A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord.

abstract：BACKGROUND AND PURPOSE:Subunit-specific modulators of gamma-aminobutyric acid (GABA) type A (GABA(A)) receptors can help to assess the physiological function of receptors with different subunit composition and also provide the basis for the development of new drugs. Valerenic acid (VA) was recently identified as a beta...

journal_title：British journal of pharmacology

authors： Khom S,Strommer B,Ramharter J,Schwarz T,Schwarzer C,Erker T,Ecker GF,Mulzer J,Hering S

更新日期：2010-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Conventional determination of agonist efficacy at G-protein coupled receptors is measured by stimulation of guanosine-5'-γ-thiotriphosphate (GTPγS) binding. We analysed the role of guanosine diphosphate (GDP) in the process of activation of the M₂ muscarinic acetylcholine receptor and provide evi...

journal_title：British journal of pharmacology

authors： Jakubík J,Janíčková H,El-Fakahany EE,Doležal V

更新日期：2011-03-01 00:00:00

abstract：:1. ATP, UTP, ADP and ADP-beta-S elicited Ca2+ -signals in cultured aortic smooth muscle cells although ADP, UDP and ADP-beta-S gave approximately 40% of the maximal response seen with ATP and UTP. Adenosine, AMP or alpha,beta-methylene-ATP had no effect. These responses were attributed to P2Y2/4 and P2Y1 receptors, wh...

journal_title：British journal of pharmacology

authors： Pediani JD,McGrath JC,Wilson SM

更新日期：1999-04-01 00:00:00

abstract：:1. Effects were studied of 6-(3-dimethylaminopropionyl) forskolin (NKH477), a water-soluble forskolin derivative and of dibutyryl-cyclic AMP, a membrane-permeable cyclic AMP analogue on noradrenaline (NA)-induced Ca2+ mobilization in smooth muscle strips of the rabbit mesenteric artery. The intracellular concentration...

journal_title：British journal of pharmacology

authors： Ito S,Suzuki S,Itoh T

更新日期：1993-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:NO-mediated, endothelium-dependent relaxations of isolated arteries are blunted by ageing and high-fat diets, as well as by apolipoprotein E deletion. The present study was designed to test the hypothesis that apolipoprotein E deletion impairs endothelium-dependent responses to prostacyclin (IP) ...

journal_title：British journal of pharmacology

authors： Cheng Y,Vanhoutte PM,Leung SWS

更新日期：2018-09-01 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：:The effects of a new selective beta1-adrenoceptor agonist, (--)-1-(4-hydroxyphenoxy)-3-isopropyl-amino-propanol-2-hydrochloride (H 133/22), on amylase secretion from the rat parotid gland were investigated in an in vitro system. The results were compared to the secretory responses obtained with noradrenaline, adrenali...

journal_title：British journal of pharmacology

authors： Carlsöö B,Danielsson A,Henriksson R

更新日期：1978-03-01 00:00:00

abstract：:1. The psychoactive cannabinoids (-)-delta 9-tetrahydrocannabinol ((-)-delta 9-THC) and the 1,1-dimethyl-heptyl homologue of (-)-11-hydroxy-delta 8-tetrahydrocannabinol ((-)-DMH) both inhibited electrically-evoked contractions of the mouse isolated vas deferens and the myenteric plexus-longitudinal muscle preparation ...

journal_title：British journal of pharmacology

authors： Pertwee RG,Stevenson LA,Elrick DB,Mechoulam R,Corbett AD

更新日期：1992-04-01 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：:Intraperitoneal and intracerebral injections of methyl beta-carboline-3-carboxylate (beta CCM) and intracerebral injections of RO 15-1788 were given to rats. The performance of the rats in the social interaction test was measured to determine if changes in social interaction induced by beta CCM were mediated in part b...

journal_title：British journal of pharmacology

authors： Hindley SW,Hobbs A,Paterson IA,Roberts MH

更新日期：1985-11-01 00:00:00

abstract：:1. We studied the effects of various K+ channel blockers on the vasodilator responses of guinea-pig isolated basilar arteries to nitrergic nerve stimulation, the nitric oxide (NO) donor sodium nitroprusside (SNP), and the membrane permeable guanosine-3',5'-cyclic monophosphate (cyclic GMP) analogue 8-bromo-cyclic GMP ...

journal_title：British journal of pharmacology

authors： Jiang F,Li CG,Rand MJ

更新日期：1998-01-01 00:00:00

abstract：:1 Contractions of the cat nictitating membrane were elicited on stimulation of the internal carotid nerve, and the effects were studied of desipramine and two inhibitors of catechol-O-methyltransferase, U-0521 and pyrogallol, on the subsequent relaxation of the muscle. 2 The relaxation of the nictitating membrane occu...

journal_title：British journal of pharmacology

authors： Eccles R,Maclean AG

更新日期：1978-04-01 00:00:00

abstract：BACKGROUNDS AND PURPOSE:Lactic acidosis is a fatal adverse effect of metformin, but the risk factor remains unclear. Multidrug and toxin extrusion 1 (MATE1) is expressed in the luminal membrane of the kidney and liver. MATE1 was revealed to be responsible for the tubular and biliary secretion of metformin. Therefore, s...

journal_title：British journal of pharmacology

authors： Toyama K,Yonezawa A,Masuda S,Osawa R,Hosokawa M,Fujimoto S,Inagaki N,Inui K,Katsura T

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The type-5 PDE inhibitor vardenafil reduces myocardial infarct size in situ, following ischemia/reperfusion, when applied at reperfusion in animal models. Little is known about the underlying protective signaling. Here, we test whether vardenafil is protective in rat isolated hearts and in a cell...

