The TRPM4 channel inhibitor 9-phenanthrol.

abstract：:1. The ability of PD 128907 to activate dopamine receptors in the ventral tegmental area, substantia nigra pars compacta, and striatum was investigated by use of in vitro electrophysiological recording and fast cyclic voltammetry. The affinity of a novel D2 selective antagonist L-741,626 for receptors activated by thi...

journal_title：British journal of pharmacology

authors： Bowery BJ,Razzaque Z,Emms F,Patel S,Freedman S,Bristow L,Kulagowski J,Seabrook GR

更新日期：1996-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An innovative chemical approach, named peptide welding technology (PWT), allows the synthesis of multibranched peptides with extraordinary high yield, purity and reproducibility. With this approach, three different tetrabranched derivatives of nociceptin/orphanin FQ (N/OFQ) have been synthesized ...

journal_title：British journal of pharmacology

authors： Rizzi A,Malfacini D,Cerlesi MC,Ruzza C,Marzola E,Bird MF,Rowbotham DJ,Salvadori S,Guerrini R,Lambert DG,Calo G

更新日期：2014-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Arachidonyl trifluoromethyl ketone (ATK) is widely used as an inhibitor of cytosolic group IV phospholipase A(2) (cPLA(2)) and calcium-independent group VI phospholipase A(2) (iPLA(2)). ATK thus reduces arachidonic acid (AA) substrate for cyclooxygenase (COX; also known as prostaglandin H synthas...

journal_title：British journal of pharmacology

authors： Leis HJ,Windischhofer W

更新日期：2008-11-01 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：:Recent advances have improved our understanding of the renin-angiotensin system (RAS). These have included the recognition that angiotensin (Ang)-(1-7) is a biologically active product of the RAS cascade. The identification of the ACE homologue ACE2, which forms Ang-(1-7) from Ang II, and the GPCR Mas as an Ang-(1-7) ...

journal_title：British journal of pharmacology

authors： Simões e Silva AC,Silveira KD,Ferreira AJ,Teixeira MM

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT (serotonin) regulates various physiological functions, both directly and via enteric neurons. The present study investigated the role of endogenous 5-HT and 5-HT3 receptors in the pathogenic mechanisms involved in colonic inflammation, especially in relation to substance P (SP) and the neuro...

journal_title：British journal of pharmacology

authors： Utsumi D,Matsumoto K,Amagase K,Horie S,Kato S

更新日期：2016-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H2 S) is an endogenous gaseous signalling molecule with putative functions in gastrointestinal motility regulation. Characterization of H2 S effects on colonic motility is crucial to establish its potential use as therapeutic agent in the treatment of colonic disorders. EXPERI...

journal_title：British journal of pharmacology

authors： Gil V,Parsons S,Gallego D,Huizinga J,Jimenez M

更新日期：2013-05-01 00:00:00

abstract：:1. This study exploited established immunoneutralization protocols and an N-terminal annexin 1 peptide (annexin 1(Ac2 - 26)) to advance our knowledge of the role of annexin 1 as a mediator of acute glucocorticoid action in the rat neuroendocrine system in vivo. 2. Rats were treated with corticosterone (500 microg kg(-...

journal_title：British journal of pharmacology

authors： Philip JG,John CD,Cover PO,Morris JF,Christian HC,Flower RJ,Buckingham JC

更新日期：2001-10-01 00:00:00

abstract：:1,2,3,4-Tetrahydro-9-aminoacridine (THA) has an inhibitory effect on the activity of acetylcholinesterase which has led to its use in the treatment of Alzheimer's disease. Other actions of THA include the inhibition of voltage-dependent ion channels. In this paper we describe the effect of THA on the depolarization-in...

journal_title：British journal of pharmacology

authors： de Belleroche J,Gardiner IM

更新日期：1988-08-01 00:00:00

abstract：:1. The modulation of L-type calcium channel current (ICa) by fendiline, a diphenylalkylamine type of calcium channel blocker was investigated on guinea-pig ventricular myocytes by use of the whole-cell patch-clamp technique. 2. Fendiline-induced block of ICa is accompanied by modulation of the channel kinetics in a co...

journal_title：British journal of pharmacology

authors： Schreibmayer W,Tripathi O,Tritthart HA

更新日期：1992-05-01 00:00:00

abstract：:(1) We have investigated the properties of native and haemagglutinin (HA)-tagged neuropeptide Y (NPY) Y(1) receptors after mutation of the palmitoylation site Cys(337) to Ser or Ala. (2) In Chinese hamster ovary cells expressing similar receptor levels, the C337A mutation abolished incorporation of [(3)H]palmitic acid...

