graier WF

更新日期：2002-01-01 00:00:00

abstract：:1. The vasodilator responses of isolated intrapulmonary arteries (IPA) to P2-receptor agonists were investigated during adaptation to extrauterine life in the piglet. The effect of pulmonary hypertension on the normal response was determined after exposing newborn animals to chronic hypobaric hypoxia (51 kPa) for 3 da...

journal_title：British journal of pharmacology

authors： McMillan MR,Burnstock G,Haworth SG

更新日期：1999-10-01 00:00:00

abstract：:1. Opioid agonists inhibit neurogenic mucus secretion in the airways. The mechanism of the inhibition is unknown but may be via opening of potassium (K+) channels. We studied the effect on neurogenic secretion in ferret trachea in vitro of the OP1 receptor (formerly known as delta opioid receptor) agonist [D-Pen2,5]en...

journal_title：British journal of pharmacology

authors： Ramnarine SI,Liu YC,Rogers DF

更新日期：1998-04-01 00:00:00

abstract：:1. The effects of the lipoxygenase inhibitor nordihydroguaiaretic acid (NDGA) on the ionic currents of rat carotid body type I cells were investigated by use of whole-cell and outside-out patch clamp techniques. 2. NDGA (5-50 microM) produced a concentration-dependent inhibition of whole-cell K+ currents at all activa...

journal_title：British journal of pharmacology

authors： Hatton CJ,Peers C

更新日期：1997-11-01 00:00:00

abstract：:1 Rat isolated perfused hearts with the right sympathetic nerves attached were loaded with [3H]-(-)-noradrenaline. The nerves were stimulated with up to 40 trains of 10 pulses every min at 1 Hz, and the evoked increases of [3H-]noradrenaline overflow into the perfusate, of right atrial tension development and ventricu...

journal_title：British journal of pharmacology

authors： Fuder H,Muscholl E,Spemann R

更新日期：1983-05-01 00:00:00