Drug displacement from protein binding: isolation of a redistributional drug interaction in vivo.

abstract：:1 The concept that presynaptic receptors regulate noradrenergic transmitter release via a system of inhibitory receptors mediating negative feedback relies on a supposed association between increases in stimulation-induced efflux of [3H]-noradrenaline by antagonists and blockade by them of the inhibitory effects of ex...

journal_title：British journal of pharmacology

authors： Kalsner S

更新日期：1982-10-01 00:00:00

abstract：:Noradrenaline (NA) and adrenaline (Ad) are modulators of cytokine production. Here we investigated the role of these neurotransmitters in the regulation of macrophage inflammatory protein (MIP)-1alpha expression. Pretreatment of RAW 264.7 macrophages with NA or Ad decreased, in a concentration-dependent manner (1 nM-1...

journal_title：British journal of pharmacology

authors： Haskó G,Shanley TP,Egnaczyk G,Németh ZH,Salzman AL,Vizi ES,Szabó C

更新日期：1998-11-01 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

abstract：BACKGROUND AND PURPOSE:The increased proliferation and migration of vascular smooth muscle cells (VSMCs) after arterial injury contributes greatly to the pathogenesis of neointimal hyperplasia. As a major component of epigenetics, histone methylation plays an important role in several cardiovascular diseases. However, ...

journal_title：British journal of pharmacology

authors： Liang J,Li Q,Cai W,Zhang X,Yang B,Li X,Jiang S,Tian S,Zhang K,Song H,Ai D,Zhang X,Wang C,Zhu Y

更新日期：2019-09-01 00:00:00

abstract：:Synaptic transmission in the isolated olfactory cortex slice from the rat was monitored by recording the surface field potentials evoked on lateral olfactory tract (LOT) stimulation. Catechol (approximately 0.05 to 2 mM) caused a concentration-dependent, partially reversible increase in the amplitudes of all field pot...

journal_title：British journal of pharmacology

authors： Collins GG,Dewhurst DG

更新日期：1986-06-01 00:00:00

abstract：:1. The specificity of several ganglion stimulants has been tested on the isolated guinea-pig ileum by measuring the dose ratios produced by concentrations of hexamethonium.2. Most ganglion stimulants are also active at postganglionic receptors, some as blocking agents (for example, lobeline and dimethylphenylpiperazin...

journal_title：British journal of pharmacology

authors： Barlow RB,Franks F

更新日期：1971-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Ca(2+)-dependent Cl(-) secretion (CaCC) in airways and other tissues is due to activation of the Cl(-) channel TMEM16A (anoctamin 1). Earlier studies suggested that Ca(2+) -activated Cl(-) channels are regulated by membrane lipid inositol phosphates, and that 1-O-octyl-2-O-butyryl-myo-inositol 3,...

journal_title：British journal of pharmacology

authors： Tian Y,Schreiber R,Wanitchakool P,Kongsuphol P,Sousa M,Uliyakina I,Palma M,Faria D,Traynor-Kaplan AE,Fragata JI,Amaral MD,Kunzelmann K

更新日期：2013-01-01 00:00:00

abstract：:1. Pharmacological inhibitors of protein kinase A (PKA) and protein phosphatases 1/2A were used to determine whether basal L-type Ca(2+) current (I(Ca)) observed in the absence of exogenous beta-adrenergic receptor stimulation is sustained by PKA-mediated phosphorylation. Amphotericin B was used to record whole-cell I...

journal_title：British journal of pharmacology

authors： Bracken N,Elkadri M,Hart G,Hussain M

更新日期：2006-08-01 00:00:00

abstract：:1. 1-3(Chlorophenyl)piperazine (mCPP) (5 mg kg-1, i.p.) inhibited 2 h food intake in rats previously deprived of food for one day. Ten 5-hydroxytryptamine (5-HT) antagonists given s.c. opposed this hypophagic response. Calculated ID50 values correlated significantly with reported affinities (r = 0.81, n = 10, P less t...

journal_title：British journal of pharmacology

authors： Kennett GA,Curzon G

更新日期：1991-08-01 00:00:00

abstract：:1. The actions of etorphine, morphine and diprenorphine were investigated on neurones of the cerebral cortex and spinal cord of rats anaesthetized with pentobarbitone.2. In the cerebral cortex, intravenous etorphine increased the latency of the primary evoked response to a peripheral nerve stimulus and suppressed the ...

journal_title：British journal of pharmacology

authors： Biscoe TJ,Duggan AW,Lodge D

更新日期：1972-10-01 00:00:00

abstract：:Midbrain dopaminergic (DA) neurones sustain important physiological functions such as control of motricity, signalling of the error in prediction of rewards and modulation of emotions and cognition. Moreover, their degeneration leads to Parkinson's disease and they may be dysfunctional in other pathological states, su...

