TC Mps1 12, a novel Mps1 inhibitor, suppresses the growth of hepatocellular carcinoma cells via the accumulation of chromosomal instability.

abstract：:1. We have investigated the effect of phorbol esters and the down-regulation of protein kinase C on contraction of guinea-pig ileum longitudinal smooth muscle to carbachol and high K+. 2. Phorbol 12,13-dibutyrate (PDBu) enhanced the phasic component and inhibited or enhanced, respectively, the tonic component of contr...

journal_title：British journal of pharmacology

authors： Sasaguri T,Watson SP

更新日期：1989-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Resurgence in the use of chloroquine as a potential treatment for COVID-19 has seen recent cases of fatal toxicity due to unintentional overdoses. Protocols for the management of poisoning recommend diazepam, although there are uncertainties in its pharmacology and efficacy in this context. The a...

journal_title：British journal of pharmacology

authors： Hughes DA

更新日期：2020-11-01 00:00:00

abstract：:1. Acute moderate hypoxia modifies the catalytic activity and expression of certain isoenzymes of hepatic cytochrome P450 (P450). The aim of this study was to document whether hypoxia affects hepatic P450 directly or through the release of serum mediators. 2. Rabbits were subjected to a FiO(2) of 8% for 48 h, sacrific...

journal_title：British journal of pharmacology

authors： Fradette C,Bleau AM,Pichette V,Chauret N,Du Souich P

更新日期：2002-11-01 00:00:00

abstract：:1. Turning behaviour after unilateral lesions of the nigro-striatal dopamine pathway in rats has been used to compare the actions of cocaine and desipramine on central dopamine-containing neurones.2. Administration of cocaine alone (5-20 mg/kg) resulted in no turning or minimal turning towards the lesioned side; the m...

journal_title：British journal of pharmacology

authors： Christie JE,Crow TJ

更新日期：1973-01-01 00:00:00

abstract：:1. The purpose of the present study was to develop an experimental strategy for the quantification of the cardiovascular effects of non-selective adenosine receptor ligands at the adenosine A1 and A2a receptor in vivo. 2-Chloroadenosine (CADO) was used as a model compound. 2. Three groups of normotensive conscious rat...

journal_title：British journal of pharmacology

authors： Mathoôt RA,Soudijn W,Breimer DD,Ijzerman AP,Danhof M

更新日期：1996-05-01 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：:We have characterized the contribution of endothelial nitric oxide synthase (eNOS), cyclo-oxygenase (COX) and cytochrome P450 (CYP450) to the bradykinin (BK)- induced vasodilation in isolated hearts from wildtype (WT) and eNOS deficient mice (eNOS-/-). The endothelium-dependent vasodilation by bradykinin (BK, 1 microM...

journal_title：British journal of pharmacology

authors： Ding Z,Gödecke A,Schrader J

更新日期：2002-02-01 00:00:00

abstract：:1 The prostaglandin synthesizing enzymes were found to be present in fat cell ghosts isolated from rabbit adipose tissue. 2 Prostaglandin E2 (PGE2) and PGF2, were synthesized by ghosts after stimulation with adrenocorticotrophic hormone (ACTH). 3 Indomethacin was found to inhibit this synthesis but not the synthesis o...

journal_title：British journal of pharmacology

authors： Lewis GP,Piper PJ,Vigo C

更新日期：1979-11-01 00:00:00

abstract：:1. Using a guinea-pig model of allergic asthma, in which the animals display early (0-5 h) and late phase (8-23 h after antigen challenge) bronchoconstrictor reactions, the function of prejunctional inhibitory M2 and postjunctional M3 receptors in isolated tracheal preparations have been investigated. In addition, car...

journal_title：British journal of pharmacology

authors： ten Berge RE,Santing RE,Hamstra JJ,Roffel AF,Zaagsma J

更新日期：1995-02-01 00:00:00

abstract：:1. Sympathetic neurotransmission and noradrenaline content of the tail artery of Wistar rats treated for 7 days with the adenosine antagonist, 1,3-dipropyl-8-sulphophenylxanthine (DPSPX), were examined. 2. Systolic blood pressure of the DPSPX-treated rats (164.0 +/- 2.9 mmHg; n = 6) was significantly greater than sali...

