Identification and development of specific inhibitors for insulin-regulated aminopeptidase as a new class of cognitive enhancers.

abstract：:1. The sulphonylureas, tolbutamide (0.1-10 mM) and glibenclamide (0.1-100 microM) shown not to inhibit ATP-K+ channel currents when applied to inside-out membrane patches excised from rat cultured cerebral cortex or freshly-dispersed ventromedial hypothalamic nucleus (VMHN) neurones. 2. Saturable binding sites for [3H...

journal_title：British journal of pharmacology

authors： Ashford ML,Boden PR,Treherne JM

更新日期：1990-11-01 00:00:00

abstract：:Some 865 genes in man encode G-protein-coupled receptors (GPCRs). The heterotrimeric guanine nucleotide-binding proteins (G-proteins) function to transduce signals from this vast panoply of receptors to effector systems including ion channels and enzymes that alter the rate of production, release or degradation of int...

journal_title：British journal of pharmacology

authors： Milligan G,Kostenis E

更新日期：2006-01-01 00:00:00

abstract：:1. The effects of the intravenous injection of Kö 1173, a new anticonvulsant drug, phenytoin and procainamide were studied on three types of cardiac arrhythmia in dogs.2. Ventricular ectopic beats produced by intravenous injection of adrenaline in anaesthetized dogs respired with halothane were abolished by Kö 1173, 0...

journal_title：British journal of pharmacology

authors： Allen JD,Ekue JM,Shanks RG,Zaidi SA

更新日期：1972-08-01 00:00:00

abstract：:1. Propranolol, a beta-adrenoceptor blocking drug with local anaesthetic and a direct myocardial depressant action, and MJ 1999, a beta-adrenoceptor blocking drug which has no local anaesthetic or intrinsic sympathomimetic action, were compared for beta-adrenoceptor blocking activity in man.2. Propranolol was 2.67 tim...

journal_title：British journal of pharmacology

authors： Kofi Ekue JM,Lowe DC,Shanks RG

更新日期：1970-05-01 00:00:00

abstract：:1. The central and peripheral effects of the omega (benzodiazepine) site ligands, clonazepam, alpidem, zolpidem, triazolam, flumazenil, ethyl beta carboline-3-carboxylate (beta-CCE) and N-methyl beta carboline-3-carboxylate (beta-CCM) on intestinal myoelectrical activity were evaluated in conscious rats, chronically f...

journal_title：British journal of pharmacology

authors： Bonnafous C,Scatton B,Buéno L

更新日期：1994-09-01 00:00:00

abstract：:The N6-2'-O-dibutyryl derivative of adenosine 3',5'-monophosphate (db cyclic AMP) and related compounds have been micro-injected into the preoptic/anterior hypothalamic nuclei (PO/AH) of the unanaesthetized, restrained rabbit and the effects on deep body temperature observed. Db cyclic AMP (100-400 micrograms) produce...

journal_title：British journal of pharmacology

authors： Dascombe MJ

更新日期：1984-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Saponins isolated from Panax notoginseng (Burk.) F.H. Chen have been shown to relieve thrombogenesis and facilitate haemostasis. However, it is not known which saponin accounts for this haemostatic effect. Hence, in the present study we aimed to identify which saponins contribute to its haemostat...

journal_title：British journal of pharmacology

authors： Gao B,Huang L,Liu H,Wu H,Zhang E,Yang L,Wu X,Wang Z

更新日期：2014-01-01 00:00:00

abstract：:1 The actions of ethylenediamine (EDA) and structurally related compounds were investigated by microiontophoresis in Wistar rats. 2 EDA inhibited, via a bicuculline-sensitive mechanism, the spontaneous firing rate of all cortical and pallidal cells tested. 3 The results with the analogues suggest that two amine groups...

journal_title：British journal of pharmacology

authors： Perkins MN,Stone TW

更新日期：1982-01-01 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：BACKGROUND AND PURPOSE:The endocannabinoid, anandamide, has anti-arrhythmic effects. The aim of the present study was to explore the electrophysiological effects of anandamide on rat myocardium. EXPERIMENTAL APPROACH:Evoked action potentials (APs) were recorded using intracellular recording technique in rat cardiac pa...

journal_title：British journal of pharmacology

authors： Li Q,Ma HJ,Zhang H,Qi Z,Guan Y,Zhang Y

更新日期：2009-12-01 00:00:00

abstract：:In moderate-to-severe asthma, adding an inhaled long-acting β2 -adenoceptor agonist (LABA) to an inhaled corticosteroid (ICS) provides better disease control than simply increasing the dose of ICS. Acting on the glucocorticoid receptor (GR, gene NR3C1), ICSs promote anti-inflammatory/anti-asthma gene expression. In vi...