journal_title：British journal of pharmacology

authors： Seutin V

更新日期：2005-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Depolarization-induced suppression of inhibition (DSI) and excitation (DSE) are two forms of cannabinoid CB(1) receptor-mediated inhibition of synaptic transmission, whose durations are regulated by endocannabinoid (eCB) degradation. We have recently shown that in cultured hippocampal neurons mon...

journal_title：British journal of pharmacology

authors： Straiker A,Wager-Miller J,Hu SS,Blankman JL,Cravatt BF,Mackie K

更新日期：2011-11-01 00:00:00

abstract：:1 Morphine-theophylline interactions were investigated in both acute and narcotic-dependent preparations, in vitro and in vivo, using four different experimental models: LD50 doses of morphine and naloxone in the mouse; naloxone-induced contractions in the electrically-stimulated and opiate-dependent isolated ileum of...

journal_title：British journal of pharmacology

authors： Brailowsky S,Guerrero-Muñoz F,Luján M,Shkurovich M

更新日期：1981-08-01 00:00:00

abstract：:1 The metabolism of prostacyclin (PGI2) and 6-keto prostaglandin F1 alpha (6-keto PGF1 alpha) was studied in cell-free homogenates of rat, rabbit and guinea-pig kidney. 2 Rabbit kidney converted both PGI2 and 6-keto PGF1 alpha to a stable metabolite with chromatographic and biological activity identical to that of aut...

journal_title：British journal of pharmacology

authors： Griffiths RJ,Moore PK

更新日期：1983-05-01 00:00:00

abstract：:The role of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) in the upper urinary tract of the guinea-pig and rat was examined using simultaneous tension recordings of the proximal and distal regions of the renal pelvis and the ureter. The guinea-pig upper urinary tract contracted at a frequency (7.52+/-0.3 min...

journal_title：British journal of pharmacology

authors： Davidson ME,Lang RJ

更新日期：2000-02-01 00:00:00

abstract：:Along with many other mammalian ATP-binding cassette (ABC) transporters, members of the ABCG group are involved in the regulated transport of hydrophobic compounds across cellular membranes. In humans, five ABCG family members have been identified, encoding proteins ranging from 638 to 678 amino acids in length. All f...

journal_title：British journal of pharmacology

authors： Kerr ID,Haider AJ,Gelissen IC

更新日期：2011-12-01 00:00:00

abstract：:1. This study analyses the neural pathway involved in the modulation of gastric motor function by stress. 2. Systemic administration of low doses of endotoxin (40 microg kg(-1), i.v.) prevents the increase in gastric tone induced by 2-deoxy-D-glucose (200 mg kg(-1), i.v., 2-DG) in urethane-anaesthetized rats. 3. Funct...

journal_title：British journal of pharmacology

authors： Quintana E,García-Zaragozá E,Martínez-Cuesta MA,Calatayud S,Esplugues JV,Barrachina MD

更新日期：2001-09-01 00:00:00

abstract：:1. The effects of palytoxin (PTX) isolated from Palythoa tubercurosa were tested on the isolated intra-arterially perfused spinal cord of the frog. The resting and evoked potentials were recorded by means of a sucrose-gap technique. 2. PTX caused a marked depolarization of both ventral and dorsal roots. The minimum ef...

journal_title：British journal of pharmacology

authors： Kudo Y,Shibata S

更新日期：1980-01-01 00:00:00

abstract：:1. The effects of 8-bromoguanosine 3':5'-cyclic monophosphate (8-bromo-cyclic GMP) on phenylephrine-induced contractions and phosphatidylinositol (PI) hydrolysis were investigated in rat isolated caudal artery. The effects of the nucleotide were compared to those of felodipine, a dihydropyridine Ca2+ channel antagonis...

journal_title：British journal of pharmacology

authors： Lum Min SA,Tabrizchi R

更新日期：1995-09-01 00:00:00

abstract：:The processes underpinning post-developmental neurogenesis in the mammalian brain continue to be defined. Such processes involve the proliferation of neural stem cells and neural progenitor cells (NPCs), neuronal migration, differentiation and integration into a network of functional synapses within the brain. Both in...

journal_title：British journal of pharmacology

authors： Prenderville JA,Kelly ÁM,Downer EJ

更新日期：2015-08-01 00:00:00

abstract：:1. The action of adrenaline on the K(+) balance of the isolated heart was found to depend on the ionic composition and the temperature of the perfusion fluids used.2. When the perfusion fluid contained 145 mM Na(+), 1.7 mM Ca(++) and 3-9 mM K(+), adrenaline caused the hearts to gain K(+); when the K(+) concentration w...