journal_title：British journal of pharmacology

authors： Holliday ND,Cox HM

更新日期：2003-06-01 00:00:00

abstract：:1. [125I]-Tyr4-bombesin exhibited saturable binding to pancreatic acinar cells. 2. Preincubation of cells at 37 degrees C with 0.03 nM-1 microM-bombesin for 10 min followed by acid or neutral washes reduced subsequent binding of [125I]-Tyr4-bombesin in a concentration-dependent manner by up to 90%. 3. In cell suspensi...

journal_title：British journal of pharmacology

authors： Sjödin L,Gylfe E

更新日期：1994-08-01 00:00:00

abstract：:We have recently shown that in polymorphonuclear leukocytes, 11-keto boswellic acids (KBAs) induce Ca2+ mobilisation and activation of mitogen-activated protein kinases (MAPK). Here we addressed the effects of BAs on central signalling pathways in human platelets and on various platelet functions. We found that beta-B...

journal_title：British journal of pharmacology

authors： Poeckel D,Tausch L,Altmann A,Feisst C,Klinkhardt U,Graff J,Harder S,Werz O

更新日期：2005-10-01 00:00:00

abstract：:The past two decades have seen an immense increase in our appreciation of the vast range of signalling processes and supporting machinery that occur in cells. Pivotal to this is the notion of signal compartmentalization (compartmentation). Targeting by protein domains is critical in allowing signalling complexes to be...

journal_title：British journal of pharmacology

authors： Houslay MD

更新日期：2009-09-01 00:00:00

abstract：:1. The present study was aimed to determine whether propranolol improves contractile function of the ischaemic/reperfused heart through protection of the mitochondrial function during ischaemia. 2. Isolated perfused rat hearts were subjected to 35-min ischaemia followed by 60-min reperfusion. Pre-treatment with propra...

journal_title：British journal of pharmacology

authors： Iwai T,Tanonaka K,Kasahara S,Inoue R,Takeo S

更新日期：2002-06-01 00:00:00

abstract：:1. Effects of neuropeptides of the vasopressin family on Cl(-) secretion have not yet been reported in lung. Using the 16HBE14o- bronchial epithelial cell line, we investigated their action on Cl(-) secretion. 2. In symmetrical Cl(-) solutions, basolateral application of arginine vasotocin (AVT), oxytocin or isotocin ...

journal_title：British journal of pharmacology

authors： Bernard K,Bogliolo S,Ehrenfeld J

更新日期：2005-04-01 00:00:00

abstract：:1. A technique for the close-arterial administration of substances to the rat stomach in vivo has been developed. 2. Intra-arterial infusion of platelet-activating factor (Paf, 10-50 ng kg-1 min-1 for 10 min) induced macroscopically assessed damage in the corpus mucosa, characterized as vasocongestion and necrosis. 3....

journal_title：British journal of pharmacology

authors： Esplugues JV,Whittle BJ

更新日期：1988-01-01 00:00:00

abstract：:We investigated the rate of penetration into and the intra-relationship between the serum, cerebrospinal fluid (CSF) and regional brain extracellular fluid (bECF) compartments following systemic administration of lamotrigine in rat. The serum pharmacokinetics were biphasic with an initial distribution phase, (half-lif...

journal_title：British journal of pharmacology

authors： Walker MC,Tong X,Perry H,Alavijeh MS,Patsalos PN

更新日期：2000-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously demonstrated that paracetamol has to be metabolised in the brain by fatty acid amide hydrolase enzyme into AM404 (N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide) to activate CB1 receptors and TRPV1 channels, which mediate its analgesic effect. However, the brain mechanisms sup...

journal_title：British journal of pharmacology

authors： Barrière DA,Boumezbeur F,Dalmann R,Cadeddu R,Richard D,Pinguet J,Daulhac L,Sarret P,Whittingstall K,Keller M,Mériaux S,Eschalier A,Mallet C

更新日期：2020-04-01 00:00:00

abstract：:1. The possible involvement of nitric oxide (NO) in the induction and expression of morphine tolerance and dependence was studied in mice. A two-day repeated injection regimen was used to induce morphine tolerance and dependence. Tolerance was assessed by the tail flick test and physical dependence by naloxone challen...