journal_title：British journal of pharmacology

authors： Maas O,Donat U,Frenzel M,Rütz T,Kroemer HK,Felix SB,Krieg T

更新日期：2008-05-01 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：:1 Cellulose sulphate, like heparin, prolonged the clotting time in partial thromboplastin time (PTT) assays, inhibited the amidolytic activity of thrombin, was without effect on amidolysis catalysed by activated coagulation factor X(Xa), and potentiated the inhibition of both thrombin and Xa by antithrombin III (AT). ...

journal_title：British journal of pharmacology

authors： Kindness G,Long WF,Williamson FB

更新日期：1980-04-01 00:00:00

abstract：:1. Vasorelaxant properties of three nitric oxide (NO) donor drugs (glyceryl trinitrate, sodium nitroprusside and spermine NONOate) in mouse aorta (phenylephrine pre-contracted) were compared with those of endothelium-derived NO (generated with acetylcholine), NO free radical (NO*; NO gas solution) and nitroxyl ion (NO...

journal_title：British journal of pharmacology

authors： Wanstall JC,Jeffery TK,Gambino A,Lovren F,Triggle CR

更新日期：2001-10-01 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：BACKGROUND AND PURPOSE:While the slow delayed rectifier K(+) current (I(Ks)) is known to be enhanced by the stimulation of β-adrenoceptors in several mammalian species, phosphorylation-dependent regulation of the rapid delayed rectifier K(+) current (I(Kr)) is controversial. EXPERIMENTAL APPROACH:In the present study,...

journal_title：British journal of pharmacology

authors： Harmati G,Bányász T,Bárándi L,Szentandrássy N,Horváth B,Szabó G,Szentmiklósi JA,Szénási G,Nánási PP,Magyar J

更新日期：2011-02-01 00:00:00

abstract：:1. To investigate the role of nitric oxide in epilepsy we have studied the effects of agents which affect nitric oxide synthesis in sound-induced seizures in DBA/2 mice and in genetically epilepsy-prone (GEP) rats. 2. The neuronal selective nitric oxide synthase inhibitor, 7-nitroindazole (7-NI) is anticonvulsant in t...

journal_title：British journal of pharmacology

authors： Smith SE,Man CM,Yip PK,Tang E,Chapman AG,Meldrum BS

更新日期：1996-09-01 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. This study sets out to examine the effect of rilmenidine administered systemically on basal and reflexly activated renal nerve activity in Wistar and stroke prone spontaneously hypertensive rats (SHRSP). 2. Animals were anaesthetized with chloralose/urethane, stimulating electrodes were placed on the brachial plexi...

journal_title：British journal of pharmacology

authors： Zhang T,Johns EJ

更新日期：1996-11-01 00:00:00

abstract：:The nature of the neurohypophyseal peptide receptor in the anococcygeus muscles from male mice was investigated. The rank order of potency of naturally occurring peptides was oxytocin greater than Arg-vasotocin greater than Arg-vasopressin greater than Lys-vasopressin, which is similar to that found in the uterus and ...

journal_title：British journal of pharmacology

authors： Gibson A

更新日期：1986-05-01 00:00:00

abstract：:Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. In this study, the effects of TAK-147 at 2 mg kg(-1) p.o. for 21 days, compared t...

journal_title：British journal of pharmacology

authors： Hatip-Al-Khatib I,Iwasaki K,Yoshimitsu Y,Arai T,Egashira N,Mishima K,Ikeda T,Fujiwara M

更新日期：2005-08-01 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：:Since December 2019 SARS-Cov-2 was found responsible for the disease COVID-19, which has spread worldwide. No specific therapies/vaccines are yet available for the treatment of COVID-19. Drug repositioning may offer a strategy and a number of drugs have been repurposed, including lopinavir/ritonavir, remdesivir, favip...

journal_title：British journal of pharmacology

authors： Scavone C,Brusco S,Bertini M,Sportiello L,Rafaniello C,Zoccoli A,Berrino L,Racagni G,Rossi F,Capuano A

更新日期：2020-11-01 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：:Cartilage destruction is a key characteristic of arthritic disease, a process now widely established to be mediated by metzincins such as MMPs. Despite showing promise in preclinical trials during the 1990s, MMP inhibitors for the blockade of extracellular matrix turnover in the treatment of cancer and arthritis faile...

journal_title：British journal of pharmacology

authors： Wilkinson DJ,Arques MDC,Huesa C,Rowan AD

更新日期：2019-01-01 00:00:00

abstract：:The aim of the present study was to determine whether inhibition of cyclic nucleotide phosphodiesterase (PDE) modulates the stimulated generation of the cytokines, interleukin-4 (IL-4) and IL-13, from human basophils. This was addressed by evaluating the effects of both nonselective and selective inhibitors of PDEs on...

journal_title：British journal of pharmacology

authors： Eskandari N,Wickramasinghe T,Peachell PT

更新日期：2004-08-01 00:00:00

abstract：:1. The purpose of the present study was to identify and investigate the role of 5-hydroxytryptamine3 (5-HT3) receptors in the area postrema in the control of cisplatin-induced emesis in the ferret. 2. Homogenate binding and autoradiography experiments using the high affinity 5-HT3 receptor ligand, [3H]-GR65630, identi...

journal_title：British journal of pharmacology

authors： Higgins GA,Kilpatrick GJ,Bunce KT,Jones BJ,Tyers MB

更新日期：1989-05-01 00:00:00