journal_title：British journal of pharmacology

authors： Stafford A

更新日期：1969-07-01 00:00:00

abstract：:1. To investigate the role of long-term stimulation of nicotinic acetylcholine receptors (AChRs) on the regulation of membrane potential, non-contracting C2C12 myotubes were stimulated for 1-4 days with carbachol (10 microM) and membrane potentials were measured by the intracellular microelectrode technique after wash...

journal_title：British journal of pharmacology

authors： Henning RH,Nelemans SA,van den Akker J,den Hertog A

更新日期：1994-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The thiazolidine carboxylic acid, BML-241, has been proposed as a lead compound in development of selective antagonists at the sphingosine-1-phosphate receptor (S1P3), based on its inhibition of the rise in intracellular calcium concentrations ([Ca2+]i) in HeLa cells overexpressing S1P receptors....

journal_title：British journal of pharmacology

authors： Jongsma M,Hendriks-Balk MC,Michel MC,Peters SL,Alewijnse AE

更新日期：2006-10-01 00:00:00

abstract：:1. The role of adenosine 3':5'-cyclic monophosphate (cyclic AMP) in the regulation of catecholamine (CA) secretion in chromaffin cells remains equivocal from previous studies. 2. In the present study the effect of this cyclic nucleotide on basal CA secretion, as well as on intracellular calcium and membrane potential ...

journal_title：British journal of pharmacology

authors： Parramón M,González MP,Oset-Gasque MJ

更新日期：1995-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide reduces uterine contractility and is of potential interest as a treatment for uterine disorders. The aim of this study was to explore the mechanism of sodium sulphide (Na2 S)-induced relaxation of rat uterus, investigate the importance of redox effects and ion channel-mediated m...

journal_title：British journal of pharmacology

authors： Mijušković A,Kokić AN,Dušić ZO,Slavić M,Spasić MB,Blagojević D

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic fatty liver disease (NAFLD) is considered to be one of the most common chronic liver diseases across worldwide. Astaxanthin (Ax) is a carotenoid, and beneficial effects of astaxanthin, including anti-oxidative, anti-inflammatory, and anti-tumour activity, have been identified. The p...

journal_title：British journal of pharmacology

authors： Wu L,Mo W,Feng J,Li J,Yu Q,Li S,Zhang J,Chen K,Ji J,Dai W,Wu J,Xu X,Mao Y,Guo C

更新日期：2020-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Postsystolic wall thickening (PSWT) is part of thickening that occurs after end-systole and represents wasted effort as it does not contribute to ejection. The effects of antianginal drugs on PSWT remain to be established. We compared the effects on PSWT of two agents that reduce heart rate, the ...

journal_title：British journal of pharmacology

authors： Lucats L,Ghaleh B,Colin P,Monnet X,Bizé A,Berdeaux A

更新日期：2007-02-01 00:00:00

abstract：:Among the five human 5-HT(4) (h5-HT(4)) receptor isoforms, the h5-HT(4(a)) receptor was studied with a particular emphasis on the molecular interactions involved in ligand binding. For this purpose, we used site-directed mutagenesis of the transmembrane domain. Twelve mutants were constructed with a special focus on t...

journal_title：British journal of pharmacology

authors： Mialet J,Dahmoune Y,Lezoualc'h F,Berque-Bestel I,Eftekhari P,Hoebeke J,Sicsic S,Langlois M,Fischmeister R

更新日期：2000-06-01 00:00:00

abstract：:The concentration of intracellular free Ca2+ ( [Ca2+]i) in human blood platelets was measured by use of the fluorescent probe quin-2. 5-Hydroxytryptamine (5-HT) caused a rapid increase of [Ca2+]i in the presence or absence of Ca2+ in the medium. The [Ca2+]i-rise was less marked in the absence of Ca2+ and could be anta...

journal_title：British journal of pharmacology

authors： Erne P,Pletscher A

更新日期：1985-02-01 00:00:00

abstract：:1 We previously reported that four lignans isolated from the bark of Machilus thunbergii Sieb. et Zucc. (Lauraceae) protected primary cultures of rat cortical neurons from neurotoxicity induced by glutamate. 2 Among the lignans, meso-dihydroguaiarectic acid (MDGA) and licarin A significantly attenuated glutamate-induc...

journal_title：British journal of pharmacology

authors： Ma CJ,Kim SR,Kim J,Kim YC

更新日期：2005-11-01 00:00:00