journal_title：British journal of pharmacology

authors： Newton R,Giembycz MA

更新日期：2016-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled glucocorticoid (ICS)/long-acting β2 -adrenoceptor agonist (LABA) combination therapy is a recommended treatment option for patients with moderate/severe asthma in whom adequate control cannot be achieved by an ICS alone. Previously, we discovered that LABAs can augment dexamethasone-induc...

journal_title：British journal of pharmacology

authors： Joshi T,Johnson M,Newton R,Giembycz MA

更新日期：2015-05-01 00:00:00

abstract：:The effect of adenosine on transepithelial ion transport was investigated in isolated preparations of murine trachea mounted in Ussing chambers. The possible regulation of adenosine receptors in an established model of allergic airway inflammation was also investigated. Mucosally applied adenosine caused increases in ...

journal_title：British journal of pharmacology

authors： Kornerup KN,Page CP,Moffatt JD

更新日期：2005-04-01 00:00:00

abstract：:1 Noradrenaline and clonidine were applied by microiontophoresis to single neurones in the cerebral cortex and medullary reticular formation of anaesthetized rats.2 Of a total of 247 neurones studied, 79% of medullary units and 60% of cortical units responded in the same manner to both noradrenaline and clonidine. The...

journal_title：British journal of pharmacology

authors： Anderson C,Stone TW

更新日期：1974-07-01 00:00:00

abstract：:1 The effects of pretreatment with aspirin, and of prostacyclin (PGI(2)) infusions, on responses to myocardial ischaemia and infarction produced by ligation of a coronary artery were investigated in conscious rats.2 Surgical preparation, under halothane anaesthesia, consisted of implanting exteriorized aortic and jugu...

journal_title：British journal of pharmacology

authors： Johnston KM,MacLeod BA,Walker MJ

更新日期：1983-01-01 00:00:00

abstract：:N-terminal labelled fluorescent BODIPY-NPY peptide analogues were tested in Y1, Y2, Y4 and Y5 receptor-binding assays performed in rat brain membrane preparations and HEK293 cells expressing the rat Y1, Y2, Y4 and Y5 receptors. BODIPY TMR/FL-[Leu31, Pro34]NPY/PYY were able to compete for specific [125][Leu31, Pro34]PY...

journal_title：British journal of pharmacology

authors： Dumont Y,Gaudreau P,Mazzuferi M,Langlois D,Chabot JG,Fournier A,Simonato M,Quirion R

更新日期：2005-12-01 00:00:00

abstract：:Allergic inflammatory responses contribute to the symptoms of a number of diseases including atopic dermatitis, asthma and rhinitis. Cationic proteins are released from inflammatory cells and levels are known to be raised in disease states. Using an in vivo model of acute inflammation, we investigated the characterist...

journal_title：British journal of pharmacology

authors： Jones H,Paul W,Page CP

更新日期：2001-08-01 00:00:00

abstract：:1 In cats anaesthetized with pentobarbitone and vagotomized, observations were made on the phrenic nerve action potential and the diaphragm electromyogram (EMG) at constant end-tidal Pco(2). Arterial blood pressure was stabilized by intravenous infusions of noradrenaline.2 Intravenous administration of saxitoxin (STX)...

journal_title：British journal of pharmacology

authors： Borison HL,Culp WJ,Gonsalves SF,McCarthy LE

更新日期：1980-02-01 00:00:00

abstract：:In intact mesenteric arteries, increasing [K(+)]o by 5 mM hyperpolarized both endothelial and smooth muscle cells. Subsequent exposure to 10 microM phenylephrine depolarized both cell types which were then repolarized by a 5 mM increase in [K(+)]o. In endothelium-denuded vessels, increasing [K(+)]o by 5 mM hyperpolari...

journal_title：British journal of pharmacology

authors： Richards GR,Weston AH,Burnham MP,Félétou M,Vanhoutte PM,Edwards G

更新日期：2001-09-01 00:00:00

abstract：:We performed intracellular recordings from a rat corticostriatal slice preparation in order to compare the electrophysiological effects of the classical antiepileptic drug (AED) phenytoin (PHT) and the new AEDs lamotrigine (LTG) and gabapentin (GBP) on striatal neurons. PHT, LTG and GBP affected neither the resting me...

journal_title：British journal of pharmacology

authors： Calabresi P,Centonze D,Marfia GA,Pisani A,Bernardi G

更新日期：1999-02-01 00:00:00

abstract：:1. Treatment of rat mesangial cells with interleukin 1 beta (IL-1 beta) or tumour necrosis factor alpha (TNF alpha) has been shown to induce a macrophage-type of nitric oxide (NO) synthase. Here we report that adenosine 3':5'-cyclic monophosphate (cyclic AMP) is another mediator that triggers induction of NO synthase ...