journal_title：British journal of pharmacology

authors： Karoon P,Rubino A,Burnstock G

更新日期：1995-09-01 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. 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：BACKGROUND AND PURPOSE:β-Adrenoceptor stimulation induces glucose uptake in several insulin-sensitive tissues by poorly understood mechanisms. EXPERIMENTAL APPROACH:We used a model system in CHO-K1 cells expressing the human β(2)-adrenoceptor and glucose transporter 4 (GLUT4) to investigate the signalling mechanisms i...

journal_title：British journal of pharmacology

authors： Dehvari N,Hutchinson DS,Nevzorova J,Dallner OS,Sato M,Kocan M,Merlin J,Evans BA,Summers RJ,Bengtsson T

更新日期：2012-03-01 00:00:00

abstract：:1. The effect of 1-aminocyclopropanecarboxylic acid (ACPC), a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex that exhibits neuroprotective, anxiolytic and antidepressant-like actions, was investigated in a functional assay for presynaptic NMDA receptors. 2. NMDA (100 microM) pr...

journal_title：British journal of pharmacology

authors： Clos MV,Garcia Sanz A,Trullas R,Badia A

更新日期：1996-06-01 00:00:00

abstract：:1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency...

journal_title：British journal of pharmacology

authors： Newbould BB

更新日期：1969-03-01 00:00:00

abstract：:A large range of neuroadaptations develop in response to chronic opioid exposure and these are thought to be more or less critical for expression of the major features of opioid addiction: tolerance, withdrawal and processes that may contribute to compulsive use and relapse. This review considers these adaptations at ...

journal_title：British journal of pharmacology

authors： Christie MJ

更新日期：2008-05-01 00:00:00

abstract：UNLABELLED:1. The release of somatostatin-like immunoreactivity (SRIF-LI) in the human brain was studied in synaptosomal preparations from fresh neocortical specimens obtained from patients undergoing neurosurgery to remove deeply sited tumours. 2. The basal outflow of SRIF-LI from superfused synaptosomes was increased...

journal_title：British journal of pharmacology

authors： Bonanno G,Gemignani A,Schmid G,Severi P,Cavazzani P,Raiteri M

更新日期：1996-07-01 00:00:00

abstract：:1 gamma-Aminobutyric acid (GABA, 0.1 to 1 mM) had no significant effect on the amplitude, rise time, half decay time or frequency of miniature endplate potentials (m.e.p.ps) at the frog or mouse neuromuscular junctions in vitro. 2 Addition of GABA (1 mM) to preparations previously treated with 11 mM K+-Ringer did not ...

journal_title：British journal of pharmacology

authors： Smart TG

更新日期：1980-01-01 00:00:00

abstract：:1. Phenylephrine-induced contractions of rabbit isolated trigone and urethra were antagonized in a competitive manner by alfuzosin (pA2 7.44 and 7.30, respectively) and prazosin. 2. The characteristics of [3H]-prazosin binding to human prostatic adenoma tissue were evaluated. [3H]-prazosin was potently displaced by al...

journal_title：British journal of pharmacology

authors： Lefèvre-Borg F,O'Connor SE,Schoemaker H,Hicks PE,Lechaire J,Gautier E,Pierre F,Pimoule C,Manoury P,Langer SZ

更新日期：1993-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Rhythmical transient constrictions of the lymphatic vessels provide the means for efficient lymph drainage and interstitial tissue fluid balance. This activity is critical during inflammation, to avoid or limit oedema resulting from increased vascular permeability, mediated by the release of vari...

journal_title：British journal of pharmacology

authors： Rehal S,Blanckaert P,Roizes S,von der Weid PY

更新日期：2009-12-01 00:00:00

abstract：:1. The contribution of nitric oxide (NO) and vasoactive intestinal polypeptide (VIP) to non-adrenergic non-cholinergic (NANC) relaxations in the pig gastric fundus was investigated. 2. Circular and longitudinal muscle strips were mounted for isotonic registration in the presence of atropine and guanethidine; tone was ...

journal_title：British journal of pharmacology

authors： Lefebvre RA,Smits GJ,Timmermans JP

更新日期：1995-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The endocannabinoid system and the cannabinoid CB(1) receptor have been identified in human sperm, and it is well known that endocannabinoids have pronounced adverse effects on male and female reproduction. In order to elucidate further the pathophysiological role of the endocannabinoid system in...

journal_title：British journal of pharmacology

authors： Aquila S,Guido C,Santoro A,Gazzerro P,Laezza C,Baffa MF,Andò S,Bifulco M

更新日期：2010-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of this study was to determine whether the apelin/APJ system is altered in human cardiovascular disease by investigating whether the expression of apelin or its receptor is altered at the protein level. EXPERIMENTAL APPROACH:Radioligand binding studies were used to determine apelin recep...

journal_title：British journal of pharmacology

authors： Pitkin SL,Maguire JJ,Kuc RE,Davenport AP

更新日期：2010-08-01 00:00:00

abstract：:1. To clarify the role of the first thrombin receptor/protease-activated receptor (PAR)-1 in an inflammatory process, we tested and characterized the effect of intraplantar (i.pl.) administration of the highly specific PAR-1 agonist TFLLR-NH2 in rat hindpaw. 2. TFLLR-NH2 administered i.pl. at 0.01-0.03 micromol per pa...

journal_title：British journal of pharmacology

authors： Kawabata A,Kuroda R,Nishikawa H,Asai T,Kataoka K,Taneda M

更新日期：1999-04-01 00:00:00

abstract：:1 The possible involvement of N-methyl-D-aspartate (NMDA)-receptors in epileptiform synaptic activity in the kainic acid (KA) lesioned hippocampus was investigated. In this chronic model of epilepsy there is a loss of both the early and the late components of synaptic inhibition as well as changes in the membrane prop...

journal_title：British journal of pharmacology

authors： Ashwood TJ,Wheal HV

更新日期：1987-08-01 00:00:00

abstract：:1. In the present study, we describe the expression of the neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (PACAP) as well as their receptors in PC-3 cells, a human prostate cancer cell line. In addition, we have investigated their role in apoptosis induced by s...

journal_title：British journal of pharmacology

authors： Gutiérrez-Cañas I,Rodríguez-Henche N,Bolaños O,Carmena MJ,Prieto JC,Juarranz MG

更新日期：2003-07-01 00:00:00

abstract：:The sequence similarity within the amino-terminal regions of parathyroid hormone (PTH) and PTH-related protein (PTHrP) allows the two to share actions at a common site, the PTH1 receptor. A number of biological activities have been ascribed to actions of other domains within PTHrP. PTHrP production by late stage breas...

journal_title：British journal of pharmacology

authors： Martin TJ,Johnson RW

更新日期：2019-05-14 00:00:00

abstract：:The muscarinic receptor binding of trazodone, a new nontricyclic antidepressant, was compared with established tricyclic antidepressants. The ability to inhibit the binding of [3H]-quinuclidinyl benzilate in vitro was used for comparing atropine-like effects. Trazodone was found to have essentially no activity at the ...

journal_title：British journal of pharmacology

authors： Hyslop DK,Taylor DP

更新日期：1980-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hyperbilirubinaemia and cholestasis are two major forms of liver abnormality. The Chinese herb Yin Chin has been used for thousands of years to treat liver dysfunctions. In mice, this herb and its principal ingredient scoparone were found to accelerate the clearance of bilirubin accompanied by th...

journal_title：British journal of pharmacology

authors： Yang D,Yang J,Shi D,Deng R,Yan B

更新日期：2011-11-01 00:00:00

abstract：:1. Catecholamine release from cat adrenal glands perfused at a high rate (4 ml min-1) at 37 degrees C with modified Krebs solutions lacking Ca and containing 1.2 mM K (hyperpolarizing solution) or 118 mM K (depolarizing solution) was triggered by 10-s pulses of Ca (0.5 mM) in the presence of 118 mM K. Hyperpolarized g...

journal_title：British journal of pharmacology

authors： López MG,Moro MA,Castillo CF,Artalejo CR,García AG

更新日期：1989-03-01 00:00:00