journal_title：British journal of pharmacology

authors： Dambisya YM,Lee TL

更新日期：1996-03-01 00:00:00

abstract：:1. In Ca-free solution, the contractile response of guinea-pig taenia caecum to 10(-4) M carbachol was mediated through muscarinic receptors and was reduced time-dependently by desensitization with 10(-4) M carbachol, but not 10(-4) M histamine. On the other hand, the response to 10(-4) M histamine was shown to be med...

journal_title：British journal of pharmacology

authors： Hishinuma S,Uchida MK

更新日期：1988-07-01 00:00:00

abstract：:1. The putative alpha 1-adrenoceptor subtypes of rat cerebral cortex membranes were characterized in binding. 2. Specific binding of [3H]-prazosin was saturable between 20-5000 pm. Scatchard plots of the binding data were non-linear, indicating the presence of two distinct affinity sites for prazosin (pKD, high = 10.1...

journal_title：British journal of pharmacology

authors： Oshita M,Kigoshi S,Muramatsu I

更新日期：1991-12-01 00:00:00

abstract：:1. The interaction between endogenous nitric oxide (NO) and factors from the rat submandibular salivary gland such as epidermal growth factor (EGF) on gastric mucosal integrity in the rat has been investigated. 2. Bolus administration of the NO synthase inhibitor, NG nitro-L-arginine methyl ester (L-NAME; 6.25-50 mg k...

journal_title：British journal of pharmacology

authors： Tepperman BL,Soper BD

更新日期：1993-09-01 00:00:00

abstract：:1. Dose-dependent vasodilator responses to dopamine, isoprenaline, noradrenaline, 3-isobutyl-1-methylxanthine (IBMX) and sodium nitroprusside were obtained in isolated perfused mesentery preparations, taken from reserpine-treated rats of different ages. The preparations were pretreated with phenoxybenzamine (1 microM)...

journal_title：British journal of pharmacology

authors： Wanstall JC,O'Donnell SR

更新日期：1989-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Peptides from venomous animals have long been important for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide from the venom of the armed spider Phoneutria nigriventer, produces analgesia by blocking the TRPA1 channel. EXPERIMENTA...

journal_title：British journal of pharmacology

authors： Tonello R,Fusi C,Materazzi S,Marone IM,De Logu F,Benemei S,Gonçalves MC,Coppi E,Castro-Junior CJ,Gomez MV,Geppetti P,Ferreira J,Nassini R

更新日期：2017-01-01 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. The possibility that a purine nucleotide is involved in excitatory transmission to the urinary bladder has been tested. All the purine compounds tested which contained a pyrophosphate bond produced contraction, adenosine triphosphate (ATP) being the most potent. Adenosine and adenosine monophosphate caused relaxati...

journal_title：British journal of pharmacology

authors： Burnstock G,Dumsday B,Smythe A

更新日期：1972-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Oxaliplatin is a platinum-based chemotherapeutic drug used as a first-line therapy for colorectal cancer. However, its use is associated with severe gastrointestinal side-effects resulting in dose limitations and/or cessation of treatment. In this study, we tested whether oxidative stress, caused...

journal_title：British journal of pharmacology

authors： McQuade RM,Carbone SE,Stojanovska V,Rahman A,Gwynne RM,Robinson AM,Goodman CA,Bornstein JC,Nurgali K

更新日期：2016-12-01 00:00:00

abstract：:1. We investigated the role of adenosine 3':5'-cyclic monophosphate (cyclic AMP) in non-adrenergic non-cholinergic (NANC) contraction in guinea-pig bronchial strips. 2. Forskolin (3 nM to 1 microM) reduced NANC contraction induced by electrical field stimulation (EFS) in a concentration-dependent fashion (-log EC50 wa...

journal_title：British journal of pharmacology

authors： Aikawa T,Sekizawa K,Morikawa M,Itabashi S,Sasaki H,Takishima T

更新日期：1992-03-01 00:00:00

abstract：:1. The effects of prolonged cold storage on the mechanical and membranal responses to stimulation of alpha- and beta-adrenoceptors by phenylephrine and isoprenaline, respectively, were studied on the guinea-pig taenia caecum.2. Cold storage invariably caused a decrease in the resting membrane potential, and this effec...

journal_title：British journal of pharmacology

authors： Fukuda H,Shibata S

更新日期：1972-11-01 00:00:00