journal_title：British journal of pharmacology

authors： Mühl H,Kunz D,Pfeilschifter J

更新日期：1994-05-01 00:00:00

abstract：:Analogues of gamma-aminobutyric acid (GABA) incorporating an isothiouronium salt as a replacement for a protonated amino functional group have been investigated for activity on: GABA receptors in the guinea-pig ileum; [3H]-GABA and [3H]-diazepam binding to rat brain membranes; and GABA uptake and transamination. For t...

journal_title：British journal of pharmacology

authors： Allan RD,Dickenson HW,Hiern BP,Johnston GA,Kazlauskas R

更新日期：1986-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In patients with pulmonary hypertension (PH) associated with lung disease and/or hypoxia (Group III), decreased pulmonary vascular tone and tissue hypoxia is therapeutically beneficial. PGE2 and PGI2 induce potent relaxation of human bronchi from non-PH (control) patients via EP4 and IP receptors...

journal_title：British journal of pharmacology

authors： Ozen G,Benyahia C,Mani S,Boukais K,Silverstein AM,Bayles R,Nelsen AC,Castier Y,Danel C,Mal H,Clapp LH,Longrois D,Norel X

更新日期：2020-01-01 00:00:00

abstract：:We studied the effects of endothelium-derived relaxing factor (EDRF), bovine retractor penis muscle inhibitory factor and sodium nitroprusside, three stimulants of guanylate cyclase, on the in vitro aggregation of washed human platelets. Platelet aggregation induced either by collagen or by the thromboxane A2 analogue...

journal_title：British journal of pharmacology

authors： Furlong B,Henderson AH,Lewis MJ,Smith JA

更新日期：1987-04-01 00:00:00

abstract：:1 The effects of the putative 5-hydroxytryptamine (5-HT) receptor antagonists, methysergide, mianserin and methergoline, the dopamine receptor antagonists, haloperidol, thioridazine and clozapine, and the noradrenaline (NA) receptor antagonists, phentolamine, phenoxybenzamine and propranolol on the behavioural respons...

journal_title：British journal of pharmacology

authors： Dourish CT

更新日期：1982-09-01 00:00:00

abstract：:1. The ability of the nitric oxide (NO)-releasing aspirin, NCX 4016, to control vasoconstrictor responses induced by electrical field stimulation (TNS) or by exogenous norepinephrine (NE) was investigated in perfused rat tail artery with intact endothelium. 2. NCX 4016 (25, 50 and 100 microM) dose-dependently antagoni...

journal_title：British journal of pharmacology

authors： Rossoni G,Manfredi B,Del Soldato P,Berti F

更新日期：2002-09-01 00:00:00

abstract：:1. To determine the possible role of Ca(2+)-activated K+ (KCa) channels in the regulation of resting tone of arteries from spontaneously hypertensive rats (SHR), the effects of agents which interact with these channels on tension and 86Rb efflux were compared in endothelium-denuded strips of carotid, femoral and mesen...

journal_title：British journal of pharmacology

authors： Asano M,Masuzawa-Ito K,Matsuda T

更新日期：1993-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We have developed a strategy to target the permanently charged lidocaine derivative lidocaine N-ethyl bromide (QX-314) selectively into nociceptive sensory neurons through the large-pore transient receptor potential cation channel subfamily V (TRPV1) noxious heat detector channel. This involves c...

journal_title：British journal of pharmacology

authors： Roberson DP,Binshtok AM,Blasl F,Bean BP,Woolf CJ

更新日期：2011-09-01 00:00:00

abstract：:1. The pharmacological profile of LR-B/081, (methyl 2-[[4-butyl-2-methyl- 6-oxo-5-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6H)- pyrimidinyl]methyl]-3-thiophenecarboxylate), a novel antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. 2. In rabbit aortic strips incubated w...

journal_title：British journal of pharmacology

authors： Cirillo R,Renzetti AR,Cucchi P,Guelfi M,Salimbeni A,Caliari S,Castellucci A,Evangelista S,Subissi A,Giachetti A

更新日期：1995-03-01 00:00:00

abstract：:1. Possible interactions between non-steroidal anti-inflammatory drugs (NSAIDs) and endogenous opioids were examined in electrophysiological experiments in alpha-chloralose anaesthetized spinalized rats without or with carrageenan-induced acute inflammation of one hindpaw. Spinal reflex responses, monitored as single ...

journal_title：British journal of pharmacology

authors： Herrero JF,Headley PM

更新日期：1996-06-01 00